预见未来 | 中国蛋白降解药物研发进展如何?这些疗法有何特点?
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根据目前公开披露信息,中国在研蛋白降解药物中,除了10款药物靶点未知以外,有25款药物针对的靶点已有获批的靶向疗法,占比58%,包括IKZF1/3、ER、AR等10个久经验证的靶点。虽然这些靶点已有药物获批上市,但是蛋白降解的治疗模式可能比抑制靶点活性的抑制剂具有更好的效力,或者在克服耐药突变方面具有更好的潜力。8款药物针对在研抑制剂等靶向疗法正在开发的靶点,但暂无针对该靶点疗法的药物上市,占比19%,包括MDM2、CDK9、SHP2等8个靶点。其中,有些靶点是难于被传统小分子抑制剂靶向的靶点,比如MYC。蛋白降解剂无需与靶点蛋白的活性位点以高亲和力结合就能够介导降解,因此可能提供靶向难于成药靶点的新方式。
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