Dosing & Uses
Dosage Forms & Strengths
capsule
- 150mg
Non-Small Cell Lung Cancer
Indicated for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test
450 mg PO qDay with food
Continue until disease progression or unacceptable toxicity
Also see administration
Dosage Modifications
Dose reduction increments
- Starting dose: 450 mg qDay
- First dose reduction: 300 mg qDay
- Second dose reduction: 150 mg qDay
- Unable to tolerate 150 mg/day: Discontinue
Coadministration with strong CYP3A4 inhibitors
- Avoid concurrent use of strong CYP3A inhibitors during treatment
- If coadministration with a strong CYP3A inhibitor is unavoidable, reduce the dose by ~one-third, rounded to the nearest multiple of the 150 mg dosage strength
- After discontinuation of a strong CYP3A inhibitor, resume the dose that was taken prior to initiating the strong CYP3A4 inhibitor
ALT/AST elevation
- ALT/AST increase >5 x ULN with total bilirubin ≤2 x ULN: Withhold until recovery to baseline or ≤3 x ULN, then resume with 150-mg dose reduction
- ALT/AST increase >3 x ULN with total bilirubin >2 x ULN in absence of cholestasis or hemolysis: Permanently discontinue
Gastrointestinal
- Lipase or amylase increase ≥2 x ULN: Withhold and monitor serum lipase and amylase; resume with 150-mg dose reduction after recovery to < 1.5 times ULN
- Severe or intolerable nausea, vomiting, or diarrhea despite optimal antiemetic therapy: Withhold until improved, then resume with 150-mg dose reduction
Hyperglycemia
- Persistent hyperglycemia >250 mg/dL despite optimal antihyperglycemic therapy: Withhold ceritinib until hyperglycemia is adequately controlled, then resume with 150-mg dose reduction
- If adequate hyperglycemic control cannot be achieved with optimal medical management, discontinue ceritinib
Pneumonitis
- Any grade treatment-related ILD/pneumonitis: Permanently discontinue
Prolonged QT interval
- QT interval >500 msec (on at least 2 separate ECGs): Withhold until QTc interval <481 msec or recovery to baseline if baseline QTc ≥481 msec, then resume with a 150-mg dose reduction
- QTc interval prolongation in combination with torsade de pointes or polymorphic ventricular tachycardia or signs/symptoms of serious arrhythmia: Permanently discontinue
Bradycardia
- Symptomatic (not life-threatening): Withhold until recovery to asymptomatic bradycardia or to a heart rate of ≥60 bpm; evaluate concomitant medications known to cause bradycardia, and adjust the dose
- Clinically significant requiring intervention or life-threatening in patients taking concomitant drug also known to cause bradycardia: Withhold until recovery to asymptomatic bradycardia or to a heart rate of ≥60 bpm; if concomitant medication can be adjusted or discontinued, resume with a 150-mg dose reduction, with frequent monitoring
- Life-threatening bradycardia in patient who are not taking a concomitant medication also known to cause bradycardia or known to cause hypotension: Permanently discontinue
Hepatic impairment
- Mild-to-moderate (Child Pugh A to B): No dosage adjustment is necessary
- Severe (Child Pugh C): Reduce dose by ~one-third, round to the nearest multiple of 150 mg dosage strength
Dosing Considerations
Selection for ceritinib treatment is based on the presence of ALK positivity in tumor specimens
Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (12)
- alfuzosin
ceritinib and alfuzosin both increase QTc interval. Contraindicated.
- cisapride
ceritinib and cisapride both increase QTc interval. Contraindicated.
- clofazimine
ceritinib and clofazimine both increase QTc interval. Contraindicated.
- dronedarone
ceritinib and dronedarone both increase QTc interval. Contraindicated.
- flibanserin
ceritinib will increase the level or effect of flibanserin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration of flibanserin with moderate or strong CYP3A4 inhibitors is contraindicated. Severe hypotension or syncope can occur.
- fluconazole
ceritinib and fluconazole both increase QTc interval. Contraindicated.
- lonafarnib
ceritinib 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.
- posaconazole
ceritinib and posaconazole both increase QTc interval. Contraindicated.
- ranolazine
ceritinib and ranolazine both increase QTc interval. Contraindicated.
- saquinavir
ceritinib and saquinavir both increase QTc interval. Contraindicated.
- thioridazine
ceritinib and thioridazine both increase QTc interval. Contraindicated.
- voclosporin
ceritinib and voclosporin both increase QTc interval. Contraindicated.
Serious - Use Alternative (191)
- abametapir
abametapir increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.
- alfentanil
ceritinib increases levels of alfentanil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP3A substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP3A during treatment with ceritinib; if use of these medications is unavoidable, consider dose reduction.
- amiodarone
ceritinib and amiodarone both increase QTc interval. Avoid or Use Alternate Drug.
- anagrelide
ceritinib and anagrelide both increase QTc interval. Avoid or Use Alternate Drug.
- apalutamide
apalutamide will decrease the level or effect of ceritinib 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.
- apomorphine
ceritinib and apomorphine both increase QTc interval. Avoid or Use Alternate Drug.
- arsenic trioxide
ceritinib and arsenic trioxide both increase QTc interval. Avoid or Use Alternate Drug.
- artemether/lumefantrine
ceritinib and artemether/lumefantrine both increase QTc interval. Avoid or Use Alternate Drug.
- asenapine
ceritinib and asenapine both increase QTc interval. Avoid or Use Alternate Drug.
- atazanavir
atazanavir increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- avapritinib
ceritinib 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
ceritinib and azithromycin both increase QTc interval. Avoid or Use Alternate Drug.
- bedaquiline
ceritinib and bedaquiline both increase QTc interval. Avoid or Use Alternate Drug.
