Dosing & Uses
Dosage Forms & Strengths
capsule
- 12.5mg
- 25mg
- 50mg
Gastrointestinal Stromal Tumor
Indicated for treatment of gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to imatinib mesylate
50 mg PO qDay for 4 weeks, THEN 2 weeks drug-free, repeat cycle
Continue until disease progression or unacceptable toxicity
Renal Cell Carcinoma
Indicated for treatment of advanced renal cell carcinoma (RCC)
50 mg PO qDay for 4 weeks, THEN 2 weeks drug-free, repeat cycle
Continue until disease progression or unacceptable toxicity
Adjuvant treatment of RCC
- Indicated for the adjuvant treatment of adult patients at high risk of recurrent RCC following nephrectomy
- 50 mg PO qDay for 4 weeks, THEN 2 weeks drug-free, repeat cycle for a total of nine 6-week cycles
Pancreatic Neuroendocrine Tumors
Indicated for progressive, well-differentiated pancreatic neuroendocrine tumors (pNET) in patients with unresectable locally advanced or metastatic disease
37.5 mg PO qDay continuously without a scheduled off-treatment period
Continue until disease progression or unacceptable toxicity
Dosage Modifications
Dosage modifications for adverse reactions
- Dose interruption and/or dose modification in 12.5-mg increments or decrements is recommended based on individual safety and tolerability
- Maximum dose administered in the pNET study was 50 mg daily
- In the adjuvant RCC study, the minimum dose administered was 37.5 mg
Coadministration with CYP3A4 inhibitors or inducers
-
Strong CYP3A4 inhibitors
- Use an alternative with no or minimal enzyme inhibition potential is recommended
- If coadministration is unavoidable, consider reducing sunitinib dose to a minimum of 37.5 mg (GIST and RCC) or 25 mg (pNET) PO qDay
-
Strong CYP3A4 inducers
- Use an alternative with no or minimal enzyme inhibition potential is recommended
- Consider increasing sunitinib dose to a maximum of 87.5 mg (GIST and RCC) or 62.5 mg (pNET) daily if coadministered with a CYP3A4 inducer cannot be avoided
- If dose is increased, monitor carefully for toxicity
Renal impairment
- No dose adjustment necessary with any degree of renal impairment in patients not on dialysis
- ESRD on hemodialysis: No adjustment to the starting dose is required; however, compared to patients with normal renal function, the sunitinib exposure is 47% lower in patients with ESRD on hemodialysis; may require gradual dose increase (up to 2-fold) based on safety and tolerability
Hepatic impairment
- Mild to moderate (Child-Pugh Class A or B): Dose adjustment not necessary for initial dose; monitor subsequent doses
- Severe (Child-Pugh Class C): Not studied
Dosing Considerations
Monitor CBC count, blood chemistries
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- lefamulin
lefamulin will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Lefamulin is contraindicated with CYP3A substrates know to prolong the QT interval.
Serious - Use Alternative (56)
- abametapir
abametapir will increase the level or effect of sunitinib 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.
- afatinib
sunitinib increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.
- alpelisib
sunitinib will increase the level or effect of alpelisib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of alpelisib (BCRP substrate) with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. If unable to avoid or use alternant drugs, closely monitor for increased adverse reactions.
- apalutamide
apalutamide will decrease the level or effect of sunitinib 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.
- bevacizumab
bevacizumab, sunitinib. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of bevacizumab and sunitinib is not recommended. Cases of microangiopathic hemolytic anemia (MAHA) have been reported. .
- bosutinib
sunitinib increases levels of bosutinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- chloramphenicol
chloramphenicol will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- cimetidine
cimetidine will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- clarithromycin
clarithromycin will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- cobicistat
cobicistat will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- deferiprone
deferiprone, sunitinib. 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.
- dofetilide
dofetilide increases toxicity of sunitinib by QTc interval. Avoid or Use Alternate Drug.
- edoxaban
sunitinib will increase the level or effect of edoxaban by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Dose adjustment may be required with strong P-gp inhibitors. DVT/PE treatment: Decrease dose to 30 mg PO once daily. NVAF: No dose reduction recommended
- entrectinib
sunitinib and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.
- enzalutamide
enzalutamide will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- eribulin
eribulin and sunitinib both increase QTc interval. Avoid or Use Alternate Drug. Potential for enhanced QTc-prolonging effects; if concurrent use is necessary then ECG monitoring is recommended.
- erythromycin base
erythromycin base will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin stearate
erythromycin stearate will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- fexinidazole
fexinidazole and sunitinib both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels or prolong QT interval.
- glasdegib
sunitinib and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.
