Abemaciclib, a Recent Novel FDA-Approved Small Molecule Inhibiting Cyclin-Dependant Kinase 4/6 for the Treatment of Metastatic Breast Cancer: A Mini-Review

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.

Molecular perspective on targeted therapy in breast cancer: a review of current status

“…Another orally administered, selective, small molecule CDK4/6 inhibitor, abemaciclib was approved by FDA in 2017 for the treatment of postmenopausal women with HR + , HER2- advanced breast cancer [ 62 ]. Abemaciclib, which has been approved for use in combination with endocrine therapy [ 63 ], can also be used as monotherapy in adult patients with disease progression following endocrine therapy and previous chemotherapy in a metastatic setting [ 64 ].…”