capmatinib (Rx)

Brand and Other Names:Tabrecta
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 150mg
  • 200mg

Non-Small Cell Lung Cancer

Indicated for metastatic non-small cell lung cancer (NSCLC) in adults whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping

400 mg PO BID

Continue until disease progression or unacceptable toxicity

Dosage Modifications

Dose reductions for adverse reactions

  • First occurrence: Restart at 300 mg PO BID
  • Second occurrence: Restart at 200 mg PO BID
  • Unable to tolerate 200 mg PO BID: Permanently discontinue

Interstitial lung disease (ILD)/pneumonitis

  • Any grade: Permanently discontinue

Liver function test abnormalities

  • ALT and/or AST >3x ULN with total bilirubin >2x ULN: Permanently discontinue
  • Increased ALT and/or AST without increased total bilirubin
    • Grade 3: Withhold until recovery to baseline ALT/AST; if recovered to baseline within 7 days, then resume at the same dose; otherwise, resume at reduced dose
    • Grade 4: Permanently discontinue
  • Increased total bilirubin without concurrent increased ALT and/or AST
    • Grade 2: Withhold until recovery to baseline ALT/AST; if recovered to baseline within 7 days, then resume at the same dose; otherwise, resume at reduced dose
    • Grade 3: Withhold until recovery to baseline ALT/AST; if recovered to baseline within 7 days, then resume at reduced dose; otherwise, permanently discontinue
    • Grade 4: Permanently discontinue

Other adverse reactions

  • Grade 2: Maintain dose level; 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 15 to <30 mL/min): Not studied

Dosing Considerations

Patient selection

  • Select patients for treatment based on the presence of mutation that leads to MET exon 14 skipping in tumor specimens
  • Information on FDA-approved tests is available at: http://www.fda.gov/CompanionDiagnostics

Safety and efficacy not established

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Interactions

Interaction Checker

and capmatinib

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 (22)

              • abametapir

                abametapir will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • amobarbital

                amobarbital will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • apalutamide

                apalutamide will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • bosentan

                bosentan will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • carbamazepine

                carbamazepine will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • conivaptan

                conivaptan will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • dabrafenib

                dabrafenib will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • efavirenz

                efavirenz will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • enzalutamide

                enzalutamide will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • fosphenytoin

                fosphenytoin will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • lorlatinib

                lorlatinib will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • mifepristone

                mifepristone will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • mitotane

                mitotane will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • nafcillin

                nafcillin will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • phenobarbital

                phenobarbital will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • phenytoin

                phenytoin will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • primidone

                primidone will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • rifabutin

                rifabutin will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • rifampin

                rifampin will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • rifapentine

                rifapentine will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • ritonavir

                ritonavir will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • secobarbital

                secobarbital will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              Monitor Closely (20)

              • atazanavir

                atazanavir will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • berotralstat

                capmatinib increases levels of berotralstat by Other (see comment). Modify Therapy/Monitor Closely. Comment: Reduced dose of berotralstat (a BCRP substrate) to 110 mg/day when coadministered with BCRP inhibitors.

              • chloramphenicol

                chloramphenicol will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

              • clarithromycin

                clarithromycin will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • cobicistat

                cobicistat will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • darunavir

                darunavir will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • etravirine

                etravirine will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • idelalisib

                idelalisib will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • indinavir

                indinavir will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • itraconazole

                itraconazole will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ivosidenib

                ivosidenib will decrease the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ketoconazole

                ketoconazole will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • lopinavir

                lopinavir will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • nefazodone

                nefazodone will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • nelfinavir

                nelfinavir will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • posaconazole

                posaconazole will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ribociclib

                ribociclib will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • saquinavir

                saquinavir will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • tipranavir

                tipranavir will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • voriconazole

                voriconazole will increase the level or effect of capmatinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              Minor (0)

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                Adverse Effects

                >10%

                All grades

                • Decreased albumin (68%)
                • Increased creatinine (62%)
                • Peripheral edema (52%)
                • Nausea (44%)
                • Decreased lymphocytes (44%)
                • Increased ALT (37%)
                • Increased alkaline phosphatase (32%)
                • Fatigue (32%)
                • Increased amylase (31%)
                • Increased gamma-glutamyltransferase (GGT) (29%)
                • Vomiting (28%)
                • Increased lipase (26%)
                • Increased AST (25%)
                • Dyspnea (24%)
                • Decreased hemoglobin (24%)
                • Decreased sodium (23%)
                • Decreased phosphate (23%)
                • Increased potassium (23%)
                • Decreased leukocytes (23%)
                • Decreased glucose (21%)
                • Decreased appetite (21%)
                • Constipation (18%)
                • Diarrhea (18%)
                • Cough (16%)
                • Noncardiac chest pain (15%)
                • Back pain (14%)
                • Pyrexia (14%)