- bosentan
bosentan decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- buprenorphine
ceritinib and buprenorphine both increase QTc interval. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- chloramphenicol
chloramphenicol, ceritinib. Either increases toxicity of the other by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration necessary, reduce dose of crizotinib to 250 mg once daily; resume original crizotinib dose after discontinuing .
- chloroquine
ceritinib and chloroquine both increase QTc interval. Avoid or Use Alternate Drug.
- chlorpromazine
ceritinib and chlorpromazine both increase QTc interval. Avoid or Use Alternate Drug.
- ciprofloxacin
ceritinib and ciprofloxacin both increase QTc interval. Avoid or Use Alternate Drug.
- citalopram
ceritinib and citalopram both increase QTc interval. Avoid or Use Alternate Drug.
- clarithromycin
clarithromycin increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
ceritinib and clarithromycin both increase QTc interval. Avoid or Use Alternate Drug. - clozapine
ceritinib and clozapine both increase QTc interval. Avoid or Use Alternate Drug.
- cobicistat
cobicistat, ceritinib. Either increases toxicity of the other by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. May increase QT prolongation.
- cobimetinib
ceritinib will increase the level or effect of cobimetinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concurrent short term (14 days or less) use of moderate CYP3A inhibitors is unavoidable for patients who are taking cobimetinib 60 mg, reduce the cobimetinib dose to 20 mg. After discontinuation of a moderate CYP3A inhibitor, resume cobimetinib 60 mg. Use an alternative to a moderate CYP3A inhibitor in patients who are taking a reduced dose of cobimetinib (40 or 20 mg daily).
- conivaptan
conivaptan increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- crizotinib
ceritinib and crizotinib both increase QTc interval. Avoid or Use Alternate Drug.
- cyclosporine
ceritinib increases levels of cyclosporine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP3A substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP3A during treatment with ceritinib; if use of these medications is unavoidable, consider dose reduction.
- dabrafenib
dabrafenib decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- darunavir
darunavir increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- dasatinib
ceritinib and dasatinib both increase QTc interval. Avoid or Use Alternate Drug.
- degarelix
ceritinib and degarelix both increase QTc interval. Avoid or Use Alternate Drug.
- desflurane
desflurane and ceritinib both increase QTc interval. Avoid or Use Alternate Drug.
- deutetrabenazine
ceritinib and deutetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.
- dexamethasone
dexamethasone decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- dihydroergotamine
ceritinib increases levels of dihydroergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP3A substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP3A during treatment with ceritinib; if use of these medications is unavoidable, consider dose reduction.
- disopyramide
ceritinib and disopyramide both increase QTc interval. Avoid or Use Alternate Drug.
- dofetilide
ceritinib and dofetilide both increase QTc interval. Avoid or Use Alternate Drug.
- dolasetron
ceritinib and dolasetron both increase QTc interval. Avoid or Use Alternate Drug.
- donepezil
donepezil and ceritinib both increase QTc interval. Avoid or Use Alternate Drug.
- droperidol
ceritinib and droperidol both increase QTc interval. Avoid or Use Alternate Drug.
- efavirenz
efavirenz decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- eliglustat
ceritinib increases levels of eliglustat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Moderate CYP3A4 inhibitors are not recommended with eliglustat poor or intermediate metabolizers; reduce eliglustat dose from 84 mg BID to 84 mg once daily in extensive metabolizers .
ceritinib and eliglustat both increase QTc interval. Avoid or Use Alternate Drug. - elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- encorafenib
ceritinib and encorafenib both increase QTc interval. Avoid or Use Alternate Drug.
- entrectinib
ceritinib 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.
ceritinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug. - enzalutamide
enzalutamide decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erdafitinib
erdafitinib will increase the level or effect of ceritinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If coadministration unavoidable, separate administration by at least 6 hr before or after administration of P-gp substrates with narrow therapeutic index.
ceritinib will increase the level or effect of erdafitinib by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. If coadministration of a strong CYP2C9 inhibitors is unavoidable, closely monitor adverse reactions and modify dose of erdafitinib accordingly. If strong CYP2C9 inhibitor is discontinued, consider increasing erdafitinib dose in the absence of any drug-related toxicities. - ergotamine
ceritinib increases levels of ergotamine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP3A substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP3A during treatment with ceritinib; if use of these medications is unavoidable, consider dose reduction.
- eribulin
ceritinib and eribulin both increase QTc interval. Avoid or Use Alternate Drug.
- erythromycin base
ceritinib and erythromycin base both increase QTc interval. Avoid or Use Alternate Drug.
- erythromycin ethylsuccinate
ceritinib and erythromycin ethylsuccinate both increase QTc interval. Avoid or Use Alternate Drug.
- erythromycin lactobionate
ceritinib and erythromycin lactobionate both increase QTc interval. Avoid or Use Alternate Drug.
- erythromycin stearate
ceritinib and erythromycin stearate both increase QTc interval. Avoid or Use Alternate Drug.
- escitalopram
ceritinib and escitalopram both increase QTc interval. Avoid or Use Alternate Drug.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- esomeprazole
esomeprazole will decrease the level or effect of ceritinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.
- etravirine
etravirine decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fentanyl
ceritinib will increase the level or effect of fentanyl by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fentanyl intranasal
ceritinib will increase the level or effect of fentanyl intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fentanyl transdermal
ceritinib will increase the level or effect of fentanyl transdermal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fentanyl transmucosal
ceritinib will increase the level or effect of fentanyl transmucosal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fexinidazole
fexinidazole and ceritinib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels or prolong QT interval.
fexinidazole will increase the level or effect of ceritinib 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. - flecainide
ceritinib and flecainide both increase QTc interval. Avoid or Use Alternate Drug.
- fluoxetine
ceritinib and fluoxetine both increase QTc interval. Avoid or Use Alternate Drug.
