Robert Bhatt

Robert Bhatt has been a central figure in the pharmaceutical development of BET bromodomain inhibitors, leading the discovery and optimization of I-BET762 (GSK525762/molibresib) as one of the first BET inhibitors to enter clinical trials in cancer. His research addressed the critical challenges of bromodomain selectivity, demonstrating how structural differences between BD1 and BD2 bromodomains can be exploited for more selective targeting. He contributed to understanding BET inhibitor resistance mechanisms including BRD4 point mutations and transcriptional rewiring. His recent work on BET-targeting PROTACs has shown superior efficacy over catalytic inhibition in preclinical cancer models.