Abstract

Cyclin-dependent kinase 4 (CDK4) and CDK6 have a crucial role in the G1-S transition of the cell cycle by mediating the phosphorylation of the retinoblastoma protein (Rb), and so are important regulators of cell division. A phase 1 trial of PD 0332991, a novel, orally bioavailable, specific inhibitor of CDK4 and CDK6 activity in patients with advanced cancers has shown it to be well-tolerated. A subsequent multi-arm phase 2 trial is nearing completion (NCT01037790).

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