Products
Alectinib was approved in capsule form in Japan in 2014, in the United States in 2015, and in many countries in 2017 (Alecensa).
Structure and properties
Alectinib (C30H34N4O2, Mr = 482.6 g/mol) is present in the drug product as alectinib hydrochloride, a white to yellow-white powder. It has an active metabolite (M4).
Effects
Alectinib (ATC L01XE36) has cytostatic, antitumor, and antiproliferative properties. The effects are based on inhibition of the tyrosine kinases ALK (Anaplastic Lymphoma Kinase) and RET (Receptor Tyrosine Kinase). This leads to cell death of tumor cells by apoptosis. The half-life is 32.5 hours.
Indications
For the treatment of patients with locally advanced or metastatic ALK-positive non-small cell lung cancer (NSCLC) after progression on crizotinib or crizotinib intolerance.
Dosage
According to the SmPC. Capsules are taken in the morning and evening with food.
Contraindications
Alectinib is contraindicated in the presence of hypersensitivity. Full precautions can be found in the drug label.
Interactions
Alectinib is a substrate of CYP3A4 and corresponding interactions are possible.
Adverse effects
The most common potential adverse effects include constipation, edema, muscle pain, and nausea.