SAN JOSE, CA, USA I June 28, 2024 I BridGene Biosciences, Inc., a leader in developing covalent small molecule drugs for traditional “hard-to-drug” targets, announced today that the first patient has been dosed in its Phase 1 clinical trial of BGC515, a novel TEAD inhibitor discovered through BridGene’s cutting-edge chemoproteomic platform, IMTAC™. This milestone highlights the potential of BridGene’s innovative chemoproteomics approach.

The Phase 1 study will enroll subjects in both the US and China (NCT06452160) to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity of BGC515 as a single agent in patients with advanced solid tumors, including malignant mesothelioma, epithelioid hemangioendothelioma, and other solid tumors with hippo pathway dysregulation. Dr. Timothy Yap, Ph.D., FRCP, Professor in the Department of Investigational Cancer Therapeutics (Phase I Program) and Head of Clinical Development, Therapeutics Discovery Division at the University of Texas MD Anderson Cancer Center, is the principal investigator at the initial US site, where the first patient has been enrolled.

“We are delighted to begin the clinical evaluation of BGC515 with the dosing of our first patient, and we look forward to the evaluation of the initial safety and efficacy of this exciting compound,” said Jeremy Barton, M.D., Chief Medical Officer of BridGene Biosciences.

“The initiation and dosing of our first drug in clinical development from our chemoproteomic platform marks a major inflection point for BridGene,” stated Ping Cao, Ph.D., Co-Founder and CEO of BridGene Biosciences. “This achievement underscores our commitment to addressing unmet medical needs through innovative therapeutic solutions. BGC515 represents a breakthrough in targeting the TEAD proteins, a critical component in the Hippo signaling pathway. We are proud of the progress we have made in a short time, developing a pipeline that includes previously undruggable targets for prominent oncology and immunology diseases.”

BridGene Biosciences is advancing multiple novel drug discovery programs toward the clinic and has over a dozen similar opportunities emerging in early discovery.

About the Hippo Pathway and BGC515
The Hippo pathway is a key pathway used by cells to control expression of a group of genes by regulating activity of transcription factors YAP and TAZ. YAP and TAZ function in a complex with partner proteins, the TEADs, which are the targets of BGC515. A variety of human cancers depend on activation of YAP and TAZ, which can occur by various mechanisms.

BGC515 is an internally-developed, orally-administered, covalent TEAD inhibitor.

About BridGene Biosciences
BridGene is a biotechnology company focused on discovering and developing innovative small molecules that drug traditionally undruggable targets, providing new paths to treat diseases. By using its proprietary chemoproteomic platform, IMTAC™, BridGene is able to screen small molecules against all proteins in live cells to discover drug candidates for high value and previously undruggable targets. For this purpose, BridGene takes advantage of its proprietary, diverse covalent library of tagged, drug-like small molecules. The ultimate goal is to enable breakthrough small-molecule drug discovery and to expand the mechanisms to treat diseases, with targets previously inaccessible to small molecules. BridGene is advancing a diversified pipeline of first-in-class drugs for targets in multiple disease areas. For more information, visit

SOURCE: BridGene Biosciences