The emerging CDK4/6 inhibitor for breast cancer treatment.
The emerging CDK4/6 inhibitor for breast cancer treatment.
复制标题
DOI：
--
复制
发表时间：
2021
期刊：
影响因子：
--
通讯作者：
M. Sheikh;Siem A Satti
中科院分区：
文献类型：
--
作者：
M. Sheikh;Siem A Satti
细胞周期蛋白依赖性激酶（CDK）抑制剂已成为重要的癌症治疗药物。迄今为止，三种CDK 4/6抑制剂与内分泌疗法联合已被美国食品和药物管理局批准用于治疗激素受体阳性、HER 2阴性的晚期乳腺癌。这些药物包括palbociclib、ribociclib和abemaciclib。最近，一种名为dalpiciclib的新型CDK 4/6抑制剂已在III期DAWNA-1研究中进行了测试，该研究是一项随机、双盲、安慰剂对照试验，旨在研究dalpiclib与氟维司群联合治疗激素受体阳性、HER 2阴性的晚期乳腺癌患者，这些患者在既往内分泌治疗后复发或进展。Dalpiciclib是一种口服药物，也是一种新兴的ATP竞争性CDK 4/6抑制剂。DAWNA-1研究的中期结果显示，dalpiciclib联合氟维司群显著延长了无进展生存期。本文综述了palbociclib、ribociclib和abemaciclib以及dalpiciclib的临床应用和副作用。
The cyclin-dependent kinase (CDK) inhibitors have emerged as important cancer therapeutics. To date, three CDK4/6 inhibitors in combination with endocrine therapy have been approved by the U.S. Food and Drug Administration for the treatment of hormone receptor-positive, HER2-negative advanced breast cancer. These include, palbociclib, ribociclib and abemaciclib. More recently, a newer CDK4/6 inhibitor named dalpiciclib has been tested in the phase III DAWNA-1 study, which is a randomized, double-blind, placebo-controlled trial that investigates dalpiciclib in combination with fulvestrant in hormone receptor-positive, HER2-negative advanced breast cancer patients that have relapsed or progressed on prior endocrine therapy. Dalpiciclib is an oral agent and an emerging ATP-competitive CDK4/6 inhibitor. The interim results of DAWNA-1 study revealed that dalpiciclib in combination with fulvestrant significantly prolonged the progression-free survival. The clinical use and side effects of palbociclib, ribociclib and abemaciclib as well as dalpiciclib are reviewed here.