用于乳腺癌的细胞周期蛋白依赖性激酶4/6选择性抑制剂瑞波西利  

A selective inhibitor of cyclin-dependent kinases 4/6,ribociclib,for the treatment of breast cancer

作　　者：李艳 崔英杰 刘娟娟 赵辉 王真真 周易 张晶 LI Yan;CUI Ying-jie;LIU Juan-juan;ZHAO Hui;WANG Zhen-zhen;ZHOU Yi;ZHANG Jing(Department of Pharmacy,Shandong Provincial Hospital Affiliated to Shandong First Medical University,Ji'nan 250021,China)

机构地区：[1]山东第一医科大学附属省立医院药学部,济南250021

出　　处：《中国新药杂志》2025年第4期364-369,共6页Chinese Journal of New Drugs

基　　金：国家自然科学基金项目(82204198);山东省自然科学基金项目(ZR2022MH317,ZR2021QH280)。

摘　　要：瑞波西利是一种选择性的、口服生物可利用的细胞周期蛋白依赖性激酶4/6(cyclin-dependent kinases 4/6,CDK4/6)小分子抑制剂,于2023年1月19日获得国家药品监督管理局批准,2023年2月18日在我国正式上市,用于治疗激素受体(hormone receptor,HR)阳性、人表皮生长因子受体2(human epidermal growth factor receptor 2,HER2)阴性局部晚期或转移性乳腺癌,并作为目前国内首个且唯一被批准用于绝经前、围绝经期乳腺癌患者初始治疗的CDK4/6抑制剂。本文对该药物的作用机制、药动学、药效学、临床研究、安全性评价等进行综述,以期为新药研发及瑞波西利的临床应用提供参考。Ribociclib is a selective,orally bioavailable small molecule inhibitor of cyclin-dependent kinases 4/6(CDK4/6),which was approved by the National Medical Products Administration on January 19,2023,and officially launched in China on February 18,2023.It is indicated for the treatment of locally advanced or metastatic breast cancer that is hormone receptor-positive and human epidermal growth factor receptor 2-negative(HR+/HER2-).Ribociclib is the first and currently the only CDK4/6 inhibitor approved for initial treatment of premenopausal and perimenopausal patients with breast cancer in China.This article reviews the mechanism of action,pharmacokinetics,pharmacodynamics,clinical studies,and safety evaluation of this drug,with the aim of providing references for new drug development and clinical application of ribociclib.

关 键 词：瑞波西利 细胞周期蛋白依赖性激酶4/6小分子抑制剂 乳腺癌 

分 类 号：R979.1[医药卫生—药品]