- hydroxychloroquine sulfate
hydroxychloroquine sulfate and sunitinib both increase QTc interval. Avoid or Use Alternate Drug.
- idelalisib
idelalisib will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates
- inotuzumab
inotuzumab and sunitinib 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.
- ivosidenib
ivosidenib will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
- ketoconazole
ketoconazole will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- lonafarnib
lonafarnib will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.
- lopinavir
lopinavir will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- macimorelin
macimorelin and sunitinib 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.
- nefazodone
nefazodone will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ondansetron
ondansetron and sunitinib both increase QTc interval. Avoid or Use Alternate Drug. Avoid with congenital long QT syndrome; ECG monitoring recommended with concomitant medications that prolong QT interval, electrolyte abnormalities, CHF, or bradyarrhythmias.
- ozanimod
sunitinib increases toxicity of ozanimod by Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of ozanimod (a BCRP substrate) with BCRP inhibitors increases the exposure of the minor (RP101988, RP101075) and major active metabolites (CC112273, CC1084037) of ozanimod, which may increase the risk of ozanimod adverse reactions. .
- palifermin
palifermin increases toxicity of sunitinib 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.
- panobinostat
sunitinib 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.
- pitolisant
sunitinib and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.
- pomalidomide
sunitinib increases levels of pomalidomide by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
- ribociclib
ribociclib increases toxicity of sunitinib by QTc interval. Avoid or Use Alternate Drug.
- rifabutin
rifabutin will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifampin
rifampin will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rimegepant
sunitinib will increase the level or effect of rimegepant by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of rimegepant (a BCRP substrate) with inhibitors of BCRP.
- riociguat
sunitinib will increase the level or effect of riociguat by decreasing metabolism. Avoid or Use Alternate Drug. Coadministration of riociguat (substrate of CYP isoenzymes 1A1, 2C8, 3A, 2J2) with strong CYP inhibitors may require a decreased initial dose of 0.5 mg PO TID; monitor for signs of hypotension and reduce dose if needed
sunitinib will increase the level or effect of riociguat by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Coadministration of riociguat (P-gp substrate) with strong P-gp inhibitors may require a decreased initial dose of 0.5 mg PO TID; monitor for signs of hypotension and reduce dose if needed - saquinavir
saquinavir increases levels of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Potential for increased toxicity. Increased risk of QT prolongation and cardiac arrhythmias.
- selinexor
selinexor, sunitinib. unspecified interaction mechanism. Avoid or Use Alternate Drug. Patients treated with selinexor may experience neurological toxicities. Avoid taking selinexor with other medications that may cause dizziness or confusion.
- St John's Wort
St John's Wort will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- talazoparib
sunitinib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- temsirolimus
temsirolimus, sunitinib. Either increases toxicity of the other by Mechanism: unspecified interaction mechanism. Avoid or Use Alternate Drug. Combo may cause severe rash, gout, cellulitis.
- toremifene
sunitinib and toremifene both increase QTc interval. Avoid or Use Alternate Drug. Concurrent use of toremifene with agents causing QT prolongation should be avoided. If concomitant use is required it's recommended that toremifene be interrupted. If interruption not possible, patients requiring therapy with a drug that prolongs QT should be closely monitored. ECGs should be obtained for high risk patients.
- tucatinib
tucatinib will increase the level or effect of sunitinib 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.
- umeclidinium bromide/vilanterol inhaled
sunitinib increases toxicity of umeclidinium bromide/vilanterol inhaled by QTc interval. Avoid or Use Alternate Drug. Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be potentiated.
- vandetanib
sunitinib, vandetanib. Either increases toxicity of the other by QTc interval. Avoid or Use Alternate Drug. Avoid coadministration with drugs known to prolong QT interval; if a drug known to prolong QT interval must be used, more frequent ECG monitoring is recommended.
- vemurafenib
vemurafenib and sunitinib both increase QTc interval. Avoid or Use Alternate Drug. Concomitant use of vemurafenib with drugs that prolong QT interval is not recommended.
- venetoclax
sunitinib will increase the level or effect of venetoclax by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If a P-gp inhibitor must be used, reduce the venetoclax dose by at least 50%. Monitor more closely for signs of venetoclax toxicities.
- vilanterol/fluticasone furoate inhaled
sunitinib increases toxicity of vilanterol/fluticasone furoate inhaled by QTc interval. Avoid or Use Alternate Drug. Exercise extreme caution when vilanterol coadministered with drugs that prolong QTc interval; adrenergic agonist effects on the cardiovascular system may be potentiated.
- voxelotor
voxelotor will increase the level or effect of sunitinib 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.
