Dosing & Uses
Dosage Forms & Strengths
tablet
- 225mg
Non–Small Cell Lung Cancer
Indicated for metastatic non–small cell lung cancer (NSCLC) in adults harboring mesenchymal-epithelial transition (MET) exon 14 (ex14) skipping alterations
450 mg PO qDay
Continue until disease progression or unacceptable toxicity
Dosage Modifications
Recommended dose reduction to manage adverse reactions: 225 mg PO qDay
Permanently discontinue if unable to tolerate 225 mg PO qDay
Interstitial lung disease (ILD)/ pneumonitis
- Suspected ILD (any grade): Withhold
- Confirmed ILD: Permanently discontinue
Increased AST/ALT and/or total bilirubin
-
Grade 3 increased AST/ALT without increased total bilirubin
- Withhold until recovery to baseline ALT/AST
- If recovered to baseline ≤7 days, resume at same dose; otherwise, resume at a reduced dose
-
Grade 3 increased total bilirubin without concurrent increased AST/ALT
- Withhold until recovery to baseline total bilirubin
- If recovered to baseline ≤7 days, resume at reduced dose; otherwise, permanently discontinue
-
Permanently discontinue
- Grade 4 increased ALT/AST without increased total bilirubin
- ALT/AST >3x ULN with total bilirubin >2x ULN without cholestasis or hemolysis
- Grade 4 increased total bilirubin without concurrent increased AST/ALT
Other adverse reactions
- Grade 2: Maintain dose; if intolerable, consider withholding until resolved, then resume at reduced dose
- Grade 3: Withhold until resolved, then resume at reduced dose
- Grade 4: Permanently discontinue
Renal impairment
- Mild-to-moderate (CrCl 30-89 mL/min): No dosage adjustment necessary
- Severe (CrCl <30 mL/min): Recommended dose not established
Hepatic impairment
- Mild-to-moderate (Child-Pugh Class A or B): No dosage adjustment necessary
- Severe (Child-Pugh Class C): Pharmacokinetics and safety not studied
Dosing Considerations
Verify pregnancy status in females of reproductive potential before initiating
Patient selection
- Select patients for treatment based on presence of METex14 skipping alterations in tumor biopsy specimen or plasma (if tumor biopsy cannot be obtained)
- If alterations are undetected in plasma, re-evaluate the feasibility of tumor biopsy
- An FDA-approved test for detection of METex14 skipping alteration is not available
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (152)
- afatinib
tepotinib will increase the level or effect of afatinib 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.
- aliskiren
tepotinib will increase the level or effect of aliskiren 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.
- ambrisentan
tepotinib will increase the level or effect of ambrisentan 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.
- amiodarone
tepotinib will increase the level or effect of amiodarone 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.
- amobarbital
amobarbital will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- apalutamide
apalutamide will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- apixaban
tepotinib will increase the level or effect of apixaban 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.
- artesunate
tepotinib will increase the level or effect of artesunate 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.
- atazanavir
tepotinib will increase the level or effect of atazanavir 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.
- atorvastatin
tepotinib will increase the level or effect of atorvastatin 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.
- avatrombopag
tepotinib will increase the level or effect of avatrombopag 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.
- bendamustine
tepotinib will increase the level or effect of bendamustine 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.
- berotralstat
tepotinib will increase the level or effect of berotralstat 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.
- betrixaban
tepotinib will increase the level or effect of betrixaban 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.
- bosentan
bosentan will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- brentuximab vedotin
tepotinib will increase the level or effect of brentuximab vedotin 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.
- budesonide
tepotinib will increase the level or effect of budesonide 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.
- butabarbital
butabarbital will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- butalbital
butalbital will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- carbamazepine
carbamazepine will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- carfilzomib
tepotinib will increase the level or effect of carfilzomib 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.
- carvedilol
tepotinib will increase the level or effect of carvedilol 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.
- ceritinib
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.
- cetirizine
tepotinib will increase the level or effect of cetirizine 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.
- cimetidine
tepotinib will increase the level or effect of cimetidine 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.
