CDK9 is a cyclin dependent kinase and an essential regulator of cancer-promoting transcriptional programs and an important driver in Myc-driven solid tumors and myeloid malignancies. PRT2527 is a potent and highly selective CDK9 inhibitor currently being evaluated in a Phase 1 dose escalation study in patients whose cancers are likely to be dependent on CDK9.
Cyclin-dependent kinase 9, or CDK9, serves as a key regulator of several cancer-promoting transcriptional programs, including those driven by MCL1, MYC, and MYB. Inhibition of CDK9 has emerged as an attractive therapeutic approach to producing synthetic lethality in genomically-selected cancers, and several non-selective CDK9 inhibitors in development have demonstrated activity in multiple tumor types. However, the approach has been significantly limited due to adverse effects associated with broad kinase inhibition and in turn, a narrow therapeutic window.