Dosing & Uses
Dosage Forms & Strengths
tablets, copackaged cartons
- Packaged for a 28-day medication cycle depending on the ribociclib daily dose
- 3 Blister packs, containing 21 tablets (200mg/tablet; 600mg daily dose) of ribociclib plus one 28-tablet count bottle of letrozole 2.5mg/tablet
- 3 Blister packs, containing 14 tablets (200mg/tablet; 400mg daily dose) of ribociclib plus one 28-tablet count bottle of letrozole 2.5mg/tablet
- 1 blister pack, containing 21 tablets (200mg/tablet; 200mg daily dose) of ribociclib plus one 28-tablet count bottle of letrozole 2.5mg/tablet
Breast Cancer
Indicated as initial endocrine-based therapy for the treatment of pre/perimenopausal, postmenopausal women, or men with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer
Ribociclib (initial dose): 600 mg PO qDay for 21 consecutive days followed by 7 days off treatment resulting in a 28-day cycle
Letrozole: 2.5 mg PO qDay taken through the 28-day cycle
Treat men or pre/perimenopausal women with a luteinizing hormone-releasing hormone (LHRH) agonist (eg, goserelin, leuprolide) according to clinical practice standards
Dosage Modifications (ribociclib)
Recommended dose modifications for adverse effects
- Starting dose: 600 mg/day
- First dose reduction: 400 mg/day
- Second dose reduction: 200 mg/day
- If further dose reduction below 200 mg/day is required, discontinue treatment
Neutropenia
- Grade 1-2 (ANC 1000/mm3 to
- Grade 3 (ANC 500 to <1000/mm3): Interrupt dose until recovery to Grade ≤2; resume at the same dose level; if toxicity recurs at Grade 3, interrupt dose until recovery, then resume at the next lower dose level
- Grade 3 febrile neutropenia (Grade 3 ANC with fever and/or concurrent infection): Dose interruption until recovery of neutropenia to Grade ≤2; resume at the next lower dose level
- Grade 4 (ANC <500/mm3): Dose interruption until recovery of neutropenia to Grade ≤2; resume at the next lower dose level
Hepatobiliary toxicity
-
AST and/or ALT increased from baseline WITHOUT increased total bilirubin >2 x ULN
- Grade 1 (>ULN to 3 x ULN): No dose adjustment required
- Grade 2 (>3-5 x ULN), baseline at
- Grade 2 (>3-5 x ULN), baseline at Grade 2: No dose interruption
- Grade 3 (>5-20 x ULN): Interrupt dose until recovery to baseline (or less) before initiating treatment, then resume at next lower dose level; if Grade 3 recurs, discontinue
- Grade 4 (>20 x ULN): Discontinue
-
AST and/or ALT increased from baseline WITH increased total bilirubin, in the absence of cholestasis
- Discontinue ribociclib if ALT and/or AST >3 x ULN plus total bilirubin >2 x ULN irrespective of baseline grade
QT prolongation
-
ECGs with QTcF >480 msec
- Interrupt treatment If QTcF resolves to <481 msec, resume treatment at same dose level
- If QTcF ≥481 msec recurs, interrupt dose until QTcF resolves to <481 msec; then resume at next lower dose level
-
ECGs with QTcF >500 msec
- Interrupt KISQALI treatment if QTcF greater than 500 msec on at least 2 separate ECGs (within same visit)
- If QTcF prolongation resolves to <481 msec, resume treatment at the next lower dose level
- Permanently discontinue if QTcF interval prolongation is either >500 msec or >60 msec change from baseline AND associated with any of the following: torsades de pointes, polymorphic ventricular tachycardia, unexplained syncope, or signs/symptoms of serious arrhythmia
Interstitial lung disease/pneumonitis (ILD)
- Grade 1 (asymptomatic): No dose interruption or adjustment required; initiate appropriate medical therapy and monitor as clinically indicated
- Grade 2 (symptomatic): Dose interruption until recovery to Grade ≤1 then consider resuming at the next lower dose level; if Grade 2 recurs, discontinue treatment
- Grade 3 (severe symptomatic) or 4 (life-threatening): Discontinue treatment
Other toxicities
- Grade 1 or 2: No dose adjustment is required; initiate appropriate medical therapy and monitor as clinically indicated
- Grade 3: Interrupt dose until recovery to Grade ≤1, then resume at the same dose level; if Grade 3 recurs, resume at the next lower dose level
- Grade 4: Discontinue
Coadministration with strong CYP3A inhibitors
- Avoid use with strong CYP3A inhibitors and consider an alternative drug with less potential for CYP3A inhibition
- If a strong CYP3A inhibitor must be coadministered, reduce ribociclib dose to 400 mg/day
- If the strong CYP3A inhibitor is discontinued, change ribociclib dose (after at least 5 half-lives of the strong CYP3A inhibitor) to the dose used before initiating the strong CYP3A inhibitor
Hepatic impairment
-
Ribociclib
- Mild (Child-Pugh class A): No dose adjustment necessary
- Moderate or severe (Child-Pugh classes B/C): Reduce starting dose to 400 mg/day
-
Letrozole
- Mild (Child-Pugh classes A/B): No dose adjustment necessary
- Patients with cirrhosis and severe hepatic dysfunction: Reduce dose by 50% (ie, 2.5 mg every other day)
- Noncirrhotic patients with elevated bilirubin levels have not been studied
Renal impairment
-
Ribociclib
- Mild-to-moderate (CrCl ≥30 mL/min): No dose adjustment necessary
- Severe (CrCl 15-30 mL/min): Decrease starting dose to 200 mg/day; only studied healthy subjects and noncancer subjects with severe renal impairment
-
Letrozole
- Mild-to-moderate (CrCl ≥30 mL/min): No dose adjustment necessary
- Severe (CrCl 10-30 mL/min): No dose adjustment necessary
Dosing Considerations (ribociclib)
Complete blood count (CBC)
- Perform CBC before initiating treatment
- Monitor CBC q2wk for the first 2 cycles, at the beginning of each subsequent 4 cycles, and as clinically indicated
Liver function tests (LFTs)
- Perform LFTs before initiating
- Monitor LFTs q2wk for the first 2 cycles, at the beginning of each subsequent 4 cycles, and as clinically indicated
- If Grade ≥2 abnormalities observed, more frequent monitoring is recommended
Electrocardiograms (ECGs) and electrolytes
- ECGs should be assessed prior to initiation of treatment
- Repeat ECGs at ~Day 14 of the first cycle and at the beginning of the second cycle, and as clinically indicated
- In case of (QTcF) prolongation at any given time during treatment, more frequent ECG monitoring is recommended
- Monitor serum electrolytes (including potassium, calcium, phosphorous and magnesium) before initiating, at the beginning of the first 6 cycles, and as clinically indicated; correct any abnormality before starting ribociclib
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (13)
- aprepitant
ribociclib will increase the level or effect of aprepitant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- budesonide
ribociclib will increase the level or effect of budesonide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- conivaptan
ribociclib will increase the level or effect of conivaptan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- elvitegravir
ribociclib will increase the level or effect of elvitegravir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- fluconazole
ribociclib increases toxicity of fluconazole by QTc interval. Contraindicated.
- fosaprepitant
ribociclib will increase the level or effect of fosaprepitant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- lefamulin
lefamulin will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lefamulin is contraindicated with CYP3A substrates know to prolong the QT interval.
- lonafarnib
ribociclib will increase the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lonafarnib is a sensitive CYP3A4 substrate. Coadministration with strong or moderate CYP3A4 inhibitors is contraindicated.
- methadone
ribociclib will increase the level or effect of methadone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- naloxegol
ribociclib will increase the level or effect of naloxegol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- posaconazole
ribociclib increases toxicity of posaconazole by QTc interval. Contraindicated.
- ranolazine
ribociclib increases toxicity of ranolazine by QTc interval. Contraindicated.
- saquinavir
ribociclib increases toxicity of saquinavir by QTc interval. Contraindicated.
Serious - Use Alternative (216)
- adagrasib
adagrasib, ribociclib. Either increases effects of the other by QTc interval. Avoid or Use Alternate Drug. Each drug prolongs the QTc interval, which may increased the risk of Torsade de pointes, other serious arryhthmias, and sudden death. If coadministration unavoidable, more frequent monitoring is recommended for such patients.
- alfuzosin
alfuzosin and ribociclib both increase QTc interval. Contraindicated.
- amiodarone
ribociclib and amiodarone both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of amiodarone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - amitriptyline
ribociclib increases toxicity of amitriptyline by QTc interval. Avoid or Use Alternate Drug.
- anagrelide
ribociclib and anagrelide both increase QTc interval. Avoid or Use Alternate Drug.
