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

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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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            Formulary

            FormularyPatient Discounts

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            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.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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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.