ORI-15412

ORI-15412 is a novel, selective, and brain-penetrant small molecule inhibitor of cyclin-dependent kinase 9 (CDK9) developed by Origenis. CDK9 is a critical component of the positive transcription elongation factor b (P-TEFb) complex, which regulates transcriptional elongation by phosphorylating RNA polymerase II. By inhibiting CDK9, ORI-15412 blocks the transcription of short-lived oncogenic proteins such as MCL-1 and MYC and has been shown to modulate immune checkpoint proteins like PD-L1. The compound is designed for oral administration and is currently in IND-enabling development for the treatment of advanced malignancies, specifically melanoma and triple-negative breast cancer.