Larotrectinib

Products

Larotrectinib has been approved in the United States since 2018, in the EU since 2019, and in many countries since 2020 in capsule and oral solution form (Vitrakvi).

Structure and properties

Larotrectinib (C21H22F2N6O2, Mr = 428.4 g/mol) is present in the drug as larotrectinib sulfate.

Effects

Larotrectinib (ATC L01XE53) has antitumor and antiproliferative properties. The effects are due to selective and competitive inhibition of the tropomyosin receptor kinases TRKA, TRKB, and TRKC. Larotrectinib has a short half-life of approximately 3 hours.

Indications

Patients with solid tumors with a neurotrophic tyrosine receptor kinase (NTRK) gene fusion.

Dosage

According to the SmPC. Capsules are taken twice daily (morning and evening), independent of meals.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Larotrectinib is a substrate of CYP3A, P-glycoprotein, and BCRP.

Adverse effects

The most common potential adverse effects include fatigue, increased ALT, dizziness, increased AST, constipation, nausea, anemia, and vomiting.