Spotlight on ixazomib: potential in the treatment of multiple myeloma.
Spotlight on ixazomib: potential in the treatment of multiple myeloma.
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DOI：
10.2147/dddt.s93602
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发表时间：
2016
期刊：
影响因子：
--
通讯作者：
Azab AK
中科院分区：
文献类型：
--
作者：
Muz B;Ghazarian RN;Ou M;Luderer MJ;Kusdono HD;Azab AK
尽管蛋白酶体抑制剂（PI）如硼替佐米和卡非佐米在延长多发性骨髓瘤患者生存期方面取得了显著的治疗进展，但耐药性、周围神经病变和药代动力学局限性的发展仍是使用这些化合物时面临的主要挑战。Ixadine是第二代PI，活性优于其他PI。与注射给药的硼替佐米和卡非佐米不同，ixazomib是美国食品药品监督管理局批准的首个口服PI。本综述讨论了导致美国食品药品监督管理局批准ixazomib的生化特性、作用机制、临床前疗效和临床试验结果。
Despite the significant therapeutic advances achieved with proteasome inhibitors (PIs) such as bortezomib and carfilzomib in prolonging the survival of patients with multiple myeloma, the development of drug resistance, peripheral neuropathy, and pharmacokinetic limitations continue to pose major challenges when using these compounds. Ixazomib is a second-generation PI with improved activity over other PIs. Unlike bortezomib and carfilzomib, which are administered by injection, ixazomib is the first oral PI approved by US Food and Drug Administration. This review discusses the biochemical properties, mechanisms of action, preclinical efficacy, and clinical trial results leading to the US Food and Drug Administration approval of ixazomib.