AU-18069

AU-18069 is a novel, potent, and selective small molecule inhibitor of the bromodomains of the epigenetic co-activators CREB-binding protein (CBP) and its paralog p300 (EP300). Developed through a collaboration between Aurigene Discovery Technologies and Orion Pharma, AU-18069 targets these co-activators which are essential for the transcriptional activity of several oncogenic drivers, including c-Myc and the androgen receptor (AR). Preclinical data presented at AACR 2021 demonstrated that AU-18069 effectively inhibits the proliferation of various cancer cell lines, particularly those derived from prostate cancer and MYC-dependent hematological malignancies. In vivo studies in MV4-11 xenograft models showed significant tumor growth inhibition and downregulation of c-Myc. Furthermore, AU-18069 has demonstrated the potential to modulate immune phenotypes, including CD4+ T cell subsets, suggesting its utility in both solid and hematologic tumors.