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Belharra Therapeutics Debuts With $130 Million in Funding

–Next-generation chemoproteomics company launched by Versant Ventures’ Inception Discovery Engine with ability to target any binding site, on any protein, in any cell type–

–Emerges from stealth with a $50 million Series A financing and multi-year collaboration with Genentech providing $80 million up front–

SAN MATEO, Calif. & SAN DIEGO–(BUSINESS WIRE)–Belharra Therapeutics, Inc. today emerged from stealth mode with a novel photoaffinity-based chemoproteomics platform capable of identifying non-covalent, small molecule drug candidates for any protein. The company has secured $130 million in capital, including $50 million in Series A financing from founding investor Versant Ventures and a multi-year collaboration with Genentech, a member of the Roche Group, that will provide $80 million in upfront capital, also announced today. Belharra is the most recent company to emerge from Versant’s Inception Discovery Engine.

Belharra’s integrated chemoproteomic-based drug discovery engine addresses the limitations of traditional screening approaches through a proprietary library of photoaffinity-based chemical probes that explore protein-ligand interactions in the native environment of the cell. The platform utilizes photoaffinity-based labeling to “trap” these unique non-covalent protein-ligand interactions. Coupled with its novel chemoproteomics platform and informatics capabilities, Belharra’s platform identifies probe-protein interactions on a global scale, revealing novel druggable pockets across a complete range of mechanisms, protein classes and cell types.

While first-generation platforms demonstrated the power of chemoproteomics to illuminate new chemical space, they required specific nucleophilic amino acid residues, such as cysteine, be present on a protein of interest and used probe libraries composed exclusively of electrophilic drug fragments. These are limiting because only a fraction of drug targets have ligandable cysteines and irreversible ligands often have complex development paths. The Belharra photoaffinity platform is not reliant on any specific amino acid for labeling, enabling profiling of the entire proteome. Photochemistry is used to identify probe-protein interactions and since the underlying mode of the Belharra platform’s ligand binding is non-covalent, it provides a more validated development path for drug candidates.

Next-generation chemoproteomics platform

Belharra’s uniquely differentiated platform builds on a legacy of chemoproteomic-based drug discovery to identify functional and actionable non-covalent, small molecule drug candidates for any binding site, on any protein, in any conformational state, in any cell type. The platform enables screens to be run in a whole cell context, which enables the small molecule library to interact with proteins in their native conformations, including protein complexes, which are virtually impossible to recapitulate in traditional biochemical screens. This creates the potential to identify next-generation therapeutics for previously difficult-to-treat conditions.

“We’ve expanded the power of traditional chemoproteomic screening approaches and integrated them into a single drug discovery engine that enables, for the first time, the ability to target the full range of protein classes and targets,” said Jeff Jonker, CEO of Belharra. “Our platform enables us to rapidly rescreen all of the previously ‘undruggable’ protein targets to identify actionable non-covalent drug-like ligands for functional binding pockets.”

The Belharra platform originated in the laboratories of Christopher G. Parker, Ph.D., John Teijaro, Ph.D., and Ben Cravatt, Ph.D., at Scripps Research. There, Drs. Parker and Cravatt developed a novel photoaffinity-based chemoproteomics technology to enable screening for small molecules that bind proteins in their native context and focused it on immunology targets leveraging the expertise of Dr. Teijaro. Stuart Schreiber of the Broad Institute joined as a co-founder to provide input on using the platform for innovative drug discovery and broad therapeutic application.

During Belharra’s formative stage, the team at Scripps worked alongside Belharra’s scientists and scientists at Versant’s San Diego-based discovery engine, Inception Therapeutics, to industrialize the technology and build a proprietary library of small molecule photoaffinity probes with superior drug-like properties. Based on targeted and phenotypic screens run by Scripps and Belharra, Belharra expects to advance internal discovery candidates for both Oncology and Immunology indications in 2023.

“Having been involved in a number of important companies in the chemical proteomics field, we have high conviction that Belharra represents a new wave of innovation in the space,” said Tom Woiwode, Ph.D., Managing Director at Versant and a Belharra board member. “We are very excited to be working with Jeff, Gary and the company’s world-class scientific founders to advance medicines for previously intractable targets and diseases.”

Leadership team and scientific founders

Belharra is led by experienced executives bolstered by scientific founders with deep expertise in chemoproteomics, chemical biology and drug discovery.

About Belharra Therapeutics

Belharra Therapeutics, Inc. is a privately held drug discovery company pioneering a novel photoaffinity-based chemoproteomics platform to disrupt the drug discovery paradigm. Guided by a diverse team of biotech trailblazers, Belharra’s proprietary discovery engine is uniquely capable of identifying novel, non-covalent small molecule starting points for developing transformative medicines to address previously difficult-to-treat diseases and conditions. The company’s next generation chemoproteomics platform enables Belharra scientists to identify small molecule drug candidates for any binding site, on any protein, in any conformational state, in any cell type. Originating with Christopher G. Parker, Ph.D. and John Teijaro, Ph.D. at Scripps Research and pioneers in the field of chemical biology and serial biotech founders Benjamin Cravatt, Ph.D. at Scripps Research and Stuart Schreiber, Ph.D. at the Broad Institute of MIT and Harvard, the four co-founded Belharra Therapeutics in 2021 with a $50M Series A financing from Versant Ventures and incubation at Inception Therapeutics. Belharra is headquartered in the San Francisco Bay Area with its primary lab and offices in San Diego, California. To learn more, please visit www.belharratx.com.

About Versant Ventures

Versant Ventures is a leading healthcare venture capital firm committed to helping exceptional entrepreneurs build the next generation of great companies. The firm’s emphasis is on biotechnology companies that are discovering and developing novel therapeutics. With $4.2 billion under management and offices in the U.S., Canada and Europe, Versant has built a team with deep investment, operating and R&D expertise that enables a hands-on approach to company building. Since the firm’s founding in 1999, more than 85 Versant companies have achieved successful acquisitions or IPOs. For more information, please visit www.versantventures.com.

Contacts

Steve Edelson

415-801-8088

sedelson@versantventures.com

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