| |
[摘要]：Proteosome inhibitors ore a new class of drugs that hove been shown to be cytotoxic and to induce apoptosis in tumor cells, particularly multiple myelomo (MM). In a bid to overcome the dose-limiting toxicity and adverse events observed with nonselective proteasome inhibitors, Proteolix is currently developing a novel, irreversible, epoxomicin-related proteasome inhibitor, carfilzomib (PR-171). Pharmacodynomic studies have suggested that this agent spares constitutive proteasome function, showing more selective inhibition of the immunoproteasomes of hemotologicol tumor cells. Clinical data presented to date indicate that carfilzomib provides sustained clinical benefits in relapsed and refractory MM patients and is active as a single agent and in combination regimens. Carfilzomib is presently undergoing phase Ib/II clinical investigation in the U.S. |
|