Monitor Closely (125)
- acalabrutinib
acalabrutinib, sunitinib. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may increase risk of myelosuppressive effects.
- alfuzosin
sunitinib and alfuzosin both increase QTc interval. Use Caution/Monitor.
- amobarbital
amobarbital will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- aprepitant
aprepitant will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- armodafinil
armodafinil will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- artemether/lumefantrine
artemether/lumefantrine will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- atazanavir
atazanavir will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- bedaquiline
sunitinib and bedaquiline both increase QTc interval. Modify Therapy/Monitor Closely. ECG should be monitored closely
- berotralstat
sunitinib increases levels of berotralstat by Other (see comment). Modify Therapy/Monitor Closely. Comment: Reduced dose of berotralstat (a BCRP substrate) to 110 mg/day when coadministered with BCRP inhibitors.
- betrixaban
sunitinib increases levels of betrixaban by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Decrease betrixaban dose to 80 mg PO once, then 40 mg PO qDay if coadministered with a P-gp inhibitor.
- bosentan
bosentan will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- budesonide
budesonide will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- butabarbital
butabarbital will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- butalbital
butalbital will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cenobamate
cenobamate will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- ceritinib
sunitinib increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- ciprofloxacin
ciprofloxacin and sunitinib both increase QTc interval. Use Caution/Monitor. Ciprofloxacin elicits minimal effects on QT interval. Caution if used in combination with other drugs known to affect QT interval or in patients with other risk factors.
- citalopram
sunitinib and citalopram both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended, along with drugs that may prolong the QT interval.
- conivaptan
conivaptan will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- cortisone
cortisone will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- crizotinib
crizotinib increases effects of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Dose reduction may be needed for coadministered drugs that are predominantly metabolized by CYP3A. ECG monitoring is recommended, along with drugs that may prolong the QT interval.
- crofelemer
crofelemer increases levels of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.
- cyclosporine
cyclosporine will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dabigatran
sunitinib will increase the level or effect of dabigatran by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Atrial fibrillation: Avoid coadministering dabigatran with P-gp inhibitors if CrCl <30 mL/min. DVT/PE treatment: Avoid coadministering dabigatran with P-gp inhibitors if CrCl <50 mL/min
- dabrafenib
dabrafenib will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- darifenacin
darifenacin will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- darunavir
darunavir will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dasatinib
dasatinib will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- deferasirox
deferasirox will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- denosumab
sunitinib, denosumab. Other (see comment). Use Caution/Monitor. Comment: Caution should be taken in patients on concomitant immunosuppressants or with impaired immune systems because of increased risk for serious infections.
- dexamethasone
dexamethasone will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- DHEA, herbal
DHEA, herbal will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dichlorphenamide
dichlorphenamide and sunitinib both decrease serum potassium. Use Caution/Monitor.
- diltiazem
diltiazem will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dronedarone
dronedarone will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- duvelisib
duvelisib will increase the level or effect of sunitinib 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.
sunitinib will increase the level or effect of duvelisib by Other (see comment). Use Caution/Monitor. Coadministration of duvelisib (a BCRP substrate) with a BCRP transport inhibitor may increase levels or effects of duvelisib. - efavirenz
efavirenz will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- elagolix
elagolix decreases levels of sunitinib 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 sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.
- encorafenib
encorafenib, sunitinib. 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.
- escitalopram
escitalopram increases toxicity of sunitinib by QTc interval. Use Caution/Monitor.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- etravirine
etravirine will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ezogabine
ezogabine, sunitinib. Either increases toxicity of the other by QTc interval. Use Caution/Monitor. Slight and transient QT-prolongation observed with ezogabine, particularly when dose titrated to 1200 mg/day. QT interval should be monitored when ezogabine is prescribed with agents known to increase QT interval.
- fedratinib
fedratinib will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- fingolimod
sunitinib increases effects of fingolimod by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Concomitant therapy is expected to increase the risk of immunosuppression. Use caution when switching patients from long-acting therapies with immune effects. .
- fluconazole
fluconazole will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fluoxetine
sunitinib and fluoxetine both increase QTc interval. Modify Therapy/Monitor Closely.
- fluvoxamine
fluvoxamine will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fosamprenavir
fosamprenavir will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fosphenytoin
fosphenytoin will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fostemsavir
sunitinib and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.
- gemtuzumab
sunitinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.
- glecaprevir/pibrentasvir
sunitinib will increase the level or effect of glecaprevir/pibrentasvir by decreasing metabolism. Use Caution/Monitor. Caution when coadministering glecaprevir/pibrentasvir with P-gp/BCRP inhibitors.