- ciprofloxacin
tepotinib will increase the level or effect of ciprofloxacin 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.
- clarithromycin
clarithromycin will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
- colchicine
tepotinib will increase the level or effect of colchicine 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.
- crizotinib
tepotinib will increase the level or effect of crizotinib 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.
- cyclosporine
tepotinib will increase the level or effect of cyclosporine 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.
- dabigatran
tepotinib will increase the level or effect of dabigatran 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.
- dabrafenib
dabrafenib will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
tepotinib will increase the level or effect of dabrafenib 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. - darolutamide
tepotinib will increase the level or effect of darolutamide 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.
- darunavir
darunavir will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
- dasabuvir
tepotinib will increase the level or effect of dasabuvir 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.
- daunorubicin
tepotinib will increase the level or effect of daunorubicin 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.
- daunorubicin liposomal
tepotinib will increase the level or effect of daunorubicin liposomal 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.
- desloratadine
tepotinib will increase the level or effect of desloratadine 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.
- dexamethasone
tepotinib will increase the level or effect of dexamethasone 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.
- digoxin
tepotinib will increase the level or effect of digoxin 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.
- diltiazem
tepotinib will increase the level or effect of diltiazem 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.
- docetaxel
tepotinib will increase the level or effect of docetaxel 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.
- doxorubicin
tepotinib will increase the level or effect of doxorubicin 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.
- duvelisib
tepotinib will increase the level or effect of duvelisib 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.
- edoxaban
tepotinib will increase the level or effect of edoxaban 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.
- efavirenz
efavirenz will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- eletriptan
tepotinib will increase the level or effect of eletriptan 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.
- enzalutamide
enzalutamide will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- erythromycin base
tepotinib will increase the level or effect of erythromycin base 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.
- erythromycin ethylsuccinate
tepotinib will increase the level or effect of erythromycin ethylsuccinate 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.
- erythromycin lactobionate
tepotinib will increase the level or effect of erythromycin lactobionate 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.
- erythromycin stearate
tepotinib will increase the level or effect of erythromycin stearate 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.
- etoposide
tepotinib will increase the level or effect of etoposide 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.
- etravirine
etravirine will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- everolimus
tepotinib will increase the level or effect of everolimus 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.
- fexofenadine
tepotinib will increase the level or effect of fexofenadine 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.
- fosphenytoin
fosphenytoin will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- glecaprevir/pibrentasvir
tepotinib will increase the level or effect of glecaprevir/pibrentasvir 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.
- grapefruit
grapefruit will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
- hydrocortisone
tepotinib will increase the level or effect of hydrocortisone 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.
- idarubicin
tepotinib will increase the level or effect of idarubicin 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.
- imatinib
tepotinib will increase the level or effect of imatinib 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.
- indinavir
tepotinib will increase the level or effect of indinavir 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.
- irinotecan
tepotinib will increase the level or effect of irinotecan 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.
- irinotecan liposomal
tepotinib will increase the level or effect of irinotecan liposomal 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.
- itraconazole
itraconazole will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
- ivermectin
tepotinib will increase the level or effect of ivermectin 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.
- ivosidenib
ivosidenib will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ketoconazole
ketoconazole will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
- lapatinib
tepotinib will increase the level or effect of lapatinib 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.
- larotrectinib
tepotinib will increase the level or effect of larotrectinib 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.
- ledipasvir/sofosbuvir
tepotinib will increase the level or effect of ledipasvir/sofosbuvir 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.
- lefamulin
tepotinib will increase the level or effect of lefamulin 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.
- lenvatinib
tepotinib will increase the level or effect of lenvatinib 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.
- letermovir
tepotinib will increase the level or effect of letermovir 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.
- linagliptin
tepotinib will increase the level or effect of linagliptin 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.
- lonafarnib
lonafarnib will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
- loperamide
tepotinib will increase the level or effect of loperamide 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.
- lopinavir
lopinavir will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
- loratadine
tepotinib will increase the level or effect of loratadine 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.
