Products
Carfilzomib was approved in many countries in 2015 as a powder for the preparation of an infusion solution (Kyprolis).
Structure and properties
Carfilzomib (C40H57N5O7, Mr = 719.9 g/mol) exists as a crystalline substance that is practically insoluble in water. It is a peptide derivative, a tetrapeptide epoxyketone. Epoxyketones are derivatives of epoxomicin, a natural product from actinomycetes.
Effects
Carfilzomib (ATC L01XX45) has antitumor, antiproliferative, and proapoptic properties. The effects are due to irreversible and selective binding to the 20S proteasome, the proteolytic core particle of the 26S proteasome. Proteasomes are large protein complexes that degrade proteins in cells.
Indications
In combination with lenalidomide and dexamethasone for the treatment of relapsed multiple myeloma (2nd-line agent).
Dosage
According to the SmPC. The drug is administered as an intravenous infusion.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Carfilzomib is a substrate of P-glycoprotein and BCRP and is metabolized by peptidase and epoxide hydrolase.
Adverse effects
The most common possible adverse effects include anemia, fatigue, thrombocytopenia, diarrhea, nausea, fever, dyspnea, respiratory infection, cough, and peripheral edema.
