Abemaciclib (1231930-82-7) is a potent and selective CDK4/6 inhibitor (IC50 = 2 nM and 10 nM respectively).1 It caused G1 cell cycle arrest in colo-205 colorectal cells, MDA-MB-361 breast cancer cells, and MV4-11 AML cells. Abemaciclib was also active in several human tumor xenograft models. It displayed efficacy in patients with various solid tumors including breast cancer, non-small cell lung cancer. Glioblastoma, melanoma, colorectal cancer, and hormone receptor-positive breast cancer.2 Abemaciclib induced a T cell inflamed tumor microenvironment and enhanced the efficacy of PD-L1 checkpoint blockade in MCF-7 breast cancer cells.3 FDA approved for the treatment of advanced breast cancers.
1) Gelbert et al. (2014), Preclinical characterization of the CDK4/6 inhibitor LY2835219: In-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine; Invest. New Drugs, 32 825
2) Patnail et al. (2016), Efficacy and Safety of Abemaciclib, an Inhibitor of CDK4 and CDK6, for Patients with Breast Cancer, Non-small Cell Lung Cancer, and Other Solid Tumors; Cancer Discov., 6 740
3) Schaer et al. (2018), The CDK4/6 Inhibitor Abemaciclib Induces a T Cell Inflamed Tumor Microenvironment and Enhances the Efficacy of PD-L1 Checkpoint Blockade; Cell Rep., 22 2978