- lovastatin
tepotinib will increase the level or effect of lovastatin 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.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- maraviroc
tepotinib will increase the level or effect of maraviroc 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.
- methotrexate
tepotinib will increase the level or effect of methotrexate 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.
- mitomycin
tepotinib will increase the level or effect of mitomycin 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.
- mitotane
mitotane will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- morphine
tepotinib will increase the level or effect of morphine 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.
- nadolol
tepotinib will increase the level or effect of nadolol 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.
- nafcillin
nafcillin will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- naldemedine
tepotinib will increase the level or effect of naldemedine 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.
- nefazodone
nefazodone will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
- nelfinavir
nelfinavir will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
tepotinib will increase the level or effect of nelfinavir 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. - nicardipine
tepotinib will increase the level or effect of nicardipine 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.
- nilotinib
tepotinib will increase the level or effect of nilotinib 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.
- ombitasvir/paritaprevir/ritonavir
tepotinib will increase the level or effect of ombitasvir/paritaprevir/ritonavir 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.
- ombitasvir/paritaprevir/ritonavir & dasabuvir
tepotinib will increase the level or effect of ombitasvir/paritaprevir/ritonavir & dasabuvir 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.
- ondansetron
tepotinib will increase the level or effect of ondansetron 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.
- osimertinib
tepotinib will increase the level or effect of osimertinib 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.
- paclitaxel
tepotinib will increase the level or effect of paclitaxel 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.
- paclitaxel protein bound
tepotinib will increase the level or effect of paclitaxel protein bound 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.
- paliperidone
tepotinib will increase the level or effect of paliperidone 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.
- pazopanib
tepotinib will increase the level or effect of pazopanib 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.
- pentobarbital
pentobarbital will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- phenobarbital
phenobarbital will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- phenytoin
phenytoin will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- pomalidomide
tepotinib will increase the level or effect of pomalidomide 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.
- posaconazole
posaconazole will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
tepotinib will increase the level or effect of posaconazole 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. - pralsetinib
tepotinib will increase the level or effect of pralsetinib 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.
- pravastatin
tepotinib will increase the level or effect of pravastatin 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.
- prednisone
tepotinib will increase the level or effect of prednisone 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.
- primidone
primidone will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- quinidine
tepotinib will increase the level or effect of quinidine 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.
- quinine
tepotinib will increase the level or effect of quinine 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.
- ranolazine
tepotinib will increase the level or effect of ranolazine 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.
- rifabutin
rifabutin will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifampin
rifampin will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
tepotinib will increase the level or effect of rifampin 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. - rifapentine
rifapentine will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifaximin
tepotinib will increase the level or effect of rifaximin 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.
- rimegepant
tepotinib will increase the level or effect of rimegepant 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.
- riociguat
tepotinib will increase the level or effect of riociguat 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.
- risperidone
tepotinib will increase the level or effect of risperidone 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.
- ritonavir
ritonavir will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
tepotinib will increase the level or effect of ritonavir 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. - saquinavir
saquinavir will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
tepotinib will increase the level or effect of saquinavir 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. - saxagliptin
tepotinib will increase the level or effect of saxagliptin 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.
- secobarbital
secobarbital will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- silodosin
tepotinib will increase the level or effect of silodosin 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.
- sirolimus
tepotinib will increase the level or effect of sirolimus 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.
- sitagliptin
tepotinib will increase the level or effect of sitagliptin 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.
- sofosbuvir
tepotinib will increase the level or effect of sofosbuvir 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.
- sofosbuvir/velpatasvir
tepotinib will increase the level or effect of sofosbuvir/velpatasvir 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.
- St John's Wort
St John's Wort will decrease the level or effect of tepotinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- stiripentol
stiripentol, tepotinib. Other (see comment). Avoid or Use Alternate Drug. Comment: Interaction not studied clinically. Metabolism and in vitro data suggest avoiding drugs that strongly inhibit both CYP3A and P-gp with tepotinib (a P-gp and CYP3A substrate). Stiripentol (a strong CYP3A4 and P-gp inhibitor; strong CYP3A4 inducer) may increase or decrease tepotinib effects.
