Products
Entrectinib was approved in capsule form in the United States in 2019 and in the EU and Switzerland in 2020 (Rozlytrek).
Structure and properties
Entrectinib (C31H34F2N6O2, Mr = 560.6 g/mol) exists as a white to faint pink powder.
Effects
Entrectinib (ATC L01XE56) has antitumor, antiproliferative, and proapoptotic properties. The effects are due to inhibition of tyrosine kinases. These include TRKA, TRKB and TRKC, ROS1 and ALK. Entrectinib has a major active metabolite involved in the effects. It also leads to tumor cell apoptosis. Entrectinib can be used in various tumor types, for example, sarcoma, head and neck cancer, non-small cell lung cancer (NSCLC), colorectal cancer, acute myeloid leukemia and glioma. Entrectinib also crosses the blood–brain barrier (BBB).
Indications
Entrectinib is used for the treatment of solid tumors with an NTRK gene fusion without a resistance mutation. Another indication is ROS1-positive non-small cell lung cancer (NSCLC).
Dosage
According to the SmPC. Capsules are taken once daily, independent of meals.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Entrectinib is metabolized primarily by CYP3A4 and to a lesser extent by other CYP enzymes and UGT1A4.
Adverse effects
The most common possible adverse effects include (> 30%):
- Fatigue.
- Constipation
- Taste changes
- Dizziness
- Diarrhea
- Nausea
