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由于心脏安全性，MCL-1抑制剂AMG 397的早期研究已被暂停

2019-09-14 Allan MedSci原创

MCL-1抑制剂Mg397心脏安全性
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Amgen在其肿瘤学管道的更新中披露，由于心脏毒性的安全信号，实验性小分子MCL-1抑制剂AMG 397的I期研究已被搁置。

MCL-1蛋白是BCL-2蛋白家族中重要的抗凋亡蛋白，至少含有一种BCL-2同源的BH结构域，是线粒体凋亡途径的关键调节因子，而含有多BH结构域的效应子BAX、BAK和BOK以及仅BH3蛋白如BIM和BAD则具有促凋亡功能。

MCL-1过表达不仅与肿瘤发生发展密切相关，而且与靶向治疗和传统化疗药物耐药密切相关，然而靶向MCL-1小分子抑制剂的研发目前尚具挑战性。Amgen在其肿瘤学管道的更新中披露，由于心脏毒性的安全信号，实验性小分子MCL-1抑制剂AMG 397的I期研究已被搁置。去年开始的AMG 397剂量递增试验迄今已招募了24例多发性骨髓瘤、非霍奇金淋巴瘤或急性髓性白血病（AML）患者。


原始出处：

http://www.firstwordpharma.com/node/1666088#axzz5zU18ApSM

本文系梅斯医学（MedSci）原创编译整理，转载需授权!

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    2019-12-09 俅侠

    #MCL-1抑制剂#

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    2020-06-26 jklm09

    #抑制剂#

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    2019-09-16 zhouqu_8

    #AMG#

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    2019-09-16 wangtianj2010@

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