- apalutamide
apalutamide will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
ribociclib will increase the level or effect of apalutamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - apomorphine
ribociclib increases toxicity of apomorphine by QTc interval. Avoid or Use Alternate Drug.
- aripiprazole
aripiprazole and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- arsenic trioxide
ribociclib and arsenic trioxide both increase QTc interval. Avoid or Use Alternate Drug.
- artemether
artemether and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- artemether/lumefantrine
ribociclib and artemether/lumefantrine both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will decrease the level or effect of artemether/lumefantrine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - asenapine
ribociclib and asenapine both increase QTc interval. Avoid or Use Alternate Drug.
- asenapine transdermal
asenapine transdermal and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- atazanavir
atazanavir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- atomoxetine
atomoxetine and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- avapritinib
ribociclib will increase the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of avapritinib with moderate CYP3A4 inhibitors. If unable to avoid, reduce avapritinib starting dose. See drug monograph Dosage Modifications.
- azithromycin
ribociclib increases toxicity of azithromycin by QTc interval. Avoid or Use Alternate Drug.
- bedaquiline
ribociclib will increase the level or effect of bedaquiline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ribociclib increases toxicity of bedaquiline by QTc interval. Avoid or Use Alternate Drug. - bosutinib
ribociclib will increase the level or effect of bosutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- brigatinib
ribociclib will increase the level or effect of brigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- bromocriptine
ribociclib will increase the level or effect of bromocriptine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- buprenorphine
buprenorphine and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine buccal
buprenorphine buccal and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine subdermal implant
buprenorphine subdermal implant and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine transdermal
buprenorphine transdermal and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- buprenorphine, long-acting injection
buprenorphine, long-acting injection and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
- ceritinib
ribociclib, ceritinib. Either increases toxicity of the other by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. May increase QT prolongation.
ceritinib and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
ceritinib will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - chloramphenicol
chloramphenicol will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- chloroquine
ribociclib and chloroquine both increase QTc interval. Avoid or Use Alternate Drug.
- chlorpromazine
ribociclib increases toxicity of chlorpromazine by QTc interval. Avoid or Use Alternate Drug.
- chlorpropamide
ribociclib and chlorpropamide both increase QTc interval. Avoid or Use Alternate Drug.
- ciprofloxacin
ribociclib increases toxicity of ciprofloxacin by QTc interval. Avoid or Use Alternate Drug.
- citalopram
ribociclib and citalopram both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of citalopram by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - clarithromycin
clarithromycin will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
ribociclib and clarithromycin both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of clarithromycin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - clofazimine
ribociclib and clofazimine both increase QTc interval. Avoid or Use Alternate Drug.
- clomipramine
ribociclib increases toxicity of clomipramine by QTc interval. Avoid or Use Alternate Drug.
- clozapine
ribociclib will increase the level or effect of clozapine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ribociclib increases toxicity of clozapine by QTc interval. Avoid or Use Alternate Drug. - cobicistat
cobicistat will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
ribociclib will increase the level or effect of cobicistat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - cobimetinib
ribociclib will increase the level or effect of cobimetinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- colchicine
ribociclib will increase the level or effect of colchicine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid use of colchicine with strong CYP3A4 inhibitors. If coadministration is necessary, decrease colchicine dose or frequency as recommended in prescribing information. Use of any colchicine product in conjunction with strong CYP3A4 inhibitors is contraindicated in patients with renal or hepatic impairment.
- conivaptan
conivaptan will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- crizotinib
ribociclib will increase the level or effect of crizotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Increase in crizotinib levels may result in QT prolongation
ribociclib increases toxicity of crizotinib by QTc interval. Avoid or Use Alternate Drug. - dabrafenib
dabrafenib will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
- darifenacin
ribociclib will increase the level or effect of darifenacin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- darunavir
darunavir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
ribociclib will increase the level or effect of darunavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - dasatinib
ribociclib increases toxicity of dasatinib by QTc interval. Avoid or Use Alternate Drug.
- deferiprone
deferiprone, ribociclib. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.
- deflazacort
ribociclib will increase the level or effect of deflazacort by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Decrease dose by one third if combination cannot be avoided
- degarelix
ribociclib increases toxicity of degarelix by QTc interval. Avoid or Use Alternate Drug.
- delavirdine
ribociclib will increase the level or effect of delavirdine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- desflurane
desflurane and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- desipramine
ribociclib increases toxicity of desipramine by QTc interval. Avoid or Use Alternate Drug.
- disopyramide
ribociclib and disopyramide both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of disopyramide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. - dofetilide
ribociclib and dofetilide both increase QTc interval. Avoid or Use Alternate Drug.
dofetilide increases toxicity of ribociclib by QTc interval. Avoid or Use Alternate Drug. - dolasetron
ribociclib increases toxicity of dolasetron by QTc interval. Avoid or Use Alternate Drug.
- donepezil
ribociclib will increase the level or effect of donepezil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
donepezil and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. - doxepin
ribociclib will increase the level or effect of doxepin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
doxepin and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. - doxorubicin
ribociclib will increase the level or effect of doxorubicin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- doxorubicin liposomal
ribociclib will increase the level or effect of doxorubicin liposomal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- dronedarone
ribociclib and dronedarone both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of dronedarone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - droperidol
ribociclib increases toxicity of droperidol by QTc interval. Avoid or Use Alternate Drug.
- efavirenz
ribociclib will increase the level or effect of efavirenz by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
efavirenz and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. - elacestrant
ribociclib will increase the level or effect of elacestrant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- eliglustat
eliglustat and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- encorafenib
ribociclib will increase the level or effect of encorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use of a moderate CYP3A4 inhibitor is unavoidable, reduce encorafenib dose to one-half of the dose (eg, reduce from 450 mg/day to 225 mg/day). After discontinuing the inhibitor for 3-5 elimination half-lives, resume previous encorafenib dose.
encorafenib and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. Encorafenib is associated with dose-dependent QTc interval prolongation. Avoid with drugs known to prolong QT interval.
ribociclib increases toxicity of encorafenib by QTc interval. Avoid or Use Alternate Drug. - entrectinib
ribociclib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of entrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of moderate CYP3A4 inhibitors with entrectinib, a CYP3A4 substrate. If coadministration unavoidable, reduce dose to 200 mg/day for patients aged 12 y or older with BSA >1.50m2. Resume previous entrectinib dose after discontinuing moderate CYP3A inhibitor for 3-5 elimination half-lives. - enzalutamide
enzalutamide will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
ribociclib will increase the level or effect of enzalutamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - erdafitinib
ribociclib will increase the level or effect of erdafitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- eribulin
ribociclib increases toxicity of eribulin by QTc interval. Avoid or Use Alternate Drug.
- erythromycin base
ribociclib increases toxicity of erythromycin base by QTc interval. Avoid or Use Alternate Drug.
- erythromycin ethylsuccinate
ribociclib increases toxicity of erythromycin ethylsuccinate by QTc interval. Avoid or Use Alternate Drug.
- erythromycin lactobionate
ribociclib increases toxicity of erythromycin lactobionate by QTc interval. Avoid or Use Alternate Drug.
- erythromycin stearate
ribociclib increases toxicity of erythromycin stearate by QTc interval. Avoid or Use Alternate Drug.
- escitalopram
ribociclib increases toxicity of escitalopram by QTc interval. Avoid or Use Alternate Drug.
escitalopram increases toxicity of ribociclib by QTc interval. Avoid or Use Alternate Drug. - ethinylestradiol
ethinylestradiol decreases effects of letrozole by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Letrozole should not be given concurrently with any estrogens or estrogen-containing products.
- ezogabine
ribociclib increases toxicity of ezogabine by QTc interval. Avoid or Use Alternate Drug. Slight and transient QT-prolongation observed, particularly when dose titrated to 1200mg/day. QT interval should be monitored when ezogabine is prescribed with agents known to increase QT interval.
- fexinidazole
fexinidazole and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels and/or prolong QT interval.
fexinidazole will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates. - fingolimod
ribociclib will increase the level or effect of fingolimod by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
fingolimod and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. - flecainide
ribociclib increases toxicity of flecainide by QTc interval. Avoid or Use Alternate Drug.
- flibanserin
ribociclib will increase the level or effect of flibanserin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- fluoxetine
ribociclib will increase the level or effect of fluoxetine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ribociclib increases toxicity of fluoxetine by QTc interval. Avoid or Use Alternate Drug. - fosamprenavir
fosamprenavir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- foscarnet
ribociclib increases toxicity of foscarnet by QTc interval. Avoid or Use Alternate Drug.
- fosphenytoin
fosphenytoin will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
- gemifloxacin
ribociclib increases toxicity of gemifloxacin by QTc interval. Avoid or Use Alternate Drug.
