Tabrecta

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  • Respiratory and thoracic cancers
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Tabrecta Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Capmatinib 150mg, 200mg; tabs.

    Pharmacological Class

    Kinase inhibitor.

    How Supplied

    Tabs—56

    Manufacturer

    Novartis Pharmaceuticals Corp

    Generic Availability

    NO

    Mechanism of Action

    Capmatinib inhibits MET, including the mutant variant produced by exon 14 skipping. This results in a protein with a missing regulatory domain that reduces its negative regulation leading to increased downstream MET signaling.

    Tabrecta Indications

    Indications

    In adults with metastatic non-small cell lung cancer (NSCLC) whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping as detected by an FDA approved test.

    Tabrecta Dosage and Administration

    Adult

    Confirm presence of a mutation that leads to MET exon 14 skipping in tumor specimens. Swallow whole. 400mg twice daily. Dose modifications for adverse reactions: see full labeling.

    Children

    Not established.

    Tabrecta Contraindications

    Not Applicable

    Tabrecta Boxed Warnings

    Not Applicable

    Tabrecta Warnings/Precautions

    Warnings/Precautions

    Monitor for pulmonary symptoms indicative of ILD/pneumonitis; withhold immediately if suspected and permanently discontinue if no other causes are identified. Monitor LFTs prior to initiation, every 2 weeks during 1st 3 months, then once monthly or as clinically indicated; test more frequently if increased AST, ALT or bilirubin develops. Monitor amylase and lipase at baseline, and regularly during treatment. Potential risk of photosensitivity. Advise patients to limit direct UV exposure. Severe renal impairment (CrCl 15–29mL/min). Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective contraception during and for 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 week after the last dose).

    Tabrecta Pharmacokinetics

    Absorption

    After oral administration of Tabrecta 400 mg (cancer patients), capmatinib peak plasma concentrations (Cmax) were reached in ~1 to 2 hours (Tmax). The absorption after oral administration is estimated to be >70%.

    Distribution

    Plasma protein bound: 96%.

    Apparent mean volume of distribution at steady-state: 164 L. 

    Metabolism

    Primarily CYP3A4  and aldehyde oxidase.

    Elimination

    Half-life: 6.5 hours. Mean (%CV) steady-state apparent clearance: 24 L/hr (82%). 

    Fecal (78%), renal (22%).

    Tabrecta Interactions

    Interactions

    Potentiated by strong CYP3A inhibitors; monitor closely. Potentiates CYP1A2, P-gp, or BCRP substrates; if unavoidable, reduce substrate dosage. May potentiate MATE1 or MATE2K substrates; if unavoidable, reduce substrate dosage. Antagonized by strong or possibly moderate CYP3A inducers; avoid.

    Tabrecta Adverse Reactions

    Adverse Reactions

    Peripheral edema, nausea, fatigue, vomiting, dyspnea, decreased appetite, constipation, diarrhea, cough; lab abnormalities, ILD/pneumonitis, hepatotoxicity, pancreatic toxicity, hypersensitivity reactions.

    Tabrecta Clinical Trials

    See Literature

    Tabrecta Note

    Not Applicable

    Tabrecta Patient Counseling

    See Literature

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