carfilzomib

Carfilzomib is a second-generation, irreversible proteasome inhibitor with a unique epoxyketone structure. It selectively and covalently binds to the N-terminal threonine of the 20S proteasome (the catalytic core of the 26S proteasome), inhibiting its chymotrypsin-like activity at both β2 and β5 subunits. This dual inhibition leads to accumulation of misfolded proteins, inducing apoptosis in malignant plasma cells while minimizing off-target effects. Carfilzomib is primarily indicated for adults with relapsed or refractory multiple myeloma who have received at least two prior therapies including a proteasome inhibitor and an immunomodulatory agent. It is administered intravenously, often in combination with dexamethasone or other agents[1][3][4][5][6]. The drug was originally developed by Onyx Pharmaceuticals (now part of Amgen) and first approved by the FDA in July 2012[6]. In China, it is marketed as Kyprolis (凯洛斯) since July 2021[1].

Brand names

Kyprolis凯洛斯

Other names

卡非佐米Carfilzomib for Injection注射用卡非佐米