- talazoparib
tepotinib will increase the level or effect of talazoparib 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.
- tazemetostat
tepotinib will increase the level or effect of tazemetostat 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.
- temsirolimus
tepotinib will increase the level or effect of temsirolimus 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.
- teniposide
tepotinib will increase the level or effect of teniposide 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.
- tenofovir AF
tepotinib will increase the level or effect of tenofovir AF 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.
- tenofovir DF
tepotinib will increase the level or effect of tenofovir DF 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.
- testosterone
tepotinib will increase the level or effect of testosterone 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.
- tipranavir
tipranavir will increase the level or effect of tepotinib by Other (see comment). Avoid or Use Alternate Drug. Interaction not studied clinically. Metabolism and data suggest drugs that are strong CYP3A4 and P-gp inhibitors may increase tepotinib (a P-gp and CYP3A4 substrate) effects and risk of toxicities.
- tolvaptan
tepotinib will increase the level or effect of tolvaptan 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.
- topotecan
tepotinib will increase the level or effect of topotecan 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.
- trabectedin
tepotinib will increase the level or effect of trabectedin 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.
- ubrogepant
tepotinib will increase the level or effect of ubrogepant 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.
- velpatasvir
tepotinib will increase the level or effect of velpatasvir 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.
- vemurafenib
tepotinib will increase the level or effect of vemurafenib 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.
- venetoclax
tepotinib will increase the level or effect of venetoclax 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.
- verapamil
tepotinib will increase the level or effect of verapamil by affecting hepatic enzyme CYP2E1 metabolism. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
tepotinib will increase the level or effect of verapamil 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. - vinblastine
tepotinib will increase the level or effect of vinblastine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
tepotinib will increase the level or effect of vinblastine 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. - vincristine
tepotinib will increase the level or effect of vincristine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
tepotinib will increase the level or effect of vincristine 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. - vincristine liposomal
tepotinib will increase the level or effect of vincristine liposomal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
tepotinib will increase the level or effect of vincristine liposomal 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. - voxilaprevir
tepotinib will increase the level or effect of voxilaprevir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
tepotinib will increase the level or effect of voxilaprevir 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.
Monitor Closely (0)
Minor (0)
Adverse Effects
>10%
All grades
- Decreased albumin (76%)
- Edema (70%)
- Increased creatinine (55%)
- Increased alkaline phosphatase (50%)
- Decreased lymphocytes (48%)
- Increased ALT (44%)
- Increased AST (35%)
- Decreased sodium (31%)
- Fatigue (27%)
- Nausea (27%)
- Decreased hemoglobin (27%)
- Diarrhea (26%)
- Increased potassium (25%)
- Increased gamma-glutamyltransferase (24%)
- Musculoskeletal pain (24%)
- Increased amylase (23%)
- Decreased leukocytes (23%)
- Dyspnea (20%)
- Decreased appetite (16%)
- Cough (15%)
- Abdominal pain (16%)
- Constipation (16%)
- Vomiting (13%)
- Pleural effusion (13%)
- Pneumonia (11%)
Grade 3 to 4
- Decreased lymphocytes (11%)
1-10%
All grades
- ILD/pneumonitis (<10%)
- Rash (<10%)
- Fever (<10%)
- Dizziness (<10%)
- Pruritus (<10%)
- Headache (<10%)
Grade 3 to 4
- Decreased albumin (9%)
- Decreased sodium (8%)
- Pleural effusion (5%)
- Increased gamma-glutamyltransferase (5%)
- Increased amylase (4.6%)
