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


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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