Vividion Therapeutics and Roche Jointly Publish Landmark Nature Paper on Clinical-Stage Covalent Allosteric Inhibitor of Werner Helicase (WRN)

2024-04-25

临床1期

VVD-133214 (also known as RO7589831), a promising drug candidate for patients with MSI-high cancers, is currently being evaluated in a Roche-sponsored Phase 1 first-in-human trial SAN DIEGO--(BUSINESS WIRE)--Vividion Therapeutics, Inc., a biopharmaceutical company utilizing novel discovery technologies to unlock high-value, traditionally undruggable targets with precision therapeutics for devastating cancers and immune disorders, today announced a landmark publication in Nature. The publication, “Chemoproteomic Discovery of a Covalent Allosteric Inhibitor of WRN Helicase,” by Kristen Baltgalvis et al, published jointly with our partner Roche, speaks to the chemical proteomic-enabled discovery of a clinical-stage, covalent allosteric inhibitor of Werner helicase (WRN), VVD-133214 (RO7589831), and further confirms Vividion’s approach to discovering and developing novel therapeutics. “Vividion discovered covalent ligands targeting a novel allosteric pocket on WRN, a well- known but challenging therapeutic target in drug development. The discovery of this allosteric pocket, early ligands and the lead series were directly enabled by Vividion’s innovative approach to drug discovery, including our chemoproteomics platform and unique covalent fragment library,” said Matt Patricelli, Ph.D., Chief Scientific Officer of Vividion. WRN is a highly sought after synthetic lethal target for cancers with microsatellite instability (MSI), a genetic state resulting from mutations in DNA damage response pathway genes. MSI is most common in colorectal, endometrial and stomach cancers. The WRN molecule was identified under the collaboration agreement entered between Vividion and Roche in 2020. Roche is currently investigating VVD-133214, also known as RO7589831, in a Phase 1 clinical trial (NCT06004245). “It has been a privilege partnering with Vividion on this significant oncology target, harnessing their leading platform capabilities, and successfully progressing an exceptional molecule into clinical trials within three years from its inception,” said Chris Claiborne, Ph.D., Head, Small Molecule Research and Head of Cancer Cell Targeted Therapy, Roche pharma Research and Early Development (pRED). “The publication of Vividion’s allosteric WRN inhibitor WRN inhibitor in Nature and being one of the first to the clinic on such a challenging target, highlights the ability of Vividion’s covalent chemoproteomic platform to identify and advance druggable vulnerabilities on historically challenging targets,” said Ben Cravatt, Ph.D., Scientific Founder of Vividion. About Vividion Vividion Therapeutics, Inc., a wholly owned and independently operated subsidiary of Bayer AG acquired in August 2021, is a biopharmaceutical company utilizing novel discovery technologies to unlock high value, traditionally undruggable targets with precision therapeutics for devastating cancers and immune disorders. The company’s platform has enabled it to identify hundreds of previously unknown functional pockets on well-validated protein targets implicated in a wide range of diseases, while simultaneously identifying compounds from its proprietary covalent chemistry library that interact in a highly selective manner with those pockets. The company is leveraging its proprietary chemoproteomic platform to advance a diversified pipeline of highly selective small molecule therapeutics targeting high value, traditionally undruggable targets in oncology and immunology. For more information, please visit . About Bayer Bayer is a global enterprise with core competencies in the life science fields of health care and nutrition. In line with its mission, “Health for all, Hunger for none,” the company’s products and services are designed to help people and the planet thrive by supporting efforts to master the major challenges presented by a growing and aging global population. Bayer is committed to driving sustainable development and generating a positive impact with its businesses. At the same time, the Group aims to increase its earning power and create value through innovation and growth. The Bayer brand stands for trust, reliability and quality throughout the world. In fiscal 2023, the Group employed around 100,000 people and had sales of 47.6 billion euros. R&D expenses before special items amounted to 5.8 billion euros. For more information, go to . Find more information at Follow us on Facebook: Follow us on Twitter: @BayerPharma