- fosamprenavir
fosamprenavir increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- foscarnet
ceritinib and foscarnet both increase QTc interval. Avoid or Use Alternate Drug.
- fosphenytoin
fosphenytoin decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ceritinib increases levels of fosphenytoin by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP2C9 substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP2C9 during treatment with ceritinib; if use of these medications is unavoidable, consider dose. - gemifloxacin
ceritinib and gemifloxacin both increase QTc interval. Avoid or Use Alternate Drug.
- gilteritinib
ceritinib and gilteritinib both increase QTc interval. Avoid or Use Alternate Drug.
- glasdegib
ceritinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- granisetron
ceritinib and granisetron both increase QTc interval. Avoid or Use Alternate Drug.
- grapefruit
grapefruit increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid grapefruit and grapefruit juice while taking ceritinib.
- haloperidol
ceritinib and haloperidol both increase QTc interval. Avoid or Use Alternate Drug.
- hydroxychloroquine sulfate
ceritinib and hydroxychloroquine sulfate both increase QTc interval. Avoid or Use Alternate Drug.
- hydroxyzine
ceritinib and hydroxyzine both increase QTc interval. Avoid or Use Alternate Drug.
- ibutilide
ceritinib and ibutilide both increase QTc interval. Avoid or Use Alternate Drug.
- idelalisib
idelalisib will increase the level or effect of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates
- iloperidone
ceritinib and iloperidone both increase QTc interval. Avoid or Use Alternate Drug.
- imatinib
imatinib increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- indinavir
indinavir increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- infigratinib
ceritinib will increase the level or effect of infigratinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- inotuzumab
inotuzumab and ceritinib 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.
- isoflurane
ceritinib and isoflurane both increase QTc interval. Avoid or Use Alternate Drug.
- isoniazid
isoniazid increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- itraconazole
itraconazole increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
ceritinib and itraconazole both increase QTc interval. Avoid or Use Alternate Drug. - ivabradine
ceritinib will increase the level or effect of ivabradine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of ivabradine with moderate CYP3A4 inhibitors.
- ivosidenib
ivosidenib will decrease the level or effect of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
ceritinib and ivosidenib both decrease QTc interval. Avoid or Use Alternate Drug. - ketoconazole
ketoconazole increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- lapatinib
ceritinib and lapatinib both increase QTc interval. Avoid or Use Alternate Drug.
- lasmiditan
lasmiditan increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- lefamulin
lefamulin and ceritinib both increase QTc interval. Avoid or Use Alternate Drug.
- lemborexant
ceritinib 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
ceritinib and levofloxacin both increase QTc interval. Avoid or Use Alternate Drug.
- lithium
ceritinib and lithium both increase QTc interval. Avoid or Use Alternate Drug.
- lofexidine
ceritinib and lofexidine both increase QTc interval. Avoid or Use Alternate Drug.
- loperamide
ceritinib and loperamide both increase QTc interval. Avoid or Use Alternate Drug.
- lopinavir
lopinavir increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
ceritinib and lopinavir both increase QTc interval. Avoid or Use Alternate Drug. - lurbinectedin
ceritinib will increase the level or effect of lurbinectedin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- maprotiline
ceritinib and maprotiline both increase QTc interval. Avoid or Use Alternate Drug.
- mefloquine
ceritinib and mefloquine both increase QTc interval. Avoid or Use Alternate Drug.
- methadone
ceritinib and methadone both increase QTc interval. Avoid or Use Alternate Drug.
- midazolam intranasal
ceritinib 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.
- midostaurin
ceritinib and midostaurin both increase QTc interval. Avoid or Use Alternate Drug.
- mifepristone
ceritinib and mifepristone both increase QTc interval. Avoid or Use Alternate Drug.
- mirtazapine
ceritinib and mirtazapine both increase QTc interval. Avoid or Use Alternate Drug.
- mitotane
mitotane decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mobocertinib
ceritinib 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.
- moxifloxacin
ceritinib and moxifloxacin both increase QTc interval. Avoid or Use Alternate Drug.
- nafcillin
nafcillin decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- naloxegol
ceritinib will increase the level or effect of naloxegol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministation of naloxegol with moderate CYP3A4 inhibitors is unavoidable, reduce naloxegol dose to 12.5 mg qDay
- nefazodone
nefazodone increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- nelfinavir
nelfinavir increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- nevirapine
nevirapine decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- nicardipine
nicardipine increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- nilotinib
ceritinib and nilotinib both increase QTc interval. Avoid or Use Alternate Drug.
- octreotide
ceritinib and octreotide both increase QTc interval. Avoid or Use Alternate Drug.
- ofloxacin
ceritinib and ofloxacin both increase QTc interval. Avoid or Use Alternate Drug.
- olanzapine
ceritinib and olanzapine both increase 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
- olaparib
ceritinib will increase the level or effect of olaparib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with moderate CYP3A inhibitors cannot be avoided, reduce olaparib dose to 200 mg (capsule) or 150 mg (tablet) PO BID. Do not substitute tablets with capsules.
- omeprazole
omeprazole decreases effects of ceritinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.
- ondansetron
ceritinib and ondansetron both increase QTc interval. Avoid or Use Alternate Drug.
- osimertinib
ceritinib and osimertinib both increase QTc interval. Avoid or Use Alternate Drug.
- oxaliplatin
ceritinib and oxaliplatin both increase QTc interval. Avoid or Use Alternate Drug.
- oxcarbazepine
oxcarbazepine decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ozanimod
ceritinib and ozanimod both increase QTc interval. Avoid or Use Alternate Drug.
- palifermin
palifermin increases toxicity of ceritinib 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
ceritinib and paliperidone both increase QTc interval. Avoid or Use Alternate Drug.
