CCS-1477

CCS-1477 is a potent, selective and orally bioavailable inhibitor of the Bromodomain of p300 and CBP, binding to the targets with high affinity (Kd = 1.3/1.7nM) and selectivity (Kd = 222nM; BRD4). E1A binding protein (p300) and CREB binding protein (CBP) are two closely related transcriptional activators of androgen receptor (AR) and its variant forms. CCS-1477 enhances degradation of numerous cellular proteins including the AR and AR variants in prostate cancer cells; Demonstrates potent single-agent efficacy using in vitro and in vivo models of prostate cancer, and enhances the efficacy of Enzalutamide when used in combination. It is currently in clinical evaluation for the treatment of castrate resistant prostate cancer by down-regulation of AR, AR-SV and c-MYC expression and function, which represents a new therapeutic option for prostate cancer patients who have progressed after failure of anti-androgen therapy and in combination with anti-androgens such as enzalutamide or abiraterone.