zemirciclib

Zemirciclib (AZD4573) is a potent and highly selective small molecule inhibitor of cyclin-dependent kinase 9 (CDK9), developed for intravenous administration. It acts by transiently inhibiting CDK9, the catalytic subunit of the RNA polymerase II elongation factor positive transcription elongation factor b (P-TEFb). This inhibition blocks phosphorylation and kinase activity of CDK9, preventing P-TEFb-mediated activation of RNA Pol II. As a result, gene transcription of anti-apoptotic proteins such as Mcl-1 is suppressed, leading to cell cycle arrest and apoptosis in tumor cells. Zemirciclib has shown strong preclinical efficacy in hematologic malignancies including multiple myeloma (MM), acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), peripheral T-cell lymphoma (PTCL), natural killer/T-cell lymphoma (NKTCL), and classical Hodgkin lymphoma (cHL). It is currently being evaluated in phase II clinical trials for relapsed/refractory PTCL or cHL[2][4][5][7].

Other names

zemirciclibAZD4573 free baseAZD-4573 free baseAZD 4573 free base