TITLE:
Abemaciclib, a Recent Novel FDA-Approved Small Molecule Inhibiting Cyclin-Dependant Kinase 4/6 for the Treatment of Metastatic Breast Cancer: A Mini-Review
AUTHORS:
Lou Anna Voli, Janat A. Mamyrbékova, Jean-Pierre Bazureau
KEYWORDS:
Approved Drug, Abemaciclib, FDA, EMA, CDK4/6, Protein Kinase Inhibitor, Metastatic Breast Cancer
JOURNAL NAME:
Open Journal of Medicinal Chemistry,
Vol.10 No.3,
September
2,
2020
ABSTRACT: 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.