BGC-515

BGC-515 is an orally administered, covalent small-molecule inhibitor of TEA domain (TEAD) transcription factors being developed by BridGene Biosciences for the treatment of advanced solid tumors, including malignant mesothelioma and epithelioid hemangioendothelioma.[1][2][5][9] Discovered using BridGene’s chemoproteomic IMTAC platform, the drug targets TEAD proteins that partner with the Hippo pathway effectors YAP and TAZ, aiming to disrupt oncogenic transcriptional programs and promote tumor cell apoptosis.[2][5][9][11] BGC-515 is currently in phase 1, first-in-human, dose-escalation and dose-expansion studies in the United States and China to evaluate its safety, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity in patients with advanced solid tumors characterized by Hippo pathway dysregulation.[1][2][4][5][8][13]