- Increased ALT (4.1%)
- Pneumonia (3.9%)
- Increased AST (2.5%)
- Musculoskeletal pain (2.4%)
- Decreased hemoglobin (2%)
- Dyspnea (2%)
- Increased alkaline phosphatase (1.6%)
- Increased potassium (1.6%)
- Vomiting (1.2%)
- Decreased appetite (1.2%)
<1%
Grade 3 to 4
- Nausea (0.8%)
- Abdominal pain (0.8%)
- Decreased leukocytes (0.8%)
- Increased creatinine (0.4%)
- Diarrhea (0.4%)
- Cough (0.4%)
Warnings
Contraindications
None
Cautions
ILD/pneumonitis, which can be fatal, occurred; monitor for new or worsening pulmonary symptoms indicative of ILD/pneumonitis (eg, dyspnea, cough, fever)
Fetal harm may occur when administered to pregnant females
Hepatoxicity
- Hepatoxicity reported
- Median time to onset of Grade ≥3 was 30 days
- Monitor liver function tests (eg, AST, ALT, total bilirubin) before initiation, q2weeks during the first 3 months, then monthly or as clinically indicated
- More frequent testing if increased AST/ALT or bilirubin develops
Drug interaction overview
Inhibits P-gp; substrate of CYP3A4, CYP2C8, and P-gp
Effects of strong CYP3A4 or P-gp inhibitors and CYP3A4 inducers on tepotinib have not been studied clinically
-
Dual strong CYP3A4 and P-gp inhibitors
- Avoid coadministration
- Data suggest drugs that strongly inhibit both CYP3A4 and P-gp may increase tepotinib exposure and risk of toxicities
-
Strong CYP3A4 inducers
- Avoid coadministration
- Data suggest drugs that are strong CYP3A4 inducers may decrease exposure and efficacy of tepotinib
-
Certain P-gp substrates
- Avoid coadministration with P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicities
- Tepotinib may increases concentration levels and risk of toxicities of P-gp substrates
Pregnancy & Lactation
Pregnancy
Based on animal studies and mechanism of action, fetal harm may occur when administered to pregnant females
Data are unavailable on use in pregnant females
Verify pregnancy status in females of reproductive potential before initiation
Animal data
- Oral administration to pregnant rabbits during organogenesis resulted in malformation (teratogenicity) and anomalies at maternal exposures less than human exposure based on AUC at 450 mg daily
- Advise pregnant females of potential risk to fetus
Contraception
- Females of reproductive potential: Use effective contraception during treatment and for 1 week after final dose
- Male partners with female partners of reproductive potential: Use effective contraception during treatment and for 1 week after final dose
Lactation
There are no data regarding tepotinib or its metabolites in human milk, its effects on breastfed infants, or milk production
Advise females not to breastfeed during treatment and for 1 week 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
MET tyrosine kinase inhibitor
Selectively binds to MET tyrosine kinase and disrupts MET and hepatocyte growth factor (HGF)–dependent signal transduction pathways, which may induce apoptosis in tumor cells overexpressing this kinase
Absorption
Peak plasma concentration (steady-state): 1,291 ng/mL
Peak plasma time: 8 hr
AUC: 27,438 ng⋅hr/mL
Absolute bioavailability: 71.6%
Effect of food
- Mean AUC increased by 1.6-fold and peak plasma concentration increased by 2-fold following a high-fat, high-calories meal (~800-1,000 calories, 150 calories [protein], 250 calories [carbohydrates], and 500-600 calories [fat])
- Median peak plasma time shifted from 12 hr to 8 hr
Distribution
Vd: 1,038 L
Protein bound: 98%
Metabolism
Primarily metabolized by CYP3A4 and CYP2C8
Major metabolite: M506
Elimination
Clearance: 23.8 L/hr
Half-life: 32 hr
Excretion
- Tepotinib: Feces (45% unchanged); urine (13.6% [7% unchanged])
- M506 (metabolite): 40.4% in plasma
Administration
Oral Administration
Take at same time every day with food
Swallow tablets whole; do not chew, crush, or split
Missed dose
- ≥8 hr from next scheduled dose: Take as soon as possible
- <8 hr from next scheduled dose: Skip dose and take next dose at regular scheduled time
- Vomited dose: Skip dose and take next dose at regular scheduled time
Storage
Store at 20-25ºC (68-77ºF); excursion permitted to 15-30ºC (59-86ºF)
Store in original package
Images
Formulary
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Adding plans allows you to:
- View the formulary and any restrictions for each plan.
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