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抗慢性淋巴细胞白血病新药venetoclax药理作用及临床评价

张亚安,任莉萍,钮娴,张晴晴,周新月,潘 喆   

  1. 东南大学 成贤学院 制药与化学工程学院 南京210088,东南大学 成贤学院 制药与化学工程学院 南京210088,东南大学 成贤学院 制药与化学工程学院 南京210088,东南大学 成贤学院 制药与化学工程学院 南京210088,东南大学成贤学院 制药与化学工程学院,东南大学成贤学院 制药与化学工程学院
  • 收稿日期:2017-03-29 修回日期:2017-09-11 出版日期:2017-11-25
  • 基金资助:
    江苏省高等学校大学生实践创新训练计划项目(项目编号:201612689021X;项目名称:药物超分子包合作用及其应用研究);东南大学成贤学院大学生实践创新训练计划项目(项目编号:yox1778;项目名称:生理药理学微信数字平台的设计与实现)

Pharmacology and Clinical Evaluation of Venetoclax for the Treatment of Chronic Lymphocytic Leukemia

ZHANG Ya-an,REN Li-ping,NIU Xian,ZHANG Qing-qing,ZHOU Xin-yue and PAN Zhe   

  1. Department of Pharmaceutical and Chemical Engineering of Southeast University Chengxian College,Department of Pharmaceutical and Chemical Engineering of Southeast University Chengxian College,Department of Pharmaceutical and Chemical Engineering of Southeast University Chengxian College,Department of Pharmaceutical and Chemical Engineering of Southeast University Chengxian College,Department of Pharmaceutical and Chemical Engineering, Southeast University Chengxian College,Department of Pharmaceutical and Chemical Engineering, Southeast University Chengxian College
  • Received:2017-03-29 Revised:2017-09-11 Online:2017-11-25

摘要: venetoclax为首个选择性口服B淋巴细胞瘤-2(Bcl-2)蛋白抑制剂,研究证实其治疗复发/难治慢性淋巴细胞白血病(CLL)具有可控的安全性,总体及完全有效率高。2016年4月11日,美国食品药品管理局(FDA)批准venetoclax用于治疗携带17p缺失突变且曾接受过至少一种治疗的CLL。本综述主要介绍venetoclax药物作用机制、药物代谢动力学、疗效、安全性及临床研究进展。

Abstract: Venetoclax, the first oral selective inhibitor of the prosurvival protein Bcl-2, has been approved for being used as monotherapy in patients with chronic lymphocytic leukaemia(CLL) with the 17p deletion who have received at least one prior therapy by FDA. Venetoclax had high overall and complete response rates and manageable safety profile in patients with relapsed CLL. This article reviews the mechanism of action, the clinical pharmacology of venetoclax and its efficacy and safety profile in clinical studies.