- goserelin
goserelin increases toxicity of sunitinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- grapefruit
grapefruit will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- griseofulvin
griseofulvin will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- haloperidol
haloperidol and sunitinib both increase QTc interval. Use Caution/Monitor.
- histrelin
histrelin increases toxicity of sunitinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- iloperidone
iloperidone increases levels of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.
- indacaterol, inhaled
indacaterol, inhaled, sunitinib. QTc interval. Use Caution/Monitor. Drugs that are known to prolong the QTc interval may have an increased the risk of ventricular arrhythmias.
- indinavir
indinavir will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- isoniazid
isoniazid will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- istradefylline
istradefylline will increase the level or effect of sunitinib 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.
- lapatinib
lapatinib will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lenvatinib
sunitinib and lenvatinib both increase QTc interval. Use Caution/Monitor. Lenvatinib prescribing information recommends monitoring ECG closely when coadministered with QT prolonging drugs.
- letermovir
letermovir increases levels of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- leuprolide
leuprolide increases toxicity of sunitinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- lorlatinib
lorlatinib will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lumefantrine
lumefantrine will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- marijuana
marijuana will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- metronidazole
metronidazole will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- miconazole vaginal
miconazole vaginal will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mifepristone
mifepristone, sunitinib. QTc interval. Modify Therapy/Monitor Closely. Use alternatives if available.
mifepristone will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If concomitant use necessary, monitor patients for QT prolongation and consider reducing dose of sunitinib, based on individual safety and tolerability, in 12.5 mg decrements to minimum of 37.5 mg (GIST and RCC) or 25 mg (pNET) daily - mitotane
mitotane decreases levels of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.
- modafinil
modafinil will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nafcillin
nafcillin will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- naldemedine
sunitinib increases levels of naldemedine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor naldemedine for potential adverse effects if coadministered with P-gp inhibitors.
- nelfinavir
nelfinavir will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nevirapine
nevirapine will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nifedipine
nifedipine will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nilotinib
nilotinib will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nintedanib
sunitinib increases levels of nintedanib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. If nintedanib adverse effects occur, management may require interruption, dose reduction, or discontinuation of therapy .
- ofatumumab SC
ofatumumab SC, sunitinib. 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.
- olodaterol inhaled
sunitinib and olodaterol inhaled both increase QTc interval. Use Caution/Monitor. Drugs that prolong the QTc interval and may potentiate the effects of beta2 agonists on the cardiovascular system; increased risk of ventricular arrhythmias
- osilodrostat
osilodrostat and sunitinib both increase QTc interval. Use Caution/Monitor.
- osimertinib
osimertinib and sunitinib both increase QTc interval. Use Caution/Monitor. Conduct periodic monitoring with ECGs and electrolytes in patients taking drugs known to prolong the QTc interval.
- oxaliplatin
oxaliplatin will increase the level or effect of sunitinib by Other (see comment). Use Caution/Monitor. Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT interval.
- oxcarbazepine
oxcarbazepine will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ozanimod
ozanimod and sunitinib 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.
- pasireotide
sunitinib and pasireotide both increase QTc interval. Modify Therapy/Monitor Closely.
- pentobarbital
pentobarbital will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- phenobarbital
phenobarbital will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- phenytoin
phenytoin will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- posaconazole
posaconazole will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- primidone
primidone will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- quetiapine
quetiapine, sunitinib. Either increases toxicity of the other by QTc interval. Use Caution/Monitor. Avoid use with drugs that prolong QT and in patients with risk factors for prolonged QT interval. Postmarketing cases show QT prolongation with overdose in patients with concomitant illness or with drugs known to cause electrolyte imbalance or prolong QT.
- quinine
sunitinib and quinine both increase QTc interval. Use Caution/Monitor.
- quinupristin/dalfopristin
quinupristin/dalfopristin will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- ribociclib
ribociclib will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rifapentine
rifapentine will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rifaximin
sunitinib increases levels of rifaximin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- rilpivirine
rilpivirine increases toxicity of sunitinib by QTc interval. Use Caution/Monitor. Rilpivirine should be used with caution when co-administered with a drug with a known risk of Torsade de Pointes.
- ritonavir
ritonavir will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rucaparib
rucaparib will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- rufinamide
rufinamide will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- secobarbital
secobarbital will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- selexipag
sunitinib will increase the level or effect of selexipag by Other (see comment). Use Caution/Monitor. Selexipag is a ABCG2 (BCRP) substrate. Monitor selexipag for increased pharmacologic or adverse effects when coadministered with ABCG2 (BCRP) inhibitors.
- selpercatinib
selpercatinib increases toxicity of sunitinib by QTc interval. Use Caution/Monitor.
- siponimod
siponimod and sunitinib 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.
