NUV-868, a BD2-selective oral small molecule bromodomain and extra-terminal (BET) inhibitor, inhibits BRD4, a key member of the BET family that epigenetically regulates proteins that control tumor growth and differentiation.
NUV-868 is almost 1,500 times more selective for BD2 than BD1 and is designed to alleviate the therapeutic limiting toxicities observed by other non-BD2 selective BET inhibitors. NUV-868 in combination with androgen-receptor directed therapies may help to overcome resistance in prostate cancer. In addition, NUV-868 in combination with PARP inhibitors may have synergistic activity to increase efficacy across multiple solid tumors.
We dosed the first patient in a Phase 1 dose escalation study of NUV-868 for the treatment of patients with advanced solid tumors in the first quarter of 2022 and enrollment is ongoing. The Phase 1 study is designed to determine the safety and dose of NUV-868 to be used as a monotherapy and in combination with olaparib or enzalutamide for the Phase 2 and 2b portions of the study.