Emerging role of carfilzomib in treatment of relapsed and refractory lymphoid neoplasms and multiple myeloma.
Emerging role of carfilzomib in treatment of relapsed and refractory lymphoid neoplasms and multiple myeloma.
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DOI：
10.2147/ce.s13838
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发表时间：
2011
期刊：
影响因子：
--
通讯作者：
O'Connor OA
中科院分区：
文献类型：
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作者：
Jain S;Diefenbach C;Zain J;O'Connor OA
蛋白酶体抑制形成抗骨髓瘤治疗的基石。第一类蛋白酶体抑制剂硼替佐米，无论是单独使用还是与其他化疗药物联合使用，均可在临床和分子定义的高危疾病患者中诱导较高的总体缓解率和缓解质量。然而，对硼替佐米的耐药性和与治疗相关的神经毒性仍然是具有挑战性的问题。卡非佐米是一种新型、耐受性良好、不可逆的蛋白酶体抑制剂，神经毒性极小。卡非佐米在硼替佐米和免疫调节剂难治性骨髓瘤患者中显示出有希望的活性。本文综述了卡非佐米在硼替佐米初治和硼替佐米暴露人群中治疗多发性骨髓瘤的药理学、安全性和疗效。
Proteasome inhibition forms the cornerstone of antimyeloma therapy. The first-in-class proteasome inhibitor, bortezomib, either alone or in combination with other chemotherapeutic agents, induces high overall response rates and response qualities in patients with clinically and molecularly defined high-risk disease. However, resistance to bortezomib and neurotoxicity associated with the treatment remain challenging issues. Carfilzomib is a novel, well tolerated, irreversible proteasome inhibitor with minimal neurotoxicity. Carfilzomib demonstrates promising activity in myeloma patients who are refractory to bortezomib and immunomodulatory agents. This review focuses on the pharmacology, safety, and efficacy of carfilzomib for the treatment of multiple myeloma in bortezomib-naïve and bortezomib-exposed populations.