- sipuleucel-T
sunitinib decreases effects of sipuleucel-T by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
- sorafenib
sorafenib and sunitinib both increase QTc interval. Use Caution/Monitor.
- stiripentol
stiripentol, sunitinib. 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.
- tazemetostat
tazemetostat will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- teniposide
sunitinib will increase the level or effect of teniposide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.
- tipranavir
tipranavir increases levels of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Potential for increased toxicity. Use alternatives if available. Increased risk of QT prolongation and cardiac arrhythmias.
- topiramate
topiramate will decrease the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- trastuzumab
trastuzumab, sunitinib. 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, sunitinib. 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.
- triclabendazole
triclabendazole and sunitinib both increase QTc interval. Use Caution/Monitor.
- triptorelin
triptorelin increases toxicity of sunitinib by QTc interval. Use Caution/Monitor. Increases risk of torsades de pointes.
- verapamil
verapamil will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- voriconazole
voriconazole will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- zafirlukast
zafirlukast will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
Minor (2)
- azithromycin
azithromycin increases toxicity of sunitinib by QTc interval. Minor/Significance Unknown.
- chloroquine
chloroquine increases toxicity of sunitinib by QTc interval. Minor/Significance Unknown.
Adverse Effects
>10%
Dyspepsia (MRCC 46%)
Altered taste (MRCC 43%; GIST 21%)
Fatigue (GIST 42%; MRCC 74%)
Diarrhea (GIST 40%; MRCC 55%)
Rash (MRCC 38%; GIST 14%)
Vomiting (MRCC 37%; GIST 24%)
Constipation (MRCC 34%; GIST 20%)
Skin discoloration (MRCC 33%; GIST 30%)
Abdominal pain (GIST 33%; MRCC 20%)
Nausea (GIST 31%; MRCC 54%)
Anorexia (MRCC 31%; GIST 33%)
Mucositis/stomatitis (GIST 29%; MRCC 53%)
Dyspnea (MRCC 28%; GIST 10%)
HTN (MRCC 28%; GIST 15%)
Arthralgia (MRCC 28%; GIST 12%)
Bleeding (MRCC 26%; GIST 18%)
Headache (MRCC 25%; GIST 13%)
Asthenia (GIST 22%)
Lymphopenia (MRCC 21%)
Fever (GIST 18%; MRCC 15%),
Limb pain (MRCC 18%)
Back pain (MRCC 17%; GIST 11%)
Myalgia (MRCC 17%; GIST 14%)
Cough (MRCC 17%; GIST 8%)
Dry skin (17%)
Hair color changes (17%)
Neutropenia (MRCC 13%; GIST 11%)
Alopecia (MRCC 12%)
Hand-foot syndrome (MRCC 12%; GIST 14%)
Dehydration (MRCC 11%)
1-10%
Venous thrombotic events
Hemorrhoids
Pancreatitis
Flu-like syndrome
<1%
Hepatotoxicity
Acute renal failure
Adrenal dysfunction
Postmarketing Reports
Blood and lymphatic system disorders: Thrombotic microangiopathy; hemorrhage associated with thrombocytopenia (hold dose, following resolution, treatment may be resumed at the discretion of the treating physician)
Immune system disorders: Hypersensitivity reactions, including angioedema Infections and infestations: Serious infection (with or without neutropenia); necrotizing fasciitis, including of the perineum; most commonly observed infections include respiratory, urinary tract, skin infections, and sepsis
Metabolism and nutrition disorders: Tumor lysis syndrome
Musculoskeletal and connective tissue disorders: Fistula formation, sometimes associated with tumor necrosis and/or regression; osteonecrosis of the jaw, and myopathy and/or rhabdomyolysis with or without acute renal failure
Renal and urinary disorders: Renal impairment and/or failure; proteinuria; rare cases of nephrotic syndrome (discontinue treatment)
Respiratory disorders: Pulmonary embolism; pulmonary hemorrhage, pleural effusion
Skin and subcutaneous tissue disorders: Pyoderma gangrenosum, including positive dechallenges
Vascular disorders: Arterial thromboembolic events, most frequent events included CVA, TIA, cerebral infarction, arterial (including aortic) aneurysms, dissections, and rupture
Reversible posterior leukoencephalopathy syndrome
Impaired wound healing
Warnings
Black Box Warnings
Hepatotoxicity
- Hepatotoxicity may be severe, and in some cases fatal
- Monitor liver function tests (ALT, AST, bilirubin) before treatment initiation, during each treatment cycle, and as clinically indicated
- Interrupted for Grade 3 or 4 drug-related hepatic related adverse events and discontinued if there is no resolution
- Do not restart if subsequently experience severe changes in liver function tests or other signs and symptoms of liver failure emerge
- Safety in patients with ALT or AST >2.5x ULN or, if due to liver metastases, >5x ULN has not been established
Contraindications
None
Cautions