- panobinostat
ceritinib and panobinostat both increase QTc interval. Avoid or Use Alternate Drug. Panobinostat is known to significantly prolong QT interval. Panobinostat prescribing information states use with drugs known to prolong QTc is not recommended.
- pasireotide
ceritinib and pasireotide both increase QTc interval. Avoid or Use Alternate Drug.
- pazopanib
ceritinib and pazopanib both increase QTc interval. Avoid or Use Alternate Drug.
- pemigatinib
ceritinib 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
ceritinib and pentamidine both increase QTc interval. Avoid or Use Alternate Drug.
- pentobarbital
pentobarbital decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- pexidartinib
ceritinib 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 decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- phenytoin
phenytoin decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
ceritinib increases levels of phenytoin by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP2C9 substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP2C9 during treatment with ceritinib; if use of these medications is unavoidable, consider dose. - pimavanserin
ceritinib and pimavanserin both increase QTc interval. Avoid or Use Alternate Drug.
- pimozide
ceritinib increases levels of pimozide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP3A substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP3A during treatment with ceritinib; if use of these medications is unavoidable, consider dose.
ceritinib and pimozide both increase QTc interval. Contraindicated. - pitolisant
ceritinib and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.
- ponesimod
ponesimod, ceritinib. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Consult cardiologist if considering treatment. Coadministration of ponesimod with drugs that decrease HR may have additive effects on decreasing HR and should generally not be initiated in these patients.
ceritinib and ponesimod both increase QTc interval. Avoid or Use Alternate Drug. - posaconazole
posaconazole increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- primaquine
ceritinib and primaquine both increase QTc interval. Avoid or Use Alternate Drug.
- primidone
primidone decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- procainamide
ceritinib and procainamide both increase QTc interval. Avoid or Use Alternate Drug.
- propafenone
ceritinib and propafenone both increase QTc interval. Avoid or Use Alternate Drug.
- propofol
ceritinib increases levels of propofol by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP2C9 substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP2C9 during treatment with ceritinib; if use of these medications is unavoidable, consider dose.
- quetiapine
ceritinib and quetiapine both increase QTc interval. Avoid or Use Alternate Drug.
- quinidine
quinidine increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
ceritinib increases levels of quinidine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP3A substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP3A during treatment with ceritinib; if use of these medications is unavoidable, consider dose.
ceritinib and quinidine both increase QTc interval. Avoid or Use Alternate Drug. - quinine
ceritinib and quinine both increase QTc interval. Avoid or Use Alternate Drug.
- ribociclib
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. - rifabutin
rifabutin decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifampin
rifampin decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifapentine
rifapentine decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rilpivirine
ceritinib and rilpivirine both increase QTc interval. Avoid or Use Alternate Drug.
- risperidone
ceritinib and risperidone both increase QTc interval. Avoid or Use Alternate Drug.
- ritonavir
ritonavir increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- romidepsin
ceritinib and romidepsin both increase QTc interval. Avoid or Use Alternate Drug.
- saquinavir
saquinavir increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- selpercatinib
ceritinib and selpercatinib both increase QTc interval. Avoid or Use Alternate Drug.
- selumetinib
ceritinib 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
ceritinib and sertraline both increase QTc interval. Avoid or Use Alternate Drug.
- sevoflurane
ceritinib and sevoflurane both increase QTc interval. Avoid or Use Alternate Drug.
- siponimod
ceritinib will increase the level or effect of siponimod by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. Coadministration of siponimod with drugs that cause moderate CYP2C9 AND a moderate or strong CYP3A4 inhibition is not recommended. Caution if siponimod coadministered with moderate CYP2C9 inhibitors alone.
ceritinib 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.
ceritinib and siponimod both increase QTc interval. Avoid or Use Alternate Drug. - sirolimus
ceritinib increases levels of sirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP3A substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP3A during treatment with ceritinib; if use of these medications is unavoidable, consider dose.
- solifenacin
ceritinib and solifenacin both increase QTc interval. Avoid or Use Alternate Drug.
- sorafenib
ceritinib and sorafenib both increase QTc interval. Avoid or Use Alternate Drug.
- sotalol
ceritinib and sotalol both increase QTc interval. Avoid or Use Alternate Drug.
- sotorasib
sotorasib will decrease the level or effect of ceritinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.
- St John's Wort
St John's Wort decreases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- sunitinib
ceritinib and sunitinib both increase QTc interval. Avoid or Use Alternate Drug.
- tacrolimus
ceritinib increases levels of tacrolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP3A substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP3A during treatment with ceritinib; if use of these medications is unavoidable, consider dose.
ceritinib and tacrolimus both increase QTc interval. Avoid or Use Alternate Drug. - tazemetostat
ceritinib 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
ceritinib and telavancin both increase QTc interval. Avoid or Use Alternate Drug.
- tepotinib
tepotinib will increase the level or effect of ceritinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
- tetrabenazine
ceritinib and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.
- theophylline
ceritinib increases levels of theophylline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP3A substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP3A during treatment with ceritinib; if use of these medications is unavoidable, consider dose.
- tipranavir
tipranavir increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
- toremifene
ceritinib and toremifene both increase QTc interval. Avoid or Use Alternate Drug.
- trazodone
ceritinib and trazodone both increase QTc interval. Avoid or Use Alternate Drug.
- triclabendazole
ceritinib and triclabendazole both increase QTc interval. Avoid or Use Alternate Drug.
- tucatinib
tucatinib will increase the level or effect of ceritinib 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.
- vandetanib
ceritinib and vandetanib both increase QTc interval. Avoid or Use Alternate Drug.
- vardenafil
ceritinib and vardenafil both increase QTc interval. Avoid or Use Alternate Drug.
