Abemaciclib, a Recent Novel FDA-Approved Small Molecule Inhibiting Cyclin-Dependant Kinase 4/6 for the Treatment of Metastatic Breast Cancer: A Mini-Review
Abemaciclib, a Recent Novel FDA-Approved Small Molecule Inhibiting Cyclin-Dependant Kinase 4/6 for the Treatment of Metastatic Breast Cancer: A Mini-Review作者机构：Institut des Sciences Chimiques de Rennes ISCR UMR CNRS 6226 Université de Rennes 1 Campus de Beaulieu Campus de Beaulieu Bat. 10A CS 74205 263 Avenue du Général Leclerc 35042 Rennes Cedex France Laboratoire de Chimie Bio-Organique et de Subtances Naturelles (LCBOSN) Université Nangui Abrogoua Voie Express d’Abobo Adjamé Abidjan Cô te d’Ivoire
出 版 物：《Open Journal of Medicinal Chemistry》 (药物化学期刊（英文）)
年 卷 期：2020年第10卷第3期
页 面：128-138页
学科分类：1002[医学-临床医学] 100214[医学-肿瘤学] 10[医学]
主 题：Approved Drug Abemaciclib FDA EMA CDK4/6 Protein Kinase Inhibitor Metastatic Breast Cancer
摘 要：Abemaciclib (Verzerio®) is a cell cycle inhibitor of both CDK4 and CDK6. In 2017, abemaciclib was approved by the Food and Drug Administration (FDA) and, in 2018 by the European Medicines Agency (EMA) for the treatment of postmenopausal women with hormone receptor positive (HR+), human epidermal growth factor receptor 2 negative (HER2−) advanced breast cancer. In this mini-review, we provide a series of information for respectively their targets and its selectivity, results on preclinical trial, clinical phase I, II and III trials, and some perspectives. We also describe the batch and flow steps used for the synthesis of this cancer drug.
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