Lerociclib

Lerociclib is an inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 (IC₅₀s = 1 and 2 nM for Cdk4/cyclin D1 and Cdk6/cyclin D3, respectively).¹ It is selective for Cdk4 and Cdk6 over seven related Cdks, including Cdk9/cyclin T, Cdk5/p25, and Cdk1/cyclin B1 (IC₅₀s = 28, 1,200, and 2,400 nM, respectively). Lerociclib induces cell cycle arrest at the G₁ phase in WM266-4 melanoma cells (EC₅₀ = ~20 nM). It selectively inhibits the proliferation of a variety of cancer cells expressing retinoblastoma protein (Rb) over non-Rb-expressing cancer cells (EC₅₀s = 23-784 and 2,691->10,000 nM, respectively). Lerociclib reduces intratumoral levels of phosphorylated Rb (pRb) in an MCF-7 mouse xenograft model when administered as a single dose of 100 mg/kg and inhibits tumor growth in the same model at doses ranging from 10 to 100 mg/kg in the diet for 28 days.

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1. Bisi, J.E., Sorrentino, J.A., Jordan, J.L., et al. Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors. Oncotarget. 8(26), 42343-42358 (2017).