Phase I Study Of The Ptefb Inhibitor Bay 1251152 In Patients With Acute Myelogenous Leukemia

Introduction: The critical role of cyclin-dependent kinases in cell division and gene transcription has made them targets for anti-cancer therapies. Positive transcription elongation factor b (PTEFb)/cyclin-dependent kinase 9 (CDK9) plays a key role in transcription of short-lived anti-apoptotic survival proteins and oncogenes such as MYC and MCL-1. BAY 1251152 (BAY) is a potent and highly selective second generation PTEFb/CDK9 inhibitor. We report here the results of a phase I study to determine the safety, tolerability, pharmacokinetics (PK), maximum tolerated dose and preliminary anti-tumor activity of BAY in patients with AML.