- gilteritinib
gilteritinib and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- glasdegib
ribociclib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- granisetron
granisetron and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- grapefruit
grapefruit will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day. Also avoid pomegranates or pomegranate juice, and grapefruits.
- haloperidol
ribociclib and haloperidol both increase QTc interval. Avoid or Use Alternate Drug.
- hydroxychloroquine sulfate
hydroxychloroquine sulfate and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib increases toxicity of hydroxychloroquine sulfate by QTc interval. Avoid or Use Alternate Drug. - hydroxyzine
hydroxyzine and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- ibutilide
ribociclib and ibutilide both increase QTc interval. Avoid or Use Alternate Drug.
- idelalisib
idelalisib will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- iloperidone
ribociclib and iloperidone both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of iloperidone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - indacaterol, inhaled
ribociclib increases toxicity of indacaterol, inhaled by QTc interval. Avoid or Use Alternate Drug.
- indinavir
indinavir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- infigratinib
ribociclib will increase the level or effect of infigratinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- inotuzumab
inotuzumab and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. If unable to avoid concomitant use, obtain ECGs and electrolytes before and after initiation of any drug known to prolong QTc, and periodically monitor as clinically indicated during treatment.
ribociclib increases toxicity of inotuzumab by QTc interval. Avoid or Use Alternate Drug. - isoflurane
isoflurane and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- istradefylline
ribociclib will increase the level or effect of istradefylline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- itraconazole
itraconazole will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
itraconazole and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. - ivosidenib
ivosidenib and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of QTc prolonging drugs with ivosidenib or replace with alternate therapies. If coadministration of a QTc prolonging drug is unavoidable, monitor for increased risk of QTc interval prolongation.
- ketoconazole
ketoconazole, ribociclib. Either increases effects of the other by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
ribociclib will increase the level or effect of ketoconazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ketoconazole increases toxicity of ribociclib by QTc interval. Avoid or Use Alternate Drug. - lapatinib
ribociclib increases toxicity of lapatinib by QTc interval. Avoid or Use Alternate Drug.
- larotrectinib
ribociclib will increase the level or effect of larotrectinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lemborexant
ribociclib will increase the level or effect of lemborexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of lemborexant with moderate or strong CYP3A inhibitors.
- levofloxacin
ribociclib increases toxicity of levofloxacin by QTc interval. Avoid or Use Alternate Drug.
- levoketoconazole
levoketoconazole, ribociclib. Either increases effects of the other by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
levoketoconazole increases toxicity of ribociclib by QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of levoketoconazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - lithium
lithium and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- lomitapide
ribociclib will increase the level or effect of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- lopinavir
lopinavir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
ribociclib and lopinavir both increase QTc interval. Avoid or Use Alternate Drug. - lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
ribociclib will increase the level or effect of lumacaftor/ivacaftor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - lumefantrine
ribociclib will increase the level or effect of lumefantrine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lurbinectedin
ribociclib will increase the level or effect of lurbinectedin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- macimorelin
macimorelin and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. Macimorelin causes an increase of ~11 msec in the corrected QT interval. Avoid coadministration with drugs that prolong QT interval, which could increase risk for developing torsade de pointes-type ventricular tachycardia. Allow sufficient washout time of drugs that are known to prolong the QT interval before administering macimorelin.
- maprotiline
ribociclib increases toxicity of maprotiline by QTc interval. Avoid or Use Alternate Drug.
- medroxyprogesterone
ribociclib will increase the level or effect of medroxyprogesterone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mefloquine
ribociclib increases toxicity of mefloquine by QTc interval. Avoid or Use Alternate Drug.
- methadone
ribociclib and methadone both increase QTc interval. Avoid or Use Alternate Drug.
- midazolam intranasal
ribociclib will increase the level or effect of midazolam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of moderate CYP3A4 inhibitors with midazolam intranasal causes higher midazolam systemic exposure, which may prolong sedation.
- mifepristone
ribociclib and mifepristone both increase QTc interval. Avoid or Use Alternate Drug.
mifepristone will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - mirtazapine
mirtazapine and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- mitotane
mitotane will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
- mobocertinib
ribociclib will increase the level or effect of mobocertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If use of moderate CYP3A4 inhibitor unavoidable, reduce mobocertinib dose by ~50% (eg, 160 to 80 mg); closely monitor QTc interval.
mobocertinib and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently. - moxifloxacin
ribociclib and moxifloxacin both increase QTc interval. Avoid or Use Alternate Drug.
- nefazodone
nefazodone will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- nelfinavir
nelfinavir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- neratinib
ribociclib will increase the level or effect of neratinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of neratinib with strong/moderate CYP3A4 inhibitors.
- nicardipine
nicardipine will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- nilotinib
ribociclib and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.
- nortriptyline
ribociclib will increase the level or effect of nortriptyline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ribociclib increases toxicity of nortriptyline by QTc interval. Avoid or Use Alternate Drug. - octreotide
ribociclib increases toxicity of octreotide by QTc interval. Avoid or Use Alternate Drug.
- ofloxacin
ribociclib increases toxicity of ofloxacin by QTc interval. Avoid or Use Alternate Drug.
- olanzapine
ribociclib increases toxicity of olanzapine by QTc interval. Avoid or Use Alternate Drug. Limited data, including some case reports, suggest that olanzapine may be associated with a significant prolongation of the QTc interval in rare instances.
- omaveloxolone
ribociclib will increase the level or effect of omaveloxolone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If unavoidable, reduce omaveloxolone dose to 100 mg/day. Closely monitor for adverse effects. If adverse effects emerge, further reduce to 50 mg/day.
- ondansetron
ribociclib and ondansetron both increase QTc interval. Avoid or Use Alternate Drug.
- osilodrostat
ribociclib and osilodrostat both increase QTc interval. Avoid or Use Alternate Drug. Dose dependent QT prolongation - avoid drugs known to prolong the QT interval
- osimertinib
ribociclib increases toxicity of osimertinib by QTc interval. Avoid or Use Alternate Drug.
- oxaliplatin
oxaliplatin and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- pacritinib
ribociclib will increase the level or effect of pacritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- palifermin
palifermin increases toxicity of ribociclib by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- paliperidone
ribociclib and paliperidone both increase QTc interval. Avoid or Use Alternate Drug.
- panobinostat
ribociclib increases toxicity of panobinostat by QTc interval. Avoid or Use Alternate Drug.
- pasireotide
ribociclib increases toxicity of pasireotide by QTc interval. Avoid or Use Alternate Drug.
- pazopanib
ribociclib increases toxicity of pazopanib by QTc interval. Avoid or Use Alternate Drug.
- pemigatinib
ribociclib will increase the level or effect of pemigatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pemigatinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pemigatinib dose.
- pentamidine
ribociclib increases toxicity of pentamidine by QTc interval. Avoid or Use Alternate Drug.
- perphenazine
ribociclib increases toxicity of perphenazine by QTc interval. Avoid or Use Alternate Drug.
- pexidartinib
ribociclib will increase the level or effect of pexidartinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors is unavoidable, reduce pexidartinib dose (refer to drug monograph dosage modifications). After discontinuing the CYP3A4 inhibitor for 3 elimination half-lives, may resume previous pexidartinib dose.
- phenobarbital
phenobarbital will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
- phenytoin
phenytoin will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
- pimavanserin
ribociclib and pimavanserin both increase QTc interval. Avoid or Use Alternate Drug.
- pimozide
ribociclib and pimozide both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of pimozide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. - pitolisant
ribociclib and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.
- ponatinib
ribociclib will increase the level or effect of ponatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- posaconazole
posaconazole will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- primaquine
primaquine and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- primidone
primidone will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
- procainamide
ribociclib and procainamide both increase QTc interval. Avoid or Use Alternate Drug.
- propafenone
ribociclib will increase the level or effect of propafenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ribociclib increases toxicity of propafenone by QTc interval. Avoid or Use Alternate Drug. - protriptyline
ribociclib increases toxicity of protriptyline by QTc interval. Avoid or Use Alternate Drug.
- quetiapine
ribociclib and quetiapine both increase QTc interval. Avoid or Use Alternate Drug.
- quinidine
ribociclib and quinidine both increase QTc interval. Avoid or Use Alternate Drug.
- quinine
ribociclib increases toxicity of quinine by QTc interval. Avoid or Use Alternate Drug.
- rifampin
rifampin will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
- rilpivirine
ribociclib increases toxicity of rilpivirine by QTc interval. Avoid or Use Alternate Drug.
- risperidone
ribociclib increases toxicity of risperidone by QTc interval. Avoid or Use Alternate Drug.
