Drug Overview
Kyprolis (carfilzomib; Amgen/Ono Pharmaceutical) is a second-generation proteasome inhibitor that irreversibly binds to the N-terminal threonine-containing active sites of the 20S proteasome, the proteolytic core particle within the 26S proteasome.
The proteasome is a cellular complex that breaks down proteins; it is believed to play a critical role in the degradation (and therefore regulation) of a number of proteins involved in the regulation of cell cycle, apoptosis, and angiogenesis. In vitro, Kyprolis has shown antiproliferative and proapoptotic activity in both solid and hematologic tumor cells. In animal studies, it was shown to inhibit proteasome activity and delay tumor growth in models of multiple myeloma, hematological malignancies, and solid tumors.
Kyprolis (carfilzomib; Amgen/Ono Pharmaceutical) is a second-generation proteasome inhibitor that irreversibly binds to the N-terminal threonine-containing active sites of the 20S proteasome, the proteolytic core particle within the 26S proteasome.
The proteasome is a cellular complex that breaks down proteins; it is believed to play a critical role in the degradation (and therefore regulation) of a number of proteins involved in the regulation of cell cycle, apoptosis, and angiogenesis. In vitro, Kyprolis has shown antiproliferative and proapoptotic activity in both solid and hematologic tumor cells. In animal studies, it was shown to inhibit proteasome activity and delay tumor growth in models of multiple myeloma, hematological malignancies, and solid tumors.
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