- vemurafenib
ceritinib and vemurafenib both increase QTc interval. Avoid or Use Alternate Drug.
- venetoclax
ceritinib will increase the level or effect of venetoclax by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If a moderate CYP3A inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- voriconazole
voriconazole increases levels of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid if possible; if concomitant use is unavoidable, reduce ceritinib dose by ~33%; after discontinuation of strong CYP3A inhibitor, resume at previous dose.
ceritinib and voriconazole both increase QTc interval. Avoid or Use Alternate Drug. - vorinostat
ceritinib and vorinostat both increase QTc interval. Avoid or Use Alternate Drug.
- voxelotor
voxelotor will increase the level or effect of ceritinib 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.
- warfarin
ceritinib increases levels of warfarin by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. Avoid concurrent use of CYP2C9 substrates known to have narrow therapeutic indices or substrates primarily metabolized by CYP2C9 during treatment with ceritinib; if use of these medications is unavoidable, consider dose.
- ziprasidone
ceritinib and ziprasidone both increase QTc interval. Avoid or Use Alternate Drug.
Monitor Closely (126)
- abiraterone
abiraterone increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- acalabrutinib
ceritinib 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.
- afatinib
afatinib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- amiodarone
amiodarone increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- amitriptyline
ceritinib and amitriptyline both increase QTc interval. Use Caution/Monitor.
- arformoterol
ceritinib and arformoterol both increase QTc interval. Use Caution/Monitor.
- atogepant
ceritinib will increase the level or effect of atogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- atorvastatin
atorvastatin increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- avatrombopag
ceritinib will increase the level or effect of avatrombopag by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. When treating ITP, coadministration of avatrombopag with a moderate or strong dual CYP2C9/3A4 inhibitor requires a decreased avatrombopag starting dose. Refer to drug monograph for specific recommendations.
- azithromycin
azithromycin increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- belzutifan
belzutifan will decrease the level or effect of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.
- berotralstat
berotralstat will increase the level or effect of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered.
- brexpiprazole
ceritinib will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.
- buprenorphine subdermal implant
ceritinib 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, long-acting injection
ceritinib 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.
- cannabidiol
ceritinib 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.
- carvedilol
carvedilol increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- clarithromycin
clarithromycin increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- clomipramine
ceritinib and clomipramine both increase QTc interval. Use Caution/Monitor.
- crizotinib
crizotinib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- cyclosporine
cyclosporine increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- darunavir
darunavir increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- deflazacort
ceritinib will increase the level or effect of deflazacort by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Decrease deflazacort dose to one-third of the recommended dose if coadministered with moderate or strong CYP3A4 inhibitors.
- desipramine
ceritinib and desipramine both increase QTc interval. Use Caution/Monitor.
- diazepam intranasal
ceritinib 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.
- dipyridamole
dipyridamole increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- dronedarone
dronedarone increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- duvelisib
duvelisib will increase the level or effect of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. will increase the level or effect of
- elagolix
elagolix will increase the level or effect of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
elagolix will decrease the level or effect of ceritinib 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. - elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- encorafenib
encorafenib, ceritinib. 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.
- erythromycin base
erythromycin base increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- erythromycin lactobionate
erythromycin lactobionate increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- erythromycin stearate
erythromycin stearate increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- etravirine
etravirine increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- fedratinib
fedratinib will increase the level or effect of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- finerenone
ceritinib 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.
- fluphenazine
ceritinib and fluphenazine both increase QTc interval. Use Caution/Monitor.
- formoterol
ceritinib and formoterol both increase QTc interval. Use Caution/Monitor.
- fostemsavir
ceritinib and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.
- gemtuzumab
ceritinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.
- goserelin
goserelin increases toxicity of ceritinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- grapefruit
grapefruit increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- guanfacine
ceritinib will increase the level or effect of guanfacine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Strong or moderate CYP3A4 inhibitors significantly increase guanfacine plasma concentrations. FDA-approved labeling for extended-release (ER) guanfacine recommends that, if coadministered, the guanfacine dosage should be decreased to half of the recommended dose. Specific recommendations for immediate-release (IR) guanfacine are not available.
- histrelin
histrelin increases toxicity of ceritinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- ibrutinib
ceritinib 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.
- ifosfamide
ceritinib will decrease the level or effect 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.
- indacaterol, inhaled
ceritinib and indacaterol, inhaled both increase QTc interval. Use Caution/Monitor.
- irinotecan
ceritinib will increase the level or effect of irinotecan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- irinotecan liposomal
ceritinib will increase the level or effect of irinotecan liposomal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- isavuconazonium sulfate
ceritinib will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- isradipine
ceritinib and isradipine both increase QTc interval. Use Caution/Monitor.
- istradefylline
istradefylline will increase the level or effect of ceritinib 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.
istradefylline will increase the level or effect of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates. - ivacaftor
ivacaftor increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Ivacaftor and its M1 metabolite has the potential to inhibit P-gp; may significantly increase systemic exposure to sensitive P-gp substrates with a narrow therapeutic index.
ceritinib 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
ceritinib 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.
- ketoconazole
ketoconazole increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- lapatinib
lapatinib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- lefamulin
ceritinib 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.
- lenvatinib
ceritinib and lenvatinib both increase QTc interval. Use Caution/Monitor. Lenvatinib prescribing information recommends monitoring ECG closely when coadministered with QT prolonging drugs.
- leuprolide
leuprolide increases toxicity of ceritinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- levalbuterol
ceritinib and levalbuterol both increase QTc interval. Use Caution/Monitor.
- levamlodipine
ceritinib 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.
