Carfilzomib is a selective proteasome inhibitor used primarily in the treatment of multiple myeloma, a cancer of plasma cells in the bone marrow. It works by irreversibly blocking the chymotrypsin-like activity of the 20S proteasome, leading to the accumulation of misfolded proteins and inducing cancer cell death. Developed as a next-generation therapy to improve upon the first proteasome inhibitor bortezomib, Carfilzomib was designed to be more potent and cause fewer side effects such as peripheral neuropathy. It was approved by the U.S. FDA in 2012 for patients with relapsed or refractory multiple myeloma who had received prior treatments, marking a significant advancement in targeted cancer therapy.
Uses of Carfilzomib
Relapsed or refractory multiple myeloma – used when patients have received prior therapies.
Combination therapy – often given with: Dexamethasone (Kd regimen), Lenalidomide and dexamethasone (KRd regimen)
Effective in bortezomib-resistant patients – works in cases where first-generation proteasome inhibitors fail.
Investigational uses – being studied for other hematologic cancers and some solid tumors.
Advantage over older therapies – more potent proteasome inhibition with lower risk of peripheral neuropathy.