tepotinib

Contraindicated in:

OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Severe renal impairment;
Severe hepatic impairment;
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema

Derm: pruritus, rash

GI: ↑amylase, ↑lipase, ↑liver enzymes, abdominal pain, constipation, diarrhea, hypoalbuminemia, nausea, vomiting, HEPATOTOXICITY

GU: ↑serum creatinine

Hemat: anemia, leukopenia, lymphopenia

Metab: ↓appetite

MS: pain

Neuro: fatigue, dizziness, headache

Resp: cough, dyspnea, pleural effusion, pneumonia, INTERSTITIAL LUNG DISEASE (ILD)/PNEUMONITIS

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

May ↑ levels and risk of toxicity of P-glycoprotein substrates, including dabigatran; avoid concurrent use. If concurrent use unavoidable, ↓ dose of P-glycoprotein substrate.

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

PO (Adults ): 450 mg once daily; continue until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a kinase inhibitor that targets MET, including the mutant variant produced by exon 14 skipping, which ultimately reduces cancer cell growth.

Therapeutic effects:

Decreased spread of NSCLC.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: 72% absorbed following oral administration; absorption ↑ with high-fat, high-calorie meals.

Distribution: Extensively distributed to tissues.

Protein Binding: 98%.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A4 and CYP2C8 isoenzymes. Primarily excreted in feces (85%; 45% as unchanged drug), with 13.6% excreted in urine (7% as unchanged drug).

Half-Life: 32 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	8 hr	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy.
Advise patient to take as directed. Advise not to make up a missed dose within 8 hr of the next scheduled dose. If vomiting occurs, advise to take the next dose at the scheduled time. Emphasize the importance of routine laboratory testing.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications. Advise patient to avoid alcohol and hepatotoxic medications.
Advise patient to notify health care professional if new or worsening respiratory symptoms or signs or symptoms of pancreatitis or hepatotoxicity occur.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding. Advise patient to use effective contraception during treatment and for 1 wk after last dose.

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Indications ⬇

Contraind./Precautions ⬆ ⬇