Fatal liver failure has been observed (see Black Box Warnings)
Hemorrhagic events including tumor-related hemorrhage reported; perform serial complete blood counts and physical examinations
Adrenal hemorrhage observed in animal studies; monitor adrenal function in case of stress such as surgery, trauma or severe infection
Monitor urine protein; interrupt treatment for 24-hr urine protein ≥3 g; discontinue for repeat episodes of protein ≥3 g despite dose reductions or nephrotic syndrome
Hyperthyroidism, some followed by hypothyroidism, have been reported; monitor thyroid function at baseline, periodically during treatment and as clinically indicated; initiate and/or adjust therapies for thyroid dysfunction as appropriate
Impaired wound healing reported; withhold therapy for at least 3 weeks prior to elective surgery; do not administer for at least 2 weeks following major surgery and until adequate wound healing; safety of resumption of therapy after resolution of wound healing complications has not been established
Severe cutaneous reactions have been reported, including cases of erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis, some of which were fatal; necrotizing fasciitis, including fatal cases, also reported
Advise women of childbearing potential of potential hazard to fetus
Prolonged QT intervals and Torsade de Pointes may occur in a dose-dependent manner; use caution in patients at higher risk for developing QT interval prolongation; consider monitoring with on-treatment ECG and electrolytes
Cases of tumor lysis syndrome (TLS) reported in patients with RCC and GIST with high tumor burden; monitor closely and treat as necessary
Thrombotic microangiopathy, including thrombotic thrombocytopenic purpura and hemolytic uremic syndrome, sometimes leading to renal failure or fatal outcome reported in clinical trials and postmarketing experience; not approved for use in combination with bevacizumab
Hypoglycemia may occur; monitor blood glucose levels regularly during and after discontinuation treatment; assess if antidiabetic drugs dosage modifications are necessary
Monitor for hypertension and treat as needed with standard antihypertensive therapy; in cases of severe hypertension, temporary suspend treatment until hypertension is controlled
Osteonecrosis
- Osteonecrosis of the jaw reported; concomitant exposure to other risk factors, such as bisphosphonates or dental disease/invasive dental procedures, may increase risk of ONJ
- Perform oral examination prior to initiation of therapy and periodically during therapy; advise patients regarding good oral hygiene practices
- Withhold treatment for at least 3 weeks prior to scheduled dental surgery or invasive dental procedures, if possible; withhold treatment for development of ONJ until complete resolution
Reversible posterior leukoencephalopathy syndrome (RPLS)
- RPLS some of which were fatal reported
- Patients can present with hypertension, headache, decreased alertness, altered mental functioning, and visual loss, including cortical blindness
- Magnetic resonance imaging is necessary to confirm diagnosis; withhold therapy until resolution;
- Safety of reinitiating therapy in patients with RPLS unknown
Cardiovascular risks
- Cardiovascular events (eg, heart failure, cardiomyopathy, myocardial ischemia, and myocardial infarction), some of which were fatal, have been reported
- Increased risk for heart failure and high grade heart failure; discontinue treatment if patient presents with signs or symptoms of congestive heart failure (CHF); interrupt and/or reduce dose in patients without clinical evidence of CHF who either have an ejection fraction (EF) of >20% but <50% below baseline or below the lower limit of normal if baseline EF is not obtained
- Cardiac dysfunction occurs 28 to 180 days after sunitinib initiation and most commonly after the third cycle
- Heart failure risk is associated with preexisting hypertension and coronary artery disease
- Monitor for signs and symptoms of congestive heart failure
Drug interaction overview
-
Coadministration with strong CYP3A4 inhibitors
- Use an alternative with no or minimal CYP3A4 activity
- Strong CYP3A4 inhibitors may increase sunitinib concentrations
-
Coadministration with strong CYP3A4 inducers
- Use an alternative with no or minimal CYP3A4 activity
- Coadministration with CYP3A4 inducers may decrease sunitinib concentrations
-
Coadministration with QT-prolonging drugs
- Treatment is associated with QTc interval prolongation; monitor QT interval with ECGs more frequently in patients who require treatment with concomitant medications known to prolong the QT interval
Pregnancy & Lactation
Pregnancy
