enitociclib

Enitociclib is a selective, small-molecule inhibitor of cyclin-dependent kinase 9 (CDK9), the catalytic subunit of the positive transcription elongation factor b (PTEFb). By inhibiting CDK9, enitociclib blocks phosphorylation and activity of RNA polymerase II, leading to suppression of gene transcription for anti-apoptotic proteins such as MYC and MCL1. This results in cell cycle arrest and apoptosis in tumor cells. Enitociclib has demonstrated preclinical efficacy in multiple myeloma, lymphoma, leukemia models, and is being developed primarily for hematological malignancies including non-Hodgkin lymphoma (NHL), chronic lymphocytic leukemia (CLL), Richter's syndrome, and solid tumors. It is administered intravenously once weekly to optimize therapeutic effects while minimizing toxicity[1][2][4][5][6].

Other names

enitociclib