Products
Venetoclax was approved in the US and EU in 2016 and in many countries in 2018 in film-coated tablet form (Venclyxto, Venclexta).
Structure and properties
Venetoclax (C45H50ClN7O7S, Mr = 868.4 g/mol) exists as a light to dark yellow powder that is sparingly soluble in water.
Effects
Venetoclax (ATC L01XX52) has antitumor and cytotoxic properties. The effects are due to selective inhibition of the anti-apoptotic BCL-2 (B Cell Lymphoma 2) protein. Overexpression of the protein has been shown to occur in CLL, contributing to tumor cell survival and resistance to chemotherapeutic agents. Venetoclax activates programmed cell death in cells overexpressing BCL-2. The half-life is 26 hours.
Indications
For the treatment of patients with chronic lymphocytic leukemia (CLL) with a 17p deletion or TP53 mutation.
Dosage
According to the SmPC. Tablets are taken once daily with a meal and always at the same time of day. Therapy is started gradually.
Contraindications
- Hypersensitivity
- Combination with strong CYP450 inhibitors at the beginning of treatment.
- Concurrent use of preparations containing St. John’s wort, a P-gp and strong CYP3A inducer.
For complete precautions, see the drug label.
Interactions
Venetoclax is metabolized primarily by CYP3A4/5 and is a substrate of P-glycoprotein and BCRP. Appropriate drug-drug interactions must be considered.
Adverse effects
The most common potential adverse effects include neutropenia, diarrhea, nausea, anemia, upper respiratory tract infection, thrombocytopenia, and fatigue.