Based on animal reproduction studies and its mechanism of action, fetal harm may occur when administered to pregnant females
No data available in pregnant women to inform a drug-associated risk
Verify pregnancy status of females of reproductive potential before initiating treatment
Animal data
- Oral administration of sunitinib to pregnant rats and rabbits throughout organogenesis resulted in teratogenicity (embryolethality, craniofacial and skeletal malformations) at 5.5 and 0.3 times the combined AUC (the combined systemic exposure of sunitinib plus its active metabolite) in patients administered the recommended daily doses of 50 mg, respectively
- Advise females of reproductive potential of the potential risk to a fetus
Contraception
- Females of reproductive potential: Use effective contraceptive during treatment and for at least 4 weeks after final dose
- Males with female partners of reproductive potential: Use effective contraceptive during treatment and for 7 weeks after final dose
Infertility
- Based on findings in animals, male and female fertility may be impaired
Lactation
There is no information regarding the presence of sunitinib and its metabolites in human milk
Sunitinib and its metabolites were excreted in rat milk at concentrations up to 12-fold higher than in plasma
Advise females not to breastfeed during treatment and for at least 4 weeks after final dose
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
Multikinase inhibitor (including VEGF and PDGF receptor tyrosine kinases) some of which are implicated in tumor growth, angiogenesis, and metastasis
Absorption
Steady-state concentrations of sunitinib and its primary active metabolite are achieved within 10-14
Peak plasma time: 6-12 hr
Distribution
Vd: 2,230 L
Protein bound
- Sunitinib: 95%
- Active metabolite: 90%
Metabolism
Primarily metabolized by CYP3A4 to its primary active metabolite, which is further metabolized by CYP3A4
Elimination
Clearance: 34-62 L/hr
Half-life
- Single-oral dose: ~40-60 hr
- Active metabolite: 80-110 hr
Excretion
- Feces: ~ 61%
- Urine: ~16%
Administration
Oral administration
Take with or without food
Do not drink grapefruit juice or eat grapefruit during your treatment
Missed dose
- Missed dose <12 hr: Take the missed dose right away
- Missed dose >12 hr: Take next dose at regular time
- Do not make up missed dose
Storage
Tablets: Store at room temperature at 68-77°F (20-25°C)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Sutent oral - | 50 mg capsule |  | |
| Sutent oral - | 37.5 mg capsule |  | |
| Sutent oral - | 25 mg capsule |  | |
| Sutent oral - | 12.5 mg capsule |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
sunitinib oral
SUNITINIB - ORAL
(soo-NI-ti-nib)
COMMON BRAND NAME(S): Sutent
WARNING: Rarely, sunitinib has caused severe (sometimes fatal) liver problems. Get medical help right away if you develop symptoms of liver problems such as persistent nausea/vomiting, severe stomach/abdominal pain, dark urine, pale stools, or yellowing eyes/skin. Your doctor will monitor for liver problems with blood tests. Tell all of your doctors and pharmacists if you have ever stopped taking sunitinib because of liver problems (including high liver enzymes).
USES: This medication is used to treat certain types of cancer (kidney, pancreas, and intestinal). It is also used to treat people who are at high risk of the kidney cancer coming back again after having kidney surgery. Sunitinib works by stopping or slowing the growth of cancer tumors. It also works by slowing the growth of new blood vessels within the tumor.
HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking sunitinib and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth as directed by your doctor, with or without food, usually once daily.Drink plenty of fluids during treatment with this medication, unless otherwise directed by your doctor.The dosage is based on your medical condition and response to treatment. For some conditions, you may be directed to take this medication for a specific period of time followed by another period of time off of the drug. For other conditions, you may be directed to take sunitinib every day without a break. Follow your doctor's instructions.Do not increase your dose or take this medication more often without your doctor's approval. Your condition will not improve any faster, and the risk of serious side effects may be increased.Use this medication regularly in order to get the most benefit from it. To help you remember, take it at the same time each day.Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor instructs you otherwise. Grapefruit can increase the amount of certain medications in your bloodstream. Consult your doctor or pharmacist for more details.
