CDK4/6抑制剂帕博西尼的研究进展

Advances of CDK4/6 inhibitor palbociclib in cancer treatment

摘要:

细胞周期蛋白依赖性激酶(cyclin-dependent kinases, CDKs)在细胞周期的调控中起着至关重要的作用，是干扰肿瘤细胞分裂和增殖的特异治疗靶点。帕博西尼是全球首个CDK4/6特异性抑制剂，临床疗效显著，毒性可控，被批准联合来曲唑治疗绝经后ER+、HER2-的晚期乳腺癌患者，作为转移性疾病的初始内分泌治疗。目前已经开始研究这种抑制剂对其他恶性肿瘤的疗效。本文综述了帕博西尼的作用机制及其在不同肿瘤治疗中的研究进展，并对帕博西尼的发展前景进行了展望。

Abstract:

Cyclin-dependent kinases(CDKs) play a pivotal role in cell cycle regulation, which makes them a distinct therapeutic target to interfere with cell division and proliferation in cancer patients. Palbociclib is the first and specific inhibitor of CDK4/6 with excellent clinical efficacy and limited toxicity. It has been approved in combination with letrozole for the treatment of postmenopausal women with ER+ and HER2- advanced metastatic breast cancer as initial endocrine-based therapy. Extensive studies have also shown that this inhibitor may be used as a potential targeting drug for treatment of other cancers. This review describes the action and mechanism of palbociclib in breast cancer treatment and preclinical studies in other cancers, as well as prospects in the development of palbociclib.