- lomitapide
lomitapide increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- lopinavir
lopinavir increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- lovastatin
lovastatin increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- mefloquine
mefloquine increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- metformin
ceritinib decreases effects of metformin by pharmacodynamic antagonism. Use Caution/Monitor.
- mifepristone
mifepristone increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
mifepristone, ceritinib. Either increases toxicity of the other by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. May increase QT prolongation. - mometasone inhaled
mometasone inhaled increases toxicity of ceritinib by Other (see comment). Use Caution/Monitor. Comment: Corticosteroids may increase hypoglycemic effects of ceritinib.
- mometasone topical
mometasone topical decreases effects of ceritinib by Other (see comment). Modify Therapy/Monitor Closely. Comment: Closely monitor for severe hyperglycemia (serum glucose >250 mg/dL) and treat appropriately. Patients with history of diabetes or glucose intolerance are at increased risk. .
- mometasone, intranasal
mometasone, intranasal increases toxicity of ceritinib by Other (see comment). Modify Therapy/Monitor Closely. Comment: May increase risk of hyperglycemia.
- naldemedine
ceritinib 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.
- nelfinavir
nelfinavir increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- nicardipine
nicardipine increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- nifedipine
nifedipine increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- nilotinib
nilotinib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- nortriptyline
ceritinib and nortriptyline both increase QTc interval. Use Caution/Monitor.
- oliceridine
ceritinib 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.
- olodaterol inhaled
ceritinib and olodaterol inhaled both increase QTc interval. Use Caution/Monitor.
- osilodrostat
osilodrostat and ceritinib both increase QTc interval. Use Caution/Monitor.
- oxaliplatin
oxaliplatin will increase the level or effect of ceritinib by Other (see comment). Use Caution/Monitor. Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT interval.
- palbociclib
ceritinib will increase the level or effect of palbociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- paliperidone
paliperidone increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- pantoprazole
pantoprazole will decrease the level or effect of ceritinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely.
- perphenazine
ceritinib and perphenazine both increase QTc interval. Use Caution/Monitor.
- ponatinib
ponatinib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- posaconazole
posaconazole increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- progesterone micronized
progesterone micronized increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- propafenone
propafenone increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- propranolol
propranolol increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- protriptyline
ceritinib and protriptyline both increase QTc interval. Use Caution/Monitor.
- quinidine
quinidine increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- quinine
quinine increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- rabeprazole
rabeprazole will decrease the level or effect of ceritinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely.
- ranolazine
ranolazine increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- rimegepant
ceritinib 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
ritonavir increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- rucaparib
rucaparib will increase the level or effect of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- saquinavir
saquinavir increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- sarecycline
sarecycline will increase the level or effect of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor for toxicities of P-gp substrates that may require dosage reduction when coadministered with P-gp inhibitors.
- simvastatin
simvastatin increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- siponimod
siponimod and ceritinib 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.
- sonidegib
ceritinib will increase the level or effect of sonidegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of sonidegib with moderate CYP3A4 inhibitors. If a moderate CYP3A inhibitor must be used, administer the moderate CYP3A inhibitor for <14 days and monitor closely for adverse reactions, particularly musculoskeletal adverse reactions.
- stiripentol
stiripentol, ceritinib. 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.
stiripentol will increase the level or effect of ceritinib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing the dose of P-glycoprotein (P-gp) substrates, if adverse reactions are experienced when administered concomitantly with stiripentol. - sufentanil SL
ceritinib 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
sunitinib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- suvorexant
ceritinib will increase the level or effect of suvorexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Decrease suvorexant starting dose to 5 mg HS if coadministered with moderate CYP3A4 inhibitors
- tacrolimus
tacrolimus increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- tamoxifen
tamoxifen increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- tazemetostat
tazemetostat will decrease the level or effect of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of ceritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- tezacaftor
ceritinib 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.
- ticagrelor
ticagrelor increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- tinidazole
ceritinib will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- trabectedin
ceritinib will increase the level or effect of trabectedin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- trimipramine
ceritinib and trimipramine both increase QTc interval. Use Caution/Monitor.
- triptorelin
triptorelin increases toxicity of ceritinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- tucatinib
tucatinib will increase the level or effect of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.
- ulipristal
ulipristal increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- vandetanib
vandetanib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- vemurafenib
vemurafenib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- verapamil
verapamil increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- vilanterol/fluticasone furoate inhaled
ceritinib and vilanterol/fluticasone furoate inhaled both increase QTc interval. Use Caution/Monitor.
- voclosporin
ceritinib 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.
- zanubrutinib
ceritinib will increase the level or effect of zanubrutinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce zanubrutinib dose when coadministered with a moderate CYP3A4 inhibitor. Interrupt dose as recommended for adverse reactions. After discontinuing the CYP3A4 inhibitor, resume previous dose of zanubrutinib. See zanubrutinib Dosage Modifications for precise recommendation.