- ritonavir
ritonavir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- romidepsin
ribociclib will increase the level or effect of romidepsin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ribociclib increases toxicity of romidepsin by QTc interval. Avoid or Use Alternate Drug. - saquinavir
saquinavir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
ribociclib will increase the level or effect of saquinavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. - selpercatinib
ribociclib will increase the level or effect of selpercatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- selumetinib
ribociclib will increase the level or effect of selumetinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with strong or moderate CYP3A4 inhibitors cannot be avoided, reduce selumetinib dosage (refer to selumetinib monograph for further information). After discontinuation of the strong or moderate CYP3A4 inhibitor for 3 elimination half-lives, resume selumetinib dose that was taken before initiating the inhibitor.
- sertraline
ribociclib increases toxicity of sertraline by QTc interval. Avoid or Use Alternate Drug.
- sevoflurane
sevoflurane and ribociclib both increase QTc interval. Avoid or Use Alternate Drug.
- silodosin
ribociclib will increase the level or effect of silodosin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- siponimod
ribociclib will increase the level or effect of siponimod by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of siponimod with a moderate or strong CYP3A4 inhibitor PLUS a moderate or strong CYP2C9 inhibitor is not recommended.
siponimod and ribociclib both increase QTc interval. Avoid or Use Alternate Drug. - solifenacin
ribociclib increases toxicity of solifenacin by QTc interval. Avoid or Use Alternate Drug.
- sorafenib
ribociclib will increase the level or effect of sorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ribociclib increases toxicity of sorafenib by QTc interval. Avoid or Use Alternate Drug. - sotalol
ribociclib and sotalol both increase QTc interval. Avoid or Use Alternate Drug.
- St John's Wort
St John's Wort will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
- sunitinib
ribociclib increases toxicity of sunitinib by QTc interval. Avoid or Use Alternate Drug.
- tacrolimus
ribociclib increases toxicity of tacrolimus by QTc interval. Avoid or Use Alternate Drug.
- tamoxifen
ribociclib increases levels of tamoxifen by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concurrent use of ribociclib and tamoxifen is not indicated. Coadministration shown to increase tamoxifen AUC and Cmax. May increase risk of adverse effects.
tamoxifen decreases levels of letrozole by unspecified interaction mechanism. Contraindicated. Letrozole should not be given concurrently with tamoxifen. Letrozole therapy after the completion of standard tamoxifen treatment is not associated with impaired effects of letrozole. - tazemetostat
ribociclib will increase the level or effect of tazemetostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of tazemetostat with moderate CYP3A4 inhibitors. If coadministration is unavoidable, reduce tazemetostat current dose (see drug monograph Dosage Modifications).
- telavancin
ribociclib increases toxicity of telavancin by QTc interval. Avoid or Use Alternate Drug.
- tetrabenazine
ribociclib and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.
- thioridazine
ribociclib and thioridazine both increase QTc interval. Avoid or Use Alternate Drug.
- ticagrelor
ribociclib will increase the level or effect of ticagrelor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- tipranavir
tipranavir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Inform patients to avoid pomegranate or pomegranate juice, and grapefruit or grapefruit juice
ribociclib will increase the level or effect of tipranavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. - tofacitinib
ribociclib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- tolterodine
ribociclib will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- tolvaptan
ribociclib will increase the level or effect of tolvaptan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- toremifene
ribociclib and toremifene both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of toremifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - trabectedin
ribociclib will increase the level or effect of trabectedin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- tramadol
ribociclib will increase the level or effect of tramadol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- trazodone
ribociclib will increase the level or effect of trazodone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- trimipramine
ribociclib will increase the level or effect of trimipramine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ribociclib increases toxicity of trimipramine by QTc interval. Avoid or Use Alternate Drug. - tucatinib
tucatinib will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.
- ubrogepant
ribociclib will increase the level or effect of ubrogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.
- valbenazine
ribociclib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- vandetanib
ribociclib and vandetanib both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of vandetanib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - vardenafil
ribociclib increases toxicity of vardenafil by QTc interval. Avoid or Use Alternate Drug.
- vemurafenib
ribociclib and vemurafenib both increase QTc interval. Avoid or Use Alternate Drug.
ribociclib will increase the level or effect of vemurafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - venetoclax
ribociclib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- venlafaxine
ribociclib will increase the level or effect of venlafaxine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- vilanterol/fluticasone furoate inhaled
ribociclib will increase the level or effect of vilanterol/fluticasone furoate inhaled by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- vilazodone
ribociclib will increase the level or effect of vilazodone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- vincristine
ribociclib will increase the level or effect of vincristine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
vincristine will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. - vorapaxar
ribociclib will increase the level or effect of vorapaxar by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- voriconazole
voriconazole will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Inform patients to avoid pomegranate or pomegranate juice, and grapefruit or grapefruit juice
ribociclib will increase the level or effect of voriconazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ribociclib increases toxicity of voriconazole by QTc interval. Avoid or Use Alternate Drug. - vorinostat
ribociclib increases toxicity of vorinostat by QTc interval. Avoid or Use Alternate Drug.
- voxelotor
voxelotor will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.
- ziprasidone
ribociclib and ziprasidone both increase QTc interval. Avoid or Use Alternate Drug.
Monitor Closely (254)
- abemaciclib
ribociclib will increase the level or effect of abemaciclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- acalabrutinib
ribociclib will increase the level or effect of acalabrutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Decrease acalabrutinib dose to 100 mg once daily if coadministered with a moderate CYP3A inhibitor.
- ado-trastuzumab emtansine
ribociclib will increase the level or effect of ado-trastuzumab emtansine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- albuterol
albuterol and ribociclib both increase QTc interval. Use Caution/Monitor.
- alfentanil
ribociclib will increase the level or effect of alfentanil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- alfuzosin
ribociclib and alfuzosin both increase QTc interval. Use Caution/Monitor.
ribociclib will increase the level or effect of alfuzosin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - almotriptan
ribociclib will increase the level or effect of almotriptan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- alosetron
ribociclib will increase the level or effect of alosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- alprazolam
ribociclib will increase the level or effect of alprazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- amlodipine
ribociclib will increase the level or effect of amlodipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- apixaban
ribociclib will increase the level or effect of apixaban by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- arformoterol
ribociclib increases toxicity of arformoterol by QTc interval. Use Caution/Monitor.
- aripiprazole
ribociclib will increase the level or effect of aripiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- atazanavir
ribociclib will increase the level or effect of atazanavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- atogepant
ribociclib will increase the level or effect of atogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- atorvastatin
ribociclib will increase the level or effect of atorvastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- avanafil
ribociclib will increase the level or effect of avanafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- axitinib
ribociclib will increase the level or effect of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- azithromycin
azithromycin increases toxicity of ribociclib by QTc interval. Use Caution/Monitor.
- benzhydrocodone/acetaminophen
ribociclib will increase the level or effect of benzhydrocodone/acetaminophen by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration with strong CYP3A4 inhibitors may increase hydrocodone (benzhydrocodone is prodrug of hydrocodone) plasma concentrations and can result in potentially fatal respiratory depression.
- bexarotene
bexarotene will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- bortezomib
ribociclib will increase the level or effect of bortezomib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- bosentan
bosentan will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
ribociclib will increase the level or effect of bosentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - brentuximab vedotin
ribociclib will increase the level or effect of brentuximab vedotin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- brexpiprazole
ribociclib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- buprenorphine
ribociclib will increase the level or effect of buprenorphine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- buprenorphine subdermal implant
ribociclib will increase the level or effect of buprenorphine subdermal implant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor patients already on buprenorphine subdermal implant who require newly-initiated treatment with CYP3A4 inhibitors for signs and symptoms of overmedication. If the dose of the concomitant CYP3A4 inhibitor cannot be reduced or discontinued, implant removal may be necessary and the patient should then be treated with a buprenorphine dosage form that permits dose adjustments. If a CYP3A4 inhibitor is discontinued in a patient who has been stabilized on buprenorphine, monitor the patient for withdrawal.
- buprenorphine transdermal
ribociclib will increase the level or effect of buprenorphine transdermal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- buprenorphine, long-acting injection
ribociclib will increase the level or effect of buprenorphine, long-acting injection by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Patients who transfer to buprenorphine long-acting injection from transmucosal buprenorphine coadministered with CYP3A4 inhibitors should be monitored to ensure buprenorphine plasma levels are adequate. Within 2 weeks, if signs and symptoms of buprenorphine toxicity or overdose occur and the concomitant CYP3A4 inhibitor cannot be reduced or discontinued, transition the patient back to a buprenorphine formulation that permits dose adjustments.
