■晚期或转移性乳腺癌(MBC)与不良预后相关,并在医疗管理和治疗决策中提出了许多挑战。作用于细胞周期机制的抗癌药物在临床前研究中显示出巨大的潜力。在临床试验中,abemaciclib,由礼来公司开发的可逆ATP竞争性细胞周期蛋白依赖性激酶4/6(CDK4/6)抑制剂,在晚期或转移性激素受体阳性(HR+)/人表皮生长因子受体2阴性(HER2-)乳腺癌患者中,联合内分泌治疗(ET)与单独ET相比具有更好的结局。代表了该人群的新护理标准。Abemaciclib已被美国食品和药物管理局(FDA)批准用于HR+/HER2-MBC。在中国,根据MONARCHplus试验的结果,abemaciclib也获得了国家医药产品管理局(NMPA)的批准。最近,abemaciclib已被FDA和NMPA批准为第一个也是唯一的CDK4/6抑制剂,用于HR+/HER2-节点阳性,早期乳腺癌(EBC)复发风险高,Ki-67评分≥20%。abemaciclib的进一步试验正在进行中。这是abemaciclib在乳腺癌中的临床发展概述。
■我们回顾了2011年至2021年在PubMed中与CDK4/6抑制剂有关的英文出版物。
■在这篇评论中,我们总结了机制,abemaciclib的临床前和临床研究结果,描述当前的治疗适应症,正在进行的临床试验,安全性和耐受性,和未来的前景。
■Abemaciclib是一种独特的CDK4/6抑制剂,具有独特的特性和有希望的数据,这给HR+带来了好处,HER2-乳腺癌患者。
UNASSIGNED: Advanced or metastatic breast cancer (MBC) is associated with poor prognosis and presents many challenges in medical management and treatment decisions. Anticancer drugs that act on cell cycle mechanisms have shown great potential in preclinical studies. In clinical trials, abemaciclib, a reversible ATP-competitive cyclin-dependent kinase 4/6 (CDK4/6) inhibitor developed by Eli Lilly and Company, combined with endocrine therapy (ET) were associated with superior outcomes compared with ET alone in patients with advanced or metastatic hormone receptor positive (HR+)/human epidermal growth factor receptor 2 negative (HER2-) breast cancer, representing a new standard-of-care in this population.
Abemaciclib has been approved by the U.S. Food and Drug Administration (FDA) for use in HR+/HER2- MBC. In China,
abemaciclib was also approved by the National Medical Products Administration (NMPA) based on findings from the MONARCH plus trial. Recently, abemaciclib have been approved as the first and only CDK4/6 inhibitor by FDA and NMPA for use in HR+/HER2-, node-positive, early breast cancer (EBC) at high risk of recurrence and Ki-67 score ≥20%. Further trials of
abemaciclib are ongoing. This is an overview of the clinical development of
abemaciclib in breast cancer.
UNASSIGNED: We reviewed English publications in PubMed related to CDK4/6 inhibitors from 2011 to 2021.
UNASSIGNED: In this
review, we summarized the mechanism, results of preclinical and clinical studies of abemaciclib, describing current indications for treatment, ongoing clinical trials, safety and tolerability, and future perspectives.
UNASSIGNED: Abemaciclib is a unique CDK4/6 inhibitor with distinctive characteristics and promising data, which bring benefit to HR+, HER2- breast cancer patients.