Products
Bortezomib is commercially available as a lyophilizate for the preparation of a solution for injection (Velcade). It has been approved in many countries since 2005. Generic versions were registered in 2018.
Structure and properties
Bortezomib (C19H25BN4O4, Mr = 384.2 g/mol) is a dipeptidyl derivative of boric acid.
Effects
Bortezomib (ATC L01XX32) has cytotoxic and antitumor properties. It is a selective and reversible inhibitor of the 26S proteasome. The 26S proteasome is a large protein complex that degrades ubiquitin-bound proteins that are, for example, misfolded or otherwise abnormal. Inhibition leads to disruption of cell homeostasis and cell death. In cancer cells, other mechanisms play a role. Bortezomib has a long half-life of up to 190 hours.
Indications
- For the treatment of multiple myeloma.
- For the treatment of mantle cell lymphoma.
Dosage
According to the professional information. The drug is administered intravenously or subcutaneously.
Contraindications
- Hypersensitivity
- Pregnancy, lactation
Full precautions can be found in the drug label.
Interactions
Bortezomib is a substrate of several CYP450 isozymes, mainly CYP3A4, 2C19, and 1A2. Corresponding drug-drug interactions are possible.
Adverse effects
The most common possible adverse effects include:
- Nausea, diarrhea, constipation, vomiting, lack of appetite.
- Fatigue
- Fever
- Thrombocytopenia, anemia, neutropenia.
- Peripheral neuropathy, headache, paresthesias.
- Respiratory disorders
- Skin rash, shingles
- Muscle pain