- buspirone
ribociclib will increase the level or effect of buspirone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cabozantinib
ribociclib will increase the level or effect of cabozantinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- calcitriol
ribociclib will increase the level or effect of calcitriol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cannabidiol
ribociclib will increase the level or effect of cannabidiol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Consider reducing the cannabidiol dose when coadministered with a moderate CYP3A4 inhibitor.
- capmatinib
ribociclib will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- carbamazepine
ribociclib will increase the level or effect of carbamazepine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- cariprazine
ribociclib will increase the level or effect of cariprazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cenobamate
cenobamate will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- cevimeline
ribociclib will increase the level or effect of cevimeline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- chlordiazepoxide
ribociclib will increase the level or effect of chlordiazepoxide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- chloroquine
chloroquine increases toxicity of ribociclib by QTc interval. Use Caution/Monitor.
ribociclib will increase the level or effect of chloroquine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - cholera vaccine
letrozole decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Immunosuppressive therapies, including irradiation, antimetabolites, alkylating agents, cytotoxic drugs and corticosteroids (used in greater than physiologic doses), may reduce the immune response to cholera vaccine.
- cilostazol
ribociclib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- cinacalcet
ribociclib will increase the level or effect of cinacalcet by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- clonazepam
ribociclib will increase the level or effect of clonazepam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- clonidine
ribociclib will increase the level or effect of clonidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- clorazepate
ribociclib will increase the level or effect of clorazepate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- codeine
ribociclib will increase the level or effect of codeine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- conjugated estrogens
ribociclib will increase the level or effect of conjugated estrogens by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- copanlisib
ribociclib will increase the level or effect of copanlisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cyclosporine
ribociclib will increase the level or effect of cyclosporine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- dabrafenib
ribociclib will increase the level or effect of dabrafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- daclatasvir
ribociclib will increase the level or effect of daclatasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- daridorexant
ribociclib will increase the level or effect of daridorexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Daridorexant dose should not exceed 25 mg per night when coadministered with moderate CYP3A4 inhibitors.
- dasatinib
ribociclib will increase the level or effect of dasatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dengue vaccine
ribociclib decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine.
letrozole decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine. - deutetrabenazine
ribociclib increases toxicity of deutetrabenazine by QTc interval. Use Caution/Monitor. At the maximum recommended dose, deutetrabenazine does not prolong QT interval to a clinically relevant extent. Certain circumstances may increase risk of torsade de pointes and/or sudden death in association with drugs that prolong the QTc interval (eg, bradycardia, hypokalemia or hypomagnesemia, coadministration with other drugs that prolong QTc interval, presence of congenital QT prolongation).
- eluxadoline
letrozole increases levels of eluxadoline by decreasing metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2A6 inhibitors.
- dexamethasone
ribociclib will increase the level or effect of dexamethasone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- diazepam
ribociclib will increase the level or effect of diazepam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- diazepam intranasal
ribociclib will increase the level or effect of diazepam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Strong or moderate CYP3A4 inhibitors may decrease rate of diazepam elimination, thereby increasing adverse reactions to diazepam.
- dihydroergotamine
ribociclib will increase the level or effect of dihydroergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- dihydroergotamine intranasal
ribociclib will increase the level or effect of dihydroergotamine intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- diltiazem
ribociclib will increase the level or effect of diltiazem by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- docetaxel
ribociclib will increase the level or effect of docetaxel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- donepezil transdermal
ribociclib will increase the level or effect of donepezil transdermal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dronabinol
ribociclib will increase the level or effect of dronabinol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dutasteride
ribociclib will increase the level or effect of dutasteride by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- duvelisib
duvelisib will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.
ribociclib will increase the level or effect of duvelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - efavirenz
efavirenz will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of ribociclib with strong CYP3A inducers should be avoided.
- elagolix
elagolix decreases levels of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.
ribociclib will increase the level or effect of elagolix by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - elbasvir/grazoprevir
ribociclib will increase the level or effect of elbasvir/grazoprevir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- eletriptan
ribociclib will increase the level or effect of eletriptan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- eliglustat
ribociclib will increase the level or effect of eliglustat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
ribociclib will increase the level or effect of elvitegravir/cobicistat/emtricitabine/tenofovir DF by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- encorafenib
encorafenib, ribociclib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
- eplerenone
ribociclib will increase the level or effect of eplerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- ergoloid mesylates
ribociclib will increase the level or effect of ergoloid mesylates by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ergonovine
ribociclib will increase the level or effect of ergonovine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ergotamine
ribociclib will increase the level or effect of ergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- erlotinib
ribociclib will increase the level or effect of erlotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- erythromycin base
ribociclib will increase the level or effect of erythromycin base by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- erythromycin ethylsuccinate
ribociclib will increase the level or effect of erythromycin ethylsuccinate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- erythromycin lactobionate
ribociclib will increase the level or effect of erythromycin lactobionate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- erythromycin stearate
ribociclib will increase the level or effect of erythromycin stearate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- escitalopram
ribociclib will increase the level or effect of escitalopram by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- estradiol
ribociclib will increase the level or effect of estradiol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- estrogens conjugated synthetic
ribociclib will increase the level or effect of estrogens conjugated synthetic by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- estrogens esterified
ribociclib will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- estropipate
ribociclib will increase the level or effect of estropipate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- eszopiclone
ribociclib will increase the level or effect of eszopiclone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ethinylestradiol
ribociclib will increase the level or effect of ethinylestradiol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ethosuximide
ribociclib will increase the level or effect of ethosuximide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- etonogestrel
ribociclib will increase the level or effect of etonogestrel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- etoposide
ribociclib will increase the level or effect of etoposide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- etravirine
etravirine will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
ribociclib will increase the level or effect of etravirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - everolimus
ribociclib will increase the level or effect of everolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- exemestane
ribociclib will increase the level or effect of exemestane by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fedratinib
fedratinib will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
ribociclib will increase the level or effect of fedratinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - felbamate
ribociclib will increase the level or effect of felbamate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- felodipine
ribociclib will increase the level or effect of felodipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fentanyl
ribociclib will increase the level or effect of fentanyl by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- fentanyl intranasal
ribociclib will increase the level or effect of fentanyl intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- fentanyl transdermal
ribociclib will increase the level or effect of fentanyl transdermal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- fentanyl transmucosal
ribociclib will increase the level or effect of fentanyl transmucosal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- finerenone
ribociclib will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or moderate CYP3A4 inhibitors. Adjust finererone dosage as needed.
- flunisolide inhaled
ribociclib will increase the level or effect of flunisolide inhaled by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fluphenazine
ribociclib increases toxicity of fluphenazine by QTc interval. Use Caution/Monitor.
- flurazepam
ribociclib will increase the level or effect of flurazepam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fluticasone furoate
ribociclib will increase the level or effect of fluticasone furoate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Strong CYP3A4 inhibitors may increase fluticasone systemic exposure
- fluticasone inhaled
ribociclib will increase the level or effect of fluticasone inhaled by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fluticasone intranasal
ribociclib will increase the level or effect of fluticasone intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- formoterol
ribociclib increases toxicity of formoterol by QTc interval. Use Caution/Monitor.
- fosamprenavir
ribociclib will increase the level or effect of fosamprenavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fostamatinib
ribociclib will increase the level or effect of fostamatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fostemsavir
ribociclib and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.
- gadobenate
gadobenate and ribociclib both increase QTc interval. Use Caution/Monitor.
- gefitinib
ribociclib will increase the level or effect of gefitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- gemtuzumab
ribociclib and gemtuzumab both increase QTc interval. Use Caution/Monitor.
- glasdegib
ribociclib will increase the level or effect of glasdegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- guanfacine
ribociclib will increase the level or effect of guanfacine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- haloperidol
ribociclib will increase the level or effect of haloperidol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- hydrocodone
ribociclib will increase the level or effect of hydrocodone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- hydroxyprogesterone caproate (DSC)
ribociclib will increase the level or effect of hydroxyprogesterone caproate (DSC) by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ibrutinib
ribociclib increases levels of ibrutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with moderate CYP3A4 inhibitors, reduce ibrutinib dose to 280 mg qDay (B-cell malignancies) or 420 mg qDay (graft versus host disease). After CYP3A inhibitor discontinuation, resume previous dose of ibrutinib.
- idelalisib
ribociclib will increase the level or effect of idelalisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ifosfamide
ribociclib decreases effects of ifosfamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Use of a CYP3A4 inhibitor may decrease metabolism of ifosfamide, potentially reducing ifosfamide therapeutic effects. .