SIDE EFFECTS: See also Warning section.Upset stomach, nausea, vomiting, diarrhea, change in taste, decreased appetite, dry/cracked/thickened skin, watering eyes, swelling around eyes, numbness/tingling of arms/legs, or tiredness may occur. In some cases, drug therapy may be necessary to prevent or relieve nausea/vomiting/diarrhea. Eating several small meals or limiting activity may help lessen some of these effects. If these effects persist or worsen, notify your doctor or pharmacist promptly.This medication may cause patchy or complete hair loss and changes in hair/skin color. These effects are not harmful. However, talk to your doctor for more details since changes in skin color may also be a sign of a more serious condition.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: headache, rash/blisters on palms of hands/soles of feet, sores/pain on the tongue/mouth, easy bruising/bleeding, cold/heat intolerance, pain/redness/swelling of arms or legs, black/bloody stools, vomit that looks like coffee grounds, coughing up blood, slow wound healing, jaw pain, toe/joint pain, signs of low blood sugar (such as hunger, shakiness, fast heartbeat, sweating), symptoms of heart failure (such as shortness of breath, swelling ankles/feet, unusual tiredness, unusual/sudden weight gain), mental/mood changes (such as decreased alertness, irritability, nervousness), vision changes (such as decreased vision).This medication may raise your blood pressure. Check your blood pressure regularly and tell your doctor if the results are high. Your doctor may control your blood pressure with medication.Sunitinib sometimes causes side effects due to the rapid destruction of cancer cells (tumor lysis syndrome). To lower your risk, your doctor may add a medication and tell you to drink plenty of fluids. Tell your doctor right away if you have symptoms such as: signs of kidney problems (such as painful urination, cloudy/pink/bloody urine, change in the amount of urine), muscle spasms/weakness.Get medical help right away if you have any very serious side effects, including: trouble breathing, chest/jaw/left arm pain, sudden/severe back pain, weakness on one side of the body, trouble speaking, severe dizziness, fainting, fast/slow/irregular heartbeat, seizures.Sunitinib has rarely caused very serious (possibly fatal) skin reactions. Get medical help right away if you develop symptoms of serious skin reactions, including: rash, hot/peeling/blistering/painful skin, red/purple skin.This medication can lower the body's ability to fight an infection. Notify your doctor promptly if you develop any signs of an infection such as fever, chills or persistent sore throat.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.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 sunitinib, 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: bleeding problems, heart problems (such as heart attack), high blood pressure, liver problems, kidney disease, thyroid disease, diabetes, blood vessel problems (such as an aneurysm or a tear/break in the aorta or other blood vessels).Sunitinib 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 sunitinib, 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 sunitinib safely.Do not have immunizations/vaccinations without the consent of your doctor, and avoid contact with people who have recently received oral polio vaccine or flu vaccine inhaled through the nose.To lower the chance of getting cut, bruised or injured, use caution with sharp objects like safety razors or nail cutters and avoid activities such as contact sports.Wash your hands well to prevent the spread of infections.Some people taking sunitinib may have serious jawbone problems. Your doctor should check your mouth before you start this medication. Tell your dentist that you are taking this medication before you have any dental work done. To help prevent jawbone problems, have regular dental exams and learn how to keep your teeth and gums healthy. If you have jaw pain, tell your doctor and dentist right away.Before having surgery (including dental procedures), tell your doctor or dentist about this medication and all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medication may cause wounds to heal slowly or poorly. Your doctor or dentist may tell you to temporarily stop treatment with this medication at least 3 weeks before surgery or a dental procedure. Ask your doctor or dentist for specific instructions about when to stop and when to restart treatment with this medication. Tell your doctor/dentist right away if you have wounds that are not healing well.Older adults may be more sensitive to the side effects of this drug, especially QT prolongation (see above).Tell your doctor if you are pregnant or plan to become pregnant. Female patients should have a pregnancy test before starting this medication. You should not become pregnant while using sunitinib. Sunitinib may harm an unborn baby. Female patients should ask about reliable forms of birth control while using this medication and for 4 weeks after stopping treatment. Male patients with female partners should ask about reliable forms of birth control while using this medication and for 7 weeks after stopping treatment. If you or your partner become pregnant, talk to your doctor right away about the risks and benefits of this medication.It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding is not recommended while using this drug and for 4 weeks after the last dose. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: 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: bevacizumab, "blood thinners" (anticoagulants such as warfarin, heparins).Many drugs besides sunitinib may affect the heart rhythm (QT prolongation), including amiodarone, dofetilide, pimozide, procainamide, quinidine, sotalol, macrolide antibiotics (such as erythromycin), among others. Therefore, before using sunitinib, report all medications you are currently using to your doctor or pharmacist.Other medications can affect the removal of sunitinib from your body, which may affect how sunitinib works. Examples include azole antifungals (such as ketoconazole, itraconazole), cimetidine, HIV protease inhibitors (such as ritonavir, saquinavir), macrolide antibiotics (such as erythromycin), rifamycins (such as rifampin, rifabutin), St. John's wort, certain drugs used to treat seizures (such as phenytoin, phenobarbital), 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.Laboratory and/or medical tests (such as blood pressure, complete blood count, heart/liver/kidney/thyroid function tests, blood sugar, uric acid level, pancreatic enzymes, urine protein levels, blood mineral levels such as sodium, potassium, phosphate) should be performed to monitor your progress or check for side effects. 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.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised August 2020. 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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