nuv-868

NUV-868 is an orally bioavailable, BD2-selective small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins, specifically targeting BRD4. BET proteins are epigenetic regulators that control the expression of oncogenes such as c-myc and play a critical role in tumor growth and differentiation. NUV-868 is designed to be highly selective for the BD2 domain over BD1 (approximately 1,500-fold selectivity), which may reduce toxicity compared to less selective BET inhibitors. The drug has been investigated as a monotherapy and in combination with PARP inhibitors (such as olaparib) or androgen receptor-directed therapies (such as enzalutamide), particularly for advanced solid tumors including triple-negative breast cancer, ovarian cancer, pancreatic cancer, and metastatic castration-resistant prostate cancer[1][3][6][7]. Development was paused after Phase I/1b studies due to safety and efficacy analysis; further development in new indications is under consideration[4].