- imatinib
ribociclib will increase the level or effect of imatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- imipramine
ribociclib will increase the level or effect of imipramine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- indinavir
ribociclib will increase the level or effect of indinavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- irinotecan
ribociclib will increase the level or effect of irinotecan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- irinotecan liposomal
ribociclib will increase the level or effect of irinotecan liposomal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. UGT1A1 inhibitors decrease irinotecan metabolism
- isavuconazonium sulfate
ribociclib will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- isosorbide dinitrate
ribociclib will increase the level or effect of isosorbide dinitrate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- isosorbide mononitrate
ribociclib will increase the level or effect of isosorbide mononitrate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- isradipine
ribociclib will increase the level or effect of isradipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
ribociclib increases toxicity of isradipine by QTc interval. Use Caution/Monitor. - istradefylline
istradefylline will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.
- itraconazole
ribociclib will increase the level or effect of itraconazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- ivacaftor
ribociclib will increase the level or effect of ivacaftor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce ivacaftor dose if coadministered with moderate CYP3A4 inhibitors. See specific ivacaftor-containing product for precise dosage modification.
- ivosidenib
ribociclib will increase the level or effect of ivosidenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration with moderate CYP3A4 inhibitors may increase ivosidenib plasma concentrations, thus increasing the risk of QTc prolongation. Monitor for increased risk of QTc interval prolongation.
- ixabepilone
ribociclib will increase the level or effect of ixabepilone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ketamine
ribociclib will increase the level or effect of ketamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lapatinib
ribociclib will increase the level or effect of lapatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lefamulin
ribociclib will increase the level or effect of lefamulin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor for adverse effects if lefamulin is coadministered with moderate CYP3A inhibitors.
- lenacapavir
lenacapavir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- letermovir
letermovir increases levels of letrozole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
letermovir will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - levamlodipine
ribociclib will increase the level or effect of levamlodipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with moderate and strong CYP3A inhibitors results in increased systemic exposure to amlodipine and may require dose reduction. Monitor for symptoms of hypotension and edema when amlodipine is coadministered with CYP3A inhibitors to determine the need for dose adjustment.
- mavacamten
letrozole will increase the level or effect of mavacamten by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Inititiation of weak CYP2C19 inhibitors may require decreased mavacamten dose.
- levomilnacipran
ribociclib will increase the level or effect of levomilnacipran by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- levonorgestrel intrauterine
ribociclib will increase the level or effect of levonorgestrel intrauterine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- levonorgestrel oral
ribociclib will increase the level or effect of levonorgestrel oral by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lofexidine
ribociclib and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.
- lopinavir
ribociclib will increase the level or effect of lopinavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- lorlatinib
ribociclib will increase the level or effect of lorlatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- lovastatin
ribociclib will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lumateperone
ribociclib will increase the level or effect of lumateperone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce lumateperone dose to 21 mg/day if coadministered with moderate CYP3A4 inhibitors.
- lurasidone
ribociclib will increase the level or effect of lurasidone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- maraviroc
ribociclib will increase the level or effect of maraviroc by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- marijuana
ribociclib will increase the level or effect of marijuana by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mavacamten
ribociclib will increase the level or effect of mavacamten by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Inititiation of moderate CYP3A4 inhibitors may require decreased mavacamten dose.
- mefloquine
ribociclib will increase the level or effect of mefloquine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mestranol
ribociclib will increase the level or effect of mestranol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- methylergonovine
ribociclib will increase the level or effect of methylergonovine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- midazolam
ribociclib will increase the level or effect of midazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- midostaurin
ribociclib will increase the level or effect of midostaurin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mifepristone
ribociclib, mifepristone. Either increases toxicity of the other by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- mirtazapine
ribociclib will increase the level or effect of mirtazapine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- modafinil
ribociclib will increase the level or effect of modafinil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mometasone inhaled
ribociclib will increase the level or effect of mometasone inhaled by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nafcillin
nafcillin will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- naldemedine
ribociclib increases levels of naldemedine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor naldemedine for potential adverse effects if coadministered with strong or moderate CYP3A4 inhibitors.
- nefazodone
ribociclib will increase the level or effect of nefazodone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- nelfinavir
ribociclib will increase the level or effect of nelfinavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- netupitant/palonosetron
ribociclib will increase the level or effect of netupitant/palonosetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nevirapine
ribociclib will increase the level or effect of nevirapine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nicardipine
ribociclib will increase the level or effect of nicardipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. If a strong CYP3A inhibitor must be coadministered with ribociclib, reduce the ribociclib starting dose to 400 mg/day.
- nifedipine
ribociclib will increase the level or effect of nifedipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nilotinib
ribociclib will increase the level or effect of nilotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- nimodipine
ribociclib will increase the level or effect of nimodipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nisoldipine
ribociclib will increase the level or effect of nisoldipine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ofatumumab SC
ofatumumab SC, ribociclib. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.
- olaparib
ribociclib will increase the level or effect of olaparib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- oliceridine
ribociclib will increase the level or effect of oliceridine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If concomitant use is necessary, may require less frequent oliceridine dosing. Closely monitor for respiratory depression and sedation and titrate subsequent doses accordingly. If inhibitor is discontinued, consider increase oliceridine dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal.
- ombitasvir/paritaprevir/ritonavir
ribociclib will increase the level or effect of ombitasvir/paritaprevir/ritonavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)
ribociclib will increase the level or effect of ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- ondansetron
ribociclib will increase the level or effect of ondansetron by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- osilodrostat
osilodrostat and ribociclib both increase QTc interval. Use Caution/Monitor.
ribociclib will increase the level or effect of osilodrostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - ospemifene
ribociclib will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- oxaliplatin
oxaliplatin will increase the level or effect of ribociclib by Other (see comment). Use Caution/Monitor. Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT interval.
- oxybutynin
ribociclib will increase the level or effect of oxybutynin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- oxybutynin transdermal
ribociclib will increase the level or effect of oxybutynin transdermal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- oxycodone
ribociclib will increase the level or effect of oxycodone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ozanimod
ozanimod and ribociclib both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.
- paclitaxel
ribociclib will increase the level or effect of paclitaxel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- paclitaxel protein bound
ribociclib will increase the level or effect of paclitaxel protein bound by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- palbociclib
ribociclib will increase the level or effect of palbociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- panobinostat
ribociclib will increase the level or effect of panobinostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- paricalcitol
ribociclib will increase the level or effect of paricalcitol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- pazopanib
ribociclib will increase the level or effect of pazopanib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- pimavanserin
ribociclib will increase the level or effect of pimavanserin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- polatuzumab vedotin
ribociclib will increase the level or effect of polatuzumab vedotin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- quazepam
ribociclib will increase the level or effect of quazepam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- quetiapine
ribociclib will increase the level or effect of quetiapine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- quinidine
ribociclib will increase the level or effect of quinidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- quinine
ribociclib will increase the level or effect of quinine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- ramelteon
ribociclib will increase the level or effect of ramelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ranolazine
ribociclib will increase the level or effect of ranolazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- regorafenib
ribociclib will increase the level or effect of regorafenib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- repaglinide
ribociclib will increase the level or effect of repaglinide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rifabutin
rifabutin will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
ribociclib will increase the level or effect of rifabutin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - rifapentine
rifapentine will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rimegepant
ribociclib will increase the level or effect of rimegepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid repeating rimegepant dose within 48 hr if coadministered with a moderate CYP3A4 inhibitor.
- ritonavir
ribociclib will increase the level or effect of ritonavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- roflumilast
ribociclib will increase the level or effect of roflumilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rucaparib
rucaparib will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- saxagliptin
ribociclib will increase the level or effect of saxagliptin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- sildenafil
ribociclib will increase the level or effect of sildenafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- simvastatin
ribociclib will increase the level or effect of simvastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- siponimod
siponimod and letrozole both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
siponimod and ribociclib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects. - sirolimus
ribociclib will increase the level or effect of sirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- sodium sulfate/?magnesium sulfate/potassium chloride
sodium sulfate/?magnesium sulfate/potassium chloride increases toxicity of ribociclib by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias. .
- sodium sulfate/potassium sulfate/magnesium sulfate
sodium sulfate/potassium sulfate/magnesium sulfate increases toxicity of ribociclib by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias. .
- solifenacin
ribociclib will increase the level or effect of solifenacin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- sonidegib
ribociclib will increase the level or effect of sonidegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- sparsentan
ribociclib will increase the level or effect of sparsentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No dosage adjustment needed. Monitor blood pressure, serum potassium, edema, and kidney function regularly if sparsentan is coadministered with moderate CYP3A4 inhibitors.
- stiripentol
stiripentol, ribociclib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
ribociclib will increase the level or effect of stiripentol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. - sufentanil
ribociclib will increase the level or effect of sufentanil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- sufentanil SL
ribociclib will increase the level or effect of sufentanil SL by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of sufentanil SL with any CYP3A4 inhibitor may increase sufentanil plasma concentration, and, thereby increase or prolonged adverse effects, including potentially fatal respiratory depression.
