口服CDK4/6抑制剂abemaciclib的药理与临床

Pharmacological effects and clinical evaluation of abemaciclib——a new oral CDK4/6 inhibitor

Abemaciclib是一种新型口服细胞周期蛋白依赖性激酶CDK4/6抑制剂。2017年9月28日,美国FDA批准其用于激素受体阳性(HR+)/人类表皮生长因子2阴性(HER-2)的晚期或转移性乳腺癌;本品对内分泌治疗无效的乳腺癌患者提供了一种新的靶向治疗选择。Abemaciclib是FDA批准的第3个CDK4/6抑制剂,也是惟一一个可以单独使用的CDK4/6抑制剂。本文就abemaciclib的作用机制、药动学、药物相互作用、临床试验及安全性等信息做一综述,以期为临床用药提供帮助。

Abemaciclib is a new oral cyclin-dependent kinase CDK4/6 inhibitor. On September 28,2017, the U.S. Food and Drug Administration approved abemaciclib for hormone receptor（HR）-positive, human epidermal growth factor receptor 2（HER-2）-negative advanced or metastatic breast cancer with disease progression following endocrine therapy adult patients. Abemaciclib is the third paragraph CDK4/6 inhibitor approved by FDA, meanwhile it is only approved as individual therapy, which can provide a new targeting therapy choice for some breast cancer patients not responding to conventional treatment. In this paper, the properties, action mechanism, pharmacokinetics, drug interaction, clinical trials and applications of abemaciclib are summarized for the purpose of providing reference for clinical treatments.