Minor (1)
- estradiol vaginal
ceritinib will increase the level or effect of estradiol vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
>10% (All grades)
Increased alanine transaminase (ALT) (91%)
Increased aspartate transaminase (AST) (86%)
Diarrhea (85%)
Increased gamma-glutamyl transpeptidase (GGT) (84%)
Increased alkaline phosphatase (81%)
Increased creatinine (77%)
Nausea (69%)
Vomiting (67%)
Anemia (67%)
Hyperglycemia (53%)
Fatigue (45%)
Abdominal pain (40%)
Increased amylase (37%)
Decreased phosphate (38%)
Decreased appetite (34%)
Neutropenia (27%)
Cough (25%)
Weight loss (24%)
Constipation (20%)
Non-cardiac chest pain (21%)
Rash (21%)
Back pain (19%)
Pyrexia (19%)
Headache (19%)
Thrombocytopenia (16%)
Esophageal disorder (15%)
Increased total bilirubin (15%)
Dizziness (12%)
Prolonged QT interval (12%)
Musculoskeletal pain (11%)
Pruritus (11%)
>10% (Grades 3-4)
Increased gamma-glutamyl transpeptidase (GGT) (49%)
Increased alanine transaminase (ALT) (34%)
Increased aspartate transaminase (AST) (21%)
Increased alkaline phosphatase (12%)
1-10% (All Grades)
Pericarditis (4.2%)
1-10% (Grade 3-4)
Hyperglycemia (10%)
Increased amylase (8%)
Fatigue (7%)
Increased lipase (6%)
Vomiting (5%)
Diarrhea (4.8%)
Increased creatinine (4.2%)
Anemia (4.2%)
Abdominal pain (3.7%)
Weight loss (3.7%)
Decreased phosphate (3.7%)
Nausea (2.6%)
Pericarditis (2.6%)
Neutropenia (2.1%)
Back pain (1.6%)
Non-cardiac chest pain (1.6%)
Decreased appetite (1.1%)
Rash (1.1%)
Dizziness (1.1%)
Thrombocytopenia (1%)
<1% (Grade 3-4)
Esophageal disorder (0.5%)
Musculoskeletal pain (0.5%)
Increased bilirubin (0.5%)
Pruritus (0.5%)
Headache (0.5%)
Warnings
Contraindications
None
Cautions
Drug-induced hepatotoxicity reported; monitor with liver laboratory tests, including ALT, AST, and total bilirubin, once a month and as clinically indicated, with more frequent testing in patients who develop transaminase elevations; based on severity of adverse reaction, withhold drug with resumption at a reduced dose, or permanently discontinue therapy
May cause severe, life-threatening, or fatal interstitial lung disease/pneumonitis
May prolong QT interval; when possible, avoid use in patients with congenital long QT syndrome; conduct periodic monitoring with ECGs and electrolytes in patients with congestive heart failure, bradyarrhythmias, electrolyte abnormalities, or those who are taking medications that are known to prolong the QTc interval; based on severity of adverse reaction, withhold drug, with resumption at a reduced dose, or permanently discontinue therapy
Hyperglycemia reported; monitor fasting serum glucose prior to the start of treatment and periodically thereafter as clinically indicated; initiate or optimize anti-hyperglycemic medications as indicated; based on severity, withhold then dose reduce, or permanently discontinue therapy
Pancreatitis reported in less than 1% of patients receiving therapy; monitor lipase and amylase prior to initiating therapy and periodically thereafter as clinically indicated; based on severity of laboratory abnormalities, withhold and resume gradually
Based on its mechanism of action, may cause fetal harm when administered to a pregnant woman (see Pregnancy)
Severe, life-threatening, or fatal ILD/pneumonitis occurred; monitor for pulmonary symptoms indicative of ILD/pneumonitis; exclude other potential causes of ILD/pneumonitis, and permanently discontinue ceritinib in patients diagnosed with treatment-related ILD/pneumonitis
Bradycardia
- Avoid using drug in combination with other products known to cause bradycardia (eg, beta-blockers, non- dihydropyridine calcium channel blockers, clonidine, and digoxin) to the extent possible
- Monitor heart rate and blood pressure regularly; based on severity of adverse reaction, withhold drug with resumption at a reduced dose upon resolution of bradycardia, or permanently discontinue therapy
Gastrointestinal adverse reactions
- Diarrhea, nausea, vomiting, or abdominal pain occurs in most patients, of which 14% have severe symptoms; monitor and manage patients using standards of care, including antidiarrheals, antiemetics, or fluid replacement, as indicated; based on severity of adverse drug reaction, withhold therapy with resumption at reduced dose
- Data in the prescribing information reflect the safety of ceritinib 750 mg daily under fasted conditions in 925 patients with ALK-positive NSCLC across a pool of seven clinical studies at systemic exposures similar to the recommended dose of 450 mg with food
- The incidence and severity of gastrointestinal adverse reactions were reduced for patients treated with 450 mg with food in a dose optimization study (ASCEND-8)
- Monitor and manage patients using standard of care, including antidiarrheals, antiemetics, or fluid replacement, as indicated; withhold therapy if gastrointestinal adverse reaction is severe or intolerable and not responsive to antiemetics or antidiarrheals; upon improvement, resume therapy at a reduced dose
Drug interactions overview
- Also see Dosage Modifications
- Coadministration with a strong CYP3A4/P-gp inhibitor (ketoconazole) increased systemic exposure of ceritinib
- Avoid grapefruit and grapefruit juice consumption; may inhibit CYP3A
- Coadministration with a strong CYP3A4/P-gp inducer (rifampin) decreased systemic exposure of ceritinib
- Avoid concurrent use of CYP3A and CYP2C9 substrates known to have narrow therapeutic indexes or substrates primarily metabolized by CYP3A and CYP2C9 during treatment; if use of these medications is unavoidable, consider dose reduction of CYP3A substrates with narrow therapeutic indexes (eg, alfentanil, cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, tacrolimus) and CYP2C9 substrates with narrow therapeutic indexes (eg, phenytoin, warfarin)
Pregnancy & Lactation
Pregnancy
Verify pregnancy status in females of reproductive potential prior to initiating therapy
Based on animal studies and its mechanism of action, therapy can cause fetal harm when administered to a pregnant woman; limited data available on use in pregnant women are insufficient to inform a risk; administration to rats and rabbits during period of organogenesis at maternal plasma exposures below the recommended human dose caused increases in skeletal anomalies in rats and rabbits; advise pregnant women of potential risk to fetus
Advise females of reproductive potential to use effective contraception during treatment with and for 6 months following completion of therapy
Based on potential for genotoxicity, advise males with female partners of reproductive potential to use condoms during treatment and for 3 months following completion of therapy
Lactation
There are no data regarding presence of ceritinib or metabolites in human milk; effects of ceritinib on breastfed infant, or effects on milk production; because of potential for serious adverse reactions including gastrointestinal toxicity, hepatotoxicity, pneumonitis, bradycardia and pancreatitis, advise a woman not to breastfeed during treatment and for 2 weeks following completion of therapy
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
Tyrosine kinase inhibitor that targets anaplastic lymphoma kinase (ALK), insulinlike growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1
