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carfilzomib (kar-FIL-zoh-mib)A drug used alone or with other drugs to treat multiple myeloma that has gotten worse or came back after treatment with other anticancer therapy. It is also being studied in the treatment of other types of cancer. Carfilzomib blocks the action of enzymes called proteasomes, which may help keep cancer cells from growing and may kill them. It is a type of proteasome inhibitor. Also called Kyprolis.

Information about Carfilzomib

Carfilzomib is an irreversible proteasome inhibitor and antineoplastic agent that is used in treatment of refractory multiple myeloma.   

Liver safety of Carfilzomib

Carfilzomib is associated with a low rate of serum enzyme elevations during treatment and has been implicated to rare instances of clinically apparent, acute liver injury some of which have been fatal. 

Mechanism of action of Carfilzomib

  Carfilzomib (kar filz’ oh mib) is an orally available, small molecule inhibitor of the 26S proteasome, the intracellular complex that degrades proteins involved in cell signaling and cell cycle regulation.  Blocking proteasome activity prevents activation of factors involved in cell growth and resistance to chemotherapy induced apoptosis, leading to cancer cell death.  Carfilzomib was the second proteasome inhibitor developed as an antineoplastic agent, differing from the initial (bortezomib) in being an irreversible inhibitor and not being metabolized by the CYP 3A4 system.  Clinical trials of carfilzomib in patients with multiple myeloma showed at least partial responses in patients who were resistant to other antineoplastic agents including bortezomib. 

FDA approval information for Carfilzomib

Carfilzomib received accelerated approval for use in the United States in 2012 for therapy of previously treated, refractory or relapsing multiple myeloma. 

Dosage and administration for Carfilzomib

Carfilzomib is available in powdered form in single use vials of 60 mg under the brand name Kyprolis.  The typical starting dose is 20 mg per meter-squared per day intravenously for two days each week for 3 weeks, and then in cycles after a rest period.  It is typically administered with dexamethasone with or without lenalidomide. 

Side effects of Carfilzomib

Common side effects include fatigue, nausea, diarrhea, constipation, anorexia, fatigue, dyspnea, thrombocytopenia, neutropenia, anemia peripheral neuropathy, rash and fever.  Infusion reactions are not uncommon with the first cycle of carfilzomib and dexamethasone pretreatment is recommended.  Other uncommon, but potentially severe side effects include peripheral neuropathy, cardiac and pulmonary toxicity, bone marrow suppression and tumor lysis syndrome.


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