                Grade 3 to 4

                • Decreased lymphocytes (14%)

                1-10%

                All grades

                • Decreased weight (10%)
                • <10%
                  • Pruritus (allergic and generalized)
                  • ILD/pneumonitis
                  • Cellulitis
                  • Acute kidney injury (including renal failure)
                  • Urticaria
                  • Acute pancreatitis

                Grade 3 to 4

                • Peripheral edema (9%)
                • Fatigue (8%)
                • Increased ALT (8%)
                • Increased GGT (7%)
                • Increased lipase (7%)
                • Dyspnea (7%)
                • Decreased sodium (6%)
                • Increased AST (4.9%)
                • Increased amylase (4.4%)
                • Increased potassium (3.1%)
                • Decreased hemoglobin (2.8%)
                • Nausea (2.7%)
                • Vomiting (2.4%)
                • Noncardiac chest pain (2.1%)
                • Decreased albumin (1.8%)

                <1%

                Grade 3 to 4

                • Back pain (0.9%)
                • Constipation (0.9%)
                • Decreased appetite (0.9%)
                • Decreased leukocytes (0.9%)
                • Pyrexia (0.6%)
                • Decreased weight (0.6%)
                • Cough (0.6%)
                • Diarrhea (0.3%)
                • Decreased glucose (0.3%)
                • Increased alkaline phosphatase (0.3%)
                • Increased creatinine (0.3%)
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                Warnings

                Contraindications

                None

                Cautions

                ILD/pneumonitis, which can be fatal, occurred during clinical trials; monitor for new or worsening pulmonary symptoms indicative of ILD/pneumonitis

                Hepatotoxicity occurred; monitor liver function tests (including ALT, AST, and total bilirubin) before initiation, every 2 weeks during the first 3 months of treatment, and then once monthly or as clinically indicated, with more frequent testing in patients who develop increased transaminases or bilirubin

                May cause photosensitivity reactions; advise patients to limit direct ultraviolet exposure; limit direct ultraviolet exposure by using sunscreen or protective clothing during treatment

                Fetal harm may occur

                Drug interaction overview

                • Capmatinib is a CYP3A4 substrate and inhibits CYP1A2, P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), MATE 1, and MATE2K
                • Strong CYP3A Inhibitors
                  • Coadministration with a strong CYP3A inhibitor increased capmatinib exposure, which may increase the incidence and severity of adverse reactions of capmatinib
                  • Closely monitor for adverse reactions
                • Strong and moderate CYP3A inducers
                  • Avoid coadministration
                  • Concomitant use with capmatinib a strong or moderate CYP3A inducer decreased capmatinib exposure and efficacy
                • Substrates of CYP1A2, P-gp, BCRP, MATE1 or MATE2K
                  • Coadministration with CYP1A2, P-gp, BCRP, MATE1 or MATE2K substrates increased the exposure and adverse reactions of these substrates
                  • If coadministration unavoidable, reduce dose of CYP1A2, P-gp, BCRP, MATE1 or MATE2K substrate in accordance with the approved prescribing information
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                Pregnancy & Lactation

                Pregnancy

                Based on animal studies and its mechanism of action, fetal harm may occur when administered to pregnant females

                No available data on use in pregnant females

                Verify pregnancy status for females of reproductive potential before starting treatment

                Contraception

                • Females of reproductive potential: Use effective contraception during treatment and for 1 week after final dose
                • Males with female partners of reproductive potential: Use effective contraception during treatment and for 1 week after final dose

                Animal data

                • Oral administration to pregnant rats and rabbits during organogenesis resulted in malformations at maternal exposures less than the human exposure based on AUC at the 400 mg BID clinical dose

                Lactation

                No data available on the presence of capmatinib or its metabolites in either human or animal milk or its effects on breastfeeding, or on 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.

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                Pharmacology

                Mechanism of Action

                MET tyrosine kinase stimulates cell scattering, invasion, protection from apoptosis, and angiogenesis; a variety of cancers (eg, lung, gastric) are associated when MET becomes dysregulated owing to MET amplifications and exon 14 skipping mutations

                Absorption

                Peak plasma time: 1-2 hr

                Steady-state reached by day 3 following BID dosing

                Absorption: >70%

                Distribution

                Protein bound: 96%

                Vd (steady-state): 164 L

                Metabolism

                Primarily metabolized by CYP3A4 and aldehyde oxidase

                Elimination

                Half-life: 6.5 hr

                Clearance: 24 L/hr

                Excretion: Feces (42%, unchanged); urine (22%, unchanged)

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                Administration

                Oral Administration

                May take with or without food

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

                Missed or vomited dose: Do not make up dose; take next dose at its scheduled time

                Storage

                Dispense in the original package with the desiccant cartridge

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

                Protect from moisture

                Discard any remaining drug after 6 weeks of first opening the bottle

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                Images

                No images available for this drug.
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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

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

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