Respiratory and thoracic cancers:
Indications for: TABRECTA
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.
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.
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).
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.
Peripheral edema, nausea, fatigue, vomiting, dyspnea, decreased appetite, constipation, diarrhea, cough; lab abnormalities, ILD/pneumonitis, hepatotoxicity, pancreatic toxicity, hypersensitivity reactions.
Half-life: 6.5 hours. Mean (%CV) steady-state apparent clearance: 24 L/hr (82%).
Fecal (78%), renal (22%).
Generic Drug Availability: