tepotinib (Rx)

Brand and Other Names:Tepmetko

Dosing & Uses

AdultPediatric

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

Next:

Interactions

Interaction Checker

and tepotinib

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (120)

              • 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.

              • 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.

              • 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.

              • 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.

              • 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

                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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • 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.

              • nelfinavir

                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 (DSC)

                tepotinib will increase the level or effect of ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) 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.

              • 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

                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.

              • 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.

              • rifampin

                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.

              • 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

                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

                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.

              • 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.

              • 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.

              • 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 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 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 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 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 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)

                  Previous
                  Next:

                  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%)

                  Postmarketing Reports

                  Increased lipase

                  Previous
                  Next:

                  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
                  • 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
                  Previous
                  Next:

                  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.

                  Previous
                  Next:

                  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
                  Previous
                  Next:

                  Administration

                  Oral Administration

                  Take at same time every day with food

                  Swallow tablets whole; do not chew, crush, or split

                  Administration to patients with difficulty swallowing solids

                  • Place tablet(s) in a glass containing 30 mL (1 ounce) of non-carbonated water
                  • No other liquids should be used or added; stir, without crushing, until tablet(s) dispersed into small pieces(tablets will not completely dissolve) and drink immediately or within 1 hour
                  • Swallow the tablet dispersion; do not chew pieces of the tablet; rinse the glass with an additional 30 mL and drink immediately ensuring no residue remains in glass and full dose is administered

                  Administration via a nasogastric tube (with at least 8 French gauge)

                  • Disperse tablet(s) in 30 mL of non-carbonated water as described above
                  • Administer 30 mL of liquid immediately or within 1 hour as per nasogastric tube manufacturer’s instructions
                  • Immediately rinse twice with 30 mL each time to ensure that no residue remains in glass or syringe and full dose is administered

                  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 regularly scheduled time

                  Storage

                  Store at 20-25ºC (68-77ºF); excursion permitted to 15-30ºC (59-86ºF)

                  Store in original package

                  Previous
                  Next:

                  Images

                  No images available for this drug.
                  Previous
                  Next:

                  Patient Handout

                  A Patient Handout is not currently available for this monograph.
                  Previous
                  Next:

                  Formulary

                  FormularyPatient Discounts

                  Adding plans allows you to compare formulary status to other drugs in the same class.

                  To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                  Adding plans allows you to:

                  • View the formulary and any restrictions for each plan.
                  • Manage and view all your plans together – even plans in different states.
                  • Compare formulary status to other drugs in the same class.
                  • Access your plan list on any device – mobile or desktop.

                  The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                  Tier Description
                  1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                  2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                  3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                  4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  NC NOT COVERED – Drugs that are not covered by the plan.
                  Code Definition
                  PA Prior Authorization
                  Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                  QL Quantity Limits
                  Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                  ST Step Therapy
                  Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                  OR Other Restrictions
                  Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
                  Additional Offers
                  Email to Patient

                  From:

                  To:

                  The recipient will receive more details and instructions to access this offer.

                  By clicking send, you acknowledge that you have permission to email the recipient with this information.

                  Email Forms to Patient

                  From:

                  To:

                  The recipient will receive more details and instructions to access this offer.

                  By clicking send, you acknowledge that you have permission to email the recipient with this information.

                  Previous
                  Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.