摘要
Abemaciclib (Verzerio<span style="white-space:nowrap;"><sup><span style="font-family:Verdana, Helvetica, Arial;white-space:normal;background-color:#FFFFFF;">®</sup>) 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<sup>+</sup>), human epidermal growth factor receptor 2 negative (HER2<sup><span style="white-space:nowrap;"><sup><span style="white-space:nowrap;">−</sup></sup>) 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.
Abemaciclib (Verzerio<span style="white-space:nowrap;"><sup><span style="font-family:Verdana, Helvetica, Arial;white-space:normal;background-color:#FFFFFF;">®</sup>) 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<sup>+</sup>), human epidermal growth factor receptor 2 negative (HER2<sup><span style="white-space:nowrap;"><sup><span style="white-space:nowrap;">−</sup></sup>) 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.
作者
Lou Anna Voli
Janat A. Mamyrbékova
Jean-Pierre Bazureau
Lou Anna Voli;Janat A. Mamyrbékova;Jean-Pierre Bazureau(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, Côte d’Ivoire)