- sunitinib
ribociclib will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- suvorexant
ribociclib will increase the level or effect of suvorexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- tacrolimus
ribociclib will increase the level or effect of tacrolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- tadalafil
ribociclib will increase the level or effect of tadalafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tamsulosin
ribociclib will increase the level or effect of tamsulosin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tazemetostat
tazemetostat will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- temsirolimus
ribociclib will increase the level or effect of temsirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tezacaftor
ribociclib will increase the level or effect of tezacaftor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust tezacaftor dosage regimen if coadministered with a moderate CYP3A inhibitor.
- ticlopidine
ribociclib will increase the level or effect of ticlopidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tinidazole
ribociclib will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- trastuzumab
trastuzumab, ribociclib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy.
- trastuzumab deruxtecan
trastuzumab deruxtecan, ribociclib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy.
- triazolam
ribociclib will increase the level or effect of triazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Caution if ribociclib is coadministered with sensitive CYP3A4 substrates that have a narrow therapeutic index. Dose reduction for sensitive CYP3A4 substrates may be needed.
- triclabendazole
triclabendazole and ribociclib both increase QTc interval. Use Caution/Monitor.
- ulipristal
ribociclib will increase the level or effect of ulipristal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- umeclidinium bromide/vilanterol inhaled
ribociclib will increase the level or effect of umeclidinium bromide/vilanterol inhaled by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- upadacitinib
ribociclib will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- vardenafil
ribociclib will increase the level or effect of vardenafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Vardenafil dose may need to be reduced if coadministered with moderate or strong CYP3A4 inhibitors
- verapamil
ribociclib will increase the level or effect of verapamil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- vilanterol/fluticasone furoate inhaled
ribociclib increases toxicity of vilanterol/fluticasone furoate inhaled by QTc interval. Use Caution/Monitor.
- vinblastine
ribociclib will increase the level or effect of vinblastine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- vinorelbine
ribociclib will increase the level or effect of vinorelbine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- voclosporin
ribociclib will increase the level or effect of voclosporin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce voclosporin daily dosage to 15.8 mg PO in AM and 7.9 mg PO in PM.
voclosporin, ribociclib. Either increases effects of the other by QTc interval. Use Caution/Monitor. - zaleplon
ribociclib will increase the level or effect of zaleplon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- zanubrutinib
ribociclib will increase the level or effect of zanubrutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce zanubrutinib (a CYP3A4 substrate) to 80 mg PO BID to when coadministered with a moderate CYP3A4 inhibitor. Interrupt dose as recommended for adverse reactions. After discontinuing the CYP3A4 inhibitor, resume previous dose of zanubrutinib.
- zolpidem
ribociclib will increase the level or effect of zolpidem by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
Minor (69)
- acetazolamide
acetazolamide will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- alpelisib
ribociclib will increase the level or effect of alpelisib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ambrisentan
ribociclib will increase the level or effect of ambrisentan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- apremilast
ribociclib will decrease the level or effect of apremilast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- armodafinil
ribociclib will increase the level or effect of armodafinil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- avatrombopag
ribociclib will increase the level or effect of avatrombopag by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- benzphetamine
ribociclib will increase the level or effect of benzphetamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- busulfan
ribociclib will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- calcifediol
ribociclib will increase the level or effect of calcifediol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- chlorpheniramine
ribociclib will increase the level or effect of chlorpheniramine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ciclesonide inhaled
ribociclib will increase the level or effect of ciclesonide inhaled by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cisapride
ribociclib will increase the level or effect of cisapride by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cocaine topical
ribociclib will increase the level or effect of cocaine topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
ribociclib will increase the level or effect of cyclophosphamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
cyclophosphamide will increase the level or effect of ribociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. - dantrolene
ribociclib will increase the level or effect of dantrolene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- dapsone
ribociclib will increase the level or effect of dapsone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- dexlansoprazole
ribociclib will increase the level or effect of dexlansoprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- doravirine
ribociclib will increase the level or effect of doravirine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- doxepin cream
ribociclib will increase the level or effect of doxepin cream by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- enfortumab vedotin
ribociclib will increase the level or effect of enfortumab vedotin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- esomeprazole
ribociclib will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- estradiol vaginal
ribociclib will increase the level or effect of estradiol vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- fenofibrate
ribociclib will increase the level or effect of fenofibrate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- fenofibrate micronized
ribociclib will increase the level or effect of fenofibrate micronized by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- fenofibric acid
ribociclib will increase the level or effect of fenofibric acid by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- flutamide
ribociclib will increase the level or effect of flutamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- glecaprevir/pibrentasvir
ribociclib will increase the level or effect of glecaprevir/pibrentasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ixazomib
ribociclib will increase the level or effect of ixazomib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- lacosamide
ribociclib will increase the level or effect of lacosamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- lansoprazole
ribociclib will increase the level or effect of lansoprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- linagliptin
ribociclib will increase the level or effect of linagliptin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- losartan
ribociclib will increase the level or effect of losartan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- macimorelin
ribociclib will increase the level or effect of macimorelin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- metaxalone
ribociclib will increase the level or effect of metaxalone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- methylprednisolone
ribociclib will increase the level or effect of methylprednisolone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- miconazole oral
ribociclib will increase the level or effect of miconazole oral by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- montelukast
ribociclib will increase the level or effect of montelukast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- norethindrone
ribociclib will increase the level or effect of norethindrone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- norgestrel
ribociclib will increase the level or effect of norgestrel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- omeprazole
ribociclib will increase the level or effect of omeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- osimertinib
ribociclib will increase the level or effect of osimertinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- perampanel
ribociclib will increase the level or effect of perampanel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- pitolisant
ribociclib will increase the level or effect of pitolisant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- pomalidomide
ribociclib will increase the level or effect of pomalidomide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- praziquantel
ribociclib will increase the level or effect of praziquantel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- primaquine
ribociclib will increase the level or effect of primaquine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- progesterone intravaginal gel
ribociclib will increase the level or effect of progesterone intravaginal gel by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- progesterone micronized
ribociclib will increase the level or effect of progesterone micronized by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- progesterone, natural
ribociclib will increase the level or effect of progesterone, natural by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- rabeprazole
ribociclib will increase the level or effect of rabeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- riociguat
ribociclib will increase the level or effect of riociguat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- rivaroxaban
ribociclib will increase the level or effect of rivaroxaban by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- rolapitant
ribociclib will increase the level or effect of rolapitant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ropivacaine
ribociclib will increase the level or effect of ropivacaine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ruxolitinib
ribociclib will increase the level or effect of ruxolitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ruxolitinib topical
ribociclib will increase the level or effect of ruxolitinib topical by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- salmeterol
ribociclib will increase the level or effect of salmeterol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- sofosbuvir/velpatasvir
ribociclib will increase the level or effect of sofosbuvir/velpatasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- tasimelteon