Inhibits autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells (in vitro and in vivo assays)
Absorption
Peak plasma time: 4-6 hr
High-fat meal increases AUC by 58% and Cmax by 43% compared with fasting (take on empty stomach 2 hr before or 2 hr after meals)
Distribution
Protein bound: 97%
Vd: 4230 L
Slight preferential distribution to RBCs, relative to plasma, with a mean in vitro blood-to-plasma ratio of 1.35
Metabolism
CYP3A (major enzymatic pathway)
Following a single 750-mg radiolabeled ceritinib dose, ceritinib as the parent compound was the main circulating component (82%) in human plasma
Elimination
Half-life: 41 hr
Clearance: 33.2 L/hr (steady-state); 88.5 L/hr (single dose)
Excretion: 92.3% feces (68% as unchanged parent compound); 1.3% urine
Administration
Oral Administration
Take with food
Missed dose: If a dose is missed, make up that dose unless the next dose is due within 12 hr
Vomited dose: If vomiting occurs during the course of treatment, do not administer an additional dose; continue with the next scheduled dose
Storage
Tablets: Store at room temperature, 25°C (77°F); excursions permitted between 15-30°C (59-86°F)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Zykadia oral - | 150 mg capsule |  | |
| Zykadia oral - | 150 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
ceritinib oral
CERITINIB - ORAL
(se-RI-ti-nib)
COMMON BRAND NAME(S): Zykadia
USES: Ceritinib is used to treat lung cancer. It is used for lung cancers that have a certain type of abnormal "ALK" gene. Ceritinib belongs to a class of drugs known as kinase inhibitors. It works by slowing or stopping the growth of cancer cells.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking ceritinib and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with food as directed by your doctor, usually once daily.The dosage is based on your medical condition, laboratory tests, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Drugs that reduce stomach acid (including antacids, proton pump inhibitors such as omeprazole, H2 blockers such as ranitidine) may make you absorb less ceritinib. This could make ceritinib work less well. Talk to your doctor or pharmacist if you are taking any of these medications.Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.Use this medication regularly to get the most benefit from it. To help you remember, use it at the same time each day.Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.If you vomit after taking a dose, do not take another dose at that time. Take your next dose at the regular time.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the capsules.
SIDE EFFECTS: Diarrhea, nausea, vomiting, abdominal pain, loss of appetite, heartburn, constipation, or tiredness may occur. Nausea and vomiting can be severe. In some cases, your doctor may prescribe medication to prevent or relieve nausea, vomiting, or diarrhea. Eating several small meals, not eating before treatment, or limiting activity may help lessen some of these effects. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.People using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.Tell your doctor right away if you have any serious side effects, including: numbness/tingling, symptoms of liver problems (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine), vision changes (such as blurred vision, decreased vision), weakness.Get medical help right away if you have any very serious side effects, including: trouble breathing, cough with or without phlegm, fast/slow/irregular heartbeat, severe dizziness, fainting, seizure.This medication may rarely make your blood sugar rise, which can cause or worsen diabetes. Tell your doctor right away if you have symptoms of high blood sugar such as increased thirst/urination. If you already have diabetes, check your blood sugar regularly as directed and share the results with your doctor. Your doctor may need to adjust your diabetes medication, exercise program, or diet.Persistent vomiting/diarrhea may result in dehydration. Contact your doctor promptly if you notice any symptoms of dehydration, such as unusual decreased urination, unusual dry mouth/thirst, fast heartbeat, or dizziness/lightheadedness.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.Ceritinib can commonly cause a rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe reaction. Tell your doctor right away if you develop any rash.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking this medication, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes or high blood sugar, liver problems.Ceritinib may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using ceritinib, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using ceritinib safely.This drug may rarely cause vision changes. Do not drive, use machinery, or do any activity that requires alertness or clear vision until you are sure you can perform such activities safely. Limit alcoholic beverages.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this drug, especially QT prolongation (see above).Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the capsules.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using ceritinib. Ceritinib may harm an unborn baby. Your doctor should order a pregnancy test before you start this medication. Women using this medication should ask about reliable forms of birth control during treatment and for 6 months after stopping treatment. Men using this medication should use condoms for birth control during treatment and for 3 months after stopping treatment. If you or your partner become pregnant or think you may be pregnant, tell your doctor right away.It is unknown if this medication passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended and for 2 weeks after stopping treatment. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: other drugs that may slow the heartbeat (including digoxin, clonidine, beta-blockers such as atenolol/metoprolol, calcium channel blockers such as diltiazem/verapamil).Other medications can affect the removal of ceritinib from your body, which may affect how ceritinib works. Examples include azole antifungals (such as itraconazole, ketoconazole), macrolide antibiotics (such as erythromycin), rifamycins (such as rifampin, rifabutin), drugs for seizures (such as carbamazepine, phenytoin), St. John's wort, among others.This medication can slow down the removal of other medications from your body, which may affect how they work. Examples include alfentanil, asunaprevir, ergots (such as ergotamine), fentanyl, finerenone, flibanserin, ivabradine, lurasidone, tacrolimus, triazolam, among others.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as liver function, blood sugar, EKG, complete blood counts, heart rate, amylase/lipase level) should be done before you start taking this medication and while you are taking it. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is less than 12 hours before the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised September 2021. Copyright(c) 2021 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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