AU-BGB-002

AU-BGB-002 is a novel, selective, and covalent small molecule inhibitor of Cyclin-dependent kinase 7 (CDK7), developed through a collaboration between Aurigene Discovery Technologies and BeiGene. CDK7 is a key component of the transcription factor II H (TFIIH) complex and plays a critical role in regulating the cellular transcriptional machinery by phosphorylating the C-terminal domain (CTD) of RNA polymerase II (RNAPII). By inhibiting CDK7, AU-BGB-002 disrupts the transcription of oncogenic genes that many tumor types depend on for survival. In preclinical studies, the compound demonstrated high potency, selectivity, and excellent drug-like properties, including oral bioavailability. It showed significant anti-tumor activity and tumor stasis in acute myeloid leukemia (AML) xenograft models, accompanied by complete target engagement and suppression of RNAPII Ser5 phosphorylation.