ribociclib will increase the level or effect of tasimelteon by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- teniposide
ribociclib will increase the level or effect of teniposide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- theophylline
ribociclib will increase the level or effect of theophylline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- tiagabine
ribociclib will increase the level or effect of tiagabine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- trimethoprim
ribociclib will increase the level or effect of trimethoprim by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- velpatasvir
ribociclib will increase the level or effect of velpatasvir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- vincristine liposomal
ribociclib will increase the level or effect of vincristine liposomal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- vortioxetine
ribociclib will increase the level or effect of vortioxetine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- voxilaprevir
ribociclib will increase the level or effect of voxilaprevir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- zonisamide
ribociclib will increase the level or effect of zonisamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
>10%
Percentage includes all grades of toxicity unless otherwise stated
Leukocyte count decreased (93%)
Neutrophil count decreased (93%)
Neutropenia (75%)
Hemoglobin decreased (57%)
Nausea (52%)
Lymphocyte count decreased (51%)
Neutropenia, grade 3 (50%)
Neutrophil count decreased, grade 3 (49%)
AST/ALT increased (44-46%)
Fatigue (37%)
Diarrhea (35%)
Leukopenia (33%)
Alopecia (33%)
Leukocyte count decreased, grade 3 (31%)
Platelets decreased (29%)
Vomiting (29%)
Constipation (25%)
Headache (22%)
Leukopenia, grade 3 (20%)
Back pain (20%)
Creatinine increased (20%)
Decreased appetite (19%)
Anemia (18%)
Abnormal LFTs (18%)
Rash (17%)
Pruritus (14%)
Pyrexia (13%)
Phosphorus decreased (13%)
Peripheral edema (12%)
Stomatitis (12%)
Insomnia (12%)
Dyspnea (12%)
Lymphopenia (11%)
Urinary tract infection (11%)
Abdominal pain (11%)
Potassium decreased (11%)
1-10%
Neutropenia, grade 4 (10%)
Postmarketing Reports
Respiratory disorders: Interstitial lung disease (ILD)/pneumonitis
Skin and subcutaneous tissue disorders: Stevens-Johnson Syndrome (SJS), toxic epidermal necrolysis (TEN), drug-induced hypersensitivity syndrome (DiHS)/drug reaction with eosinophilia and systemic symptoms (DRESS)
Warnings
Contraindications
Hypersensitivity to active substance (letrozole), or to excipients of the formulation
Cautions
May cause fetal harm; advise women of reproductive potential to use effective contraception (see Pregnancy)
Severe cutaneous reactions
- Severe cutaneous adverse reactions (SCARs), including Stevens-Johnson Syndrome (SJS), toxic epidermal necrolysis(TEN), and drug-induced hypersensitivity syndrome (DiHS)/drug reaction with eosinophilia and systemic symptoms (DRESS) can occur
- If signs or symptoms occur, interrupt treatment until the etiology of the reaction determined
- Early consultation with a dermatologist recommended to ensure greater diagnostic accuracy and appropriate management
- If SJS, TEN, or DiHS/DRESS confirmed, permanently discontinue; do not reintroduce in patients who have experienced SCARs or other life threatening cutaneous reactions during treatment
Interstitial lung disease/pneumonitis
- Severe, life-threatening, or fatal ILD and/or pneumonitis can occur; additional cases of ILD/pneumonitis have been observed in the postmarketing setting, with fatalities reported; monitor for pulmonary symptoms indicative of ILD/pneumonitis which may include hypoxia, cough, and dyspnea
- In patients who have new or worsening respiratory symptoms suspected to be due to ILD or pneumonitis, interrupt therapy immediately and evaluate patient; permanently discontinue therapy in patients with recurrent symptomatic or severe ILD/pneumonitis
QT prolongation
- Prolongs the QT interval in a concentration-dependent manner, with estimated mean increase in QTc interval exceeding 20 ms following administration at 600 mg once daily dose
- Avoid use in patients who already have or who are at significant risk of developing QTc prolongation, including those with electrolyte abnormalities, long QT syndrome, or uncontrolled or significant cardiac disease including recent myocardial infarction, congestive heart failure, unstable angina, and bradyarrhythmias
- Avoid use in patients taking drugs known to prolong QTc interval and/or strong CYP3A inhibitors as this may lead to prolongation of the QTcF interval
- Based on observed QT prolongation during treatment, drug may require dose interruption, reduction or discontinuation
- Increased in QT prolongation with concomitant use of tamoxifen; not indicated for concomitant use
Hepatobiliary toxicity
- Increased transaminases were observed in clinical trials; Grade 3 or 4 increases in ALT and AST reported
- In patients who had Grade ≥3 ALT/AST elevation, median time-to-onset was 57 days; whereas, Grade ≤2 was 24 days
Neutropenia
- Neutropenia is the most frequently reported adverse effect
- Among patients with neutropenia, the median time to Grade ≥2 is 17 days
- Median time to resolution of Grade ≥3 (to normalization or Grade <3) is 12 days
- Monitor CBC every 2 weeks for first 2 cycles, at the beginning of each subsequent 4 cycles, and as clinically indicated; based on the severity of the neutropenia, therapy may require dose interruption, reduction, or discontinuation
Drug interaction overview
- Ribociclib is a CYP3A4 substrate and CYP3A4 inhibitor
-
Drugs that may increase ribociclib plasma concentrations
- Avoid concomitant use of strong CYP3A inhibitors (eg, clarithromycin, conivaptan, grapefruit juice, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, and voriconazole) and consider alternative concomitant medications with less potential for CYP3A inhibition
- If coadministration with a strong CYP3A inhibitor cannot be avoided, reduce the ribociclib dose to 400 mg/day (also see Dosage Modifications)
- Instruct patients to avoid pomegranates or pomegranate juice, grapefruit, all of which are known to inhibit cytochrome CYP3A enzymes and may increase the exposure to ribociclib
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Drugs that may decrease ribociclib plasma concentrations
- Avoid concomitant use of strong CYP3A inducers (eg, phenytoin, rifampin, carbamazepine, St John’s Wort) and consider an alternate concomitant medication with no or minimal potential to induce CYP3A
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Effect of ribociclib on other drugs
- Caution if ribociclib is coadministered with CYP3A4 substrates that have a narrow therapeutic index (NTI), as ribociclib can increase their systemic exposure
- The dose of a sensitive CYP3A substrates with a NTI may need to be reduced
- CYP3A substrates with a NTI include (but are not limited to) alfentanil, cyclosporine, dihydroergotamine, ergotamine, everolimus, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus
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Drugs that prolong QT interval
- Avoid coadministration of ribociclib with drugs with a known potential to prolong QT
- Examples include antiarrhythmic medicines (including, but not limited to amiodarone, disopyramide, procainamide, quinidine and sotalol), and other drugs that are known to prolong the QT interval (eg, chloroquine, clarithromycin, haloperidol, methadone, moxifloxacin, pimozide, ondansetron IV)
Pregnancy & Lactation
Pregnancy
There are no available human data informing the drug-associated risk
Based on findings from animal studies and the mechanism of action, can cause fetal harm when administered to a pregnant woman
In animal reproduction studies, administration during organogenesis resulted in increased incidences of postimplantation loss and reduced fetal weights in rats and increased incidences of fetal abnormalities in rabbits at exposures 0.6 or 1.5 times the exposure in humans
Infertility: Based on animal studies, may impair fertility in males Contraception
- Females of reproductive potential should have a pregnancy test prior to starting treatment
- Females: Advise females of reproductive potential to use effective contraception (methods that result in <1% pregnancy rates) during treatment and for at least 3 weeks after the last dose
Lactation
Unknown if distributed in human breast milk
Because of the potential for serious adverse reactions in breastfed infants, advise lactating women not to breastfeed while taking ribociclib and for at least 3 weeks after the last dose
In lactating rats administered a single dose of 50 mg/kg, exposure to ribociclib was 3.56-fold higher in milk compared to maternal plasma
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
The combination of ribociclib and antiestrogen (eg, letrozole) increases tumor growth inhibition compared with each drug alone
Ribociclib
- Inhibits cyclin dependent kinases (CDK) 4 and 6; blocks cellular proliferation of G1 into S phase of the cell cycle
- These kinases are activated upon binding to D cyclins and play a crucial role in signaling pathways which lead to cell cycle progression and cellular proliferation; the cyclin D-CDK4/6 complex regulates cell cycle progression through phosphorylation of the retinoblastoma protein (pRb)
Letrozole
- Nonsteroidal competitive inhibitor of the aromatase enzyme system by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues
Absorption
Peak plasma time: 1-4 hr (ribociclib)
Distribution
Protein bound
- Ribociclib: 70%
- Letrozole: Weakly protein bound
Vd
- Ribociclib: 1090 L
- Letrozole: 1.9 L/kg
Metabolism
Ribociclib
- Undergoes extensive hepatic metabolism mainly via CYP3A4 in humans
- Primary metabolic pathways for ribociclib involved oxidation (dealkylation, C and/or N-oxygenation, oxidation (-2H)) and combinations thereof
- Phase II conjugates of ribociclib Phase I metabolites involved N-acetylation, sulfation, cysteine conjugation, glycosylation and glucuronidation
- Ribociclib was the major circulating drug-derived entity in plasma (44%)
Letrozole
- Metabolism to a pharmacologically-inactive carbinol metabolite (4,4'methanol-bisbenzonitrile) and renal excretion of the glucuronide conjugate of this metabolite is the major pathway of letrozole clearance
Elimination
Half-life (ribociclib): 32 hr; 29.7-54.7 hr (terminal half-life)
Oral clearance (ribociclib): 25.5 L/hr
Excretion
- Ribociclib (within 22 days): 69% feces; 23% urine
- Letrozole: 90% urine (75% as glucuronide of the carbinol metabolite; 9% 2 unidentified metabolites, 6% unchanged)
Administration
Oral Administration
Administer with or without food
Take doses at about the same time each day, preferably in the morning
Swallow tablets whole, do not chew, crush, or split
Do not ingest tablets that are broken, cracked, or otherwise not intact
Vomited or missed doses
- Do not take an additional dose the remainder of the day if the dose if vomited or missed
- The next prescribed dose should be taken at the usual time
Storage
Store in original package at 20-25°C (68-77°F)
Images
Formulary
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