DOI: 10.4255/mcpharmacol.21.01

The emerging CDK4/6 inhibitor for breast cancer treatment

M. Saeed Sheikh1,* and Siem A. Satti1,2

1Department of Pharmacology, Sate University of New York, Upstate Medical University, Syracuse, New York and 2New York Institute of Technology, Old Westbury, New York

Abstract

The cyclin-dependent kinase (CDK) inhibitors have emerged as important cancer therapeutics. To date, three CDK4/6 inhibitors in combination with endocrine therapy have been approved by the U.S. Food and Drug Administration for the treatment of hormone receptor-positive, HER2-negative advanced breast cancer. These include, palbociclib, ribociclib and abemaciclib. More recently, a newer CDK4/6 inhibitor named dalpiciclib has been tested in the phase III DAWNA-1 study, which is a randomized, double-blind, placebo-controlled trial that investigates dalpiciclib in combination with fulvestrant in hormone receptor-positive, HER2-negative advanced breast cancer patients that have relapsed or progressed on prior endocrine therapy. Dalpiciclib is an oral agent and an emerging ATP-competitive CDK4/6 inhibitor. The interim results of DAWNA-1 study revealed that dalpiciclib in combination with fulvestrant significantly prolonged the progression-free survival. The clinical use and side effects of palbociclib, ribociclib and abemaciclib as well as dalpiciclib are reviewed here.

Keywords: Breast cancer; Palbociclib; Ribociclib; Abemaciclib; Dalpiciclib; Fulvestrant

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