Respiratory and thoracic cancers:

Indications for: TEPMETKO

In adults with metastatic non-small cell lung cancer (NSCLC) harboring mesenchymal-epithelial transition (MET) exon 14 skipping alterations.

Adult Dosage:

Confirm presence of MET exon 14 skipping alterations in plasma or tumor specimens. Swallow whole. Take with food. 450mg once daily until disease progression or unacceptable toxicity. If difficulty swallowing solids: disperse tab(s) in 30mL non-carbonated water; stir and drink immediately or within 1hr; followed with additional 30mL rinse and drink immediately. Also, may give via NG-tube. Dose modifications for adverse reactions: see full labeling.

Children Dosage:

Not established.

TEPMETKO 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. Severe renal (CrCl <30mL/min) or hepatic (Child-Pugh C) impairment. 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).

TEPMETKO Classification:

Kinase inhibitor.

TEPMETKO Interactions:

May be potentiated by dual strong CYP3A and P-gp inhibitors; avoid. May be antagonized by strong CYP3A inducers; avoid. Potentiates certain P-gp substrates (eg, dabigatran etexilate); if unavoidable, reduce substrate dosage.

Adverse Reactions:

Edema, fatigue, nausea, diarrhea, musculoskeletal pain, dyspnea; Grade 3 or 4 lab abnormalities (decreased lymphocytes, decreased albumin, decreased sodium, increased GGT, increased amylase, increased ALT/AST, decreased hemoglobin); hepatotoxicity.

Metabolism:

CYP3A4, CYP2C8.

Drug Elimination:

Fecal (~85%), renal (13.6%).

Half-life: 32 hours.

Apparent clearance (CL/F): 23.8 L/h (87.5%). 

Generic Drug Availability:

NO

How Supplied:

Tabs—30, 60