Exelixis and Insilico Medicine Enter into Exclusive Global License Agreement for ISM3091, a Potentially Best-in-Class USP1 Inhibitor - Seite 2

USP1 facilitates DNA damage repair by removing ubiquitin from multiple substrates including proteins that stabilize the replication fork. A small molecule discovered using Insilico Medicine’s generative AI platform with extensive multiparameter optimization capabilities, ISM3091 was designed to inhibit the activity of USP1. In preclinical experiments, ISM3091 was found to be potently efficacious against multiple tumor cell lines and in vivo models with BRCA mutations, as well as in homologous recombination DNA repair (HRR)-proficient models, both as a single agent and in combination with PARP inhibitors. It is also well tolerated in different species with a high margin of safety. Insilico disclosed select data in a poster presentation at the American Association for Cancer Research Annual Meeting in April 2023. On April 17, 2023, the FDA cleared the initial IND for ISM3091 for the treatment of patients with solid tumors.

About Insilico Medicine

Insilico Medicine, a global clinical stage biotechnology company powered by generative AI, is connecting biology, chemistry, and clinical trials analysis using next-generation AI systems. The company has developed AI platforms that utilize deep generative models, reinforcement learning, transformers, and other modern machine learning techniques for novel target discovery and the generation of novel molecular structures with desired properties. Insilico Medicine is developing breakthrough solutions to discover and develop innovative drugs for cancer, fibrosis, immunity, central nervous system diseases, infectious diseases, autoimmune diseases, and aging-related diseases. www.insilico.com

About Exelixis

Exelixis is a globally ambitious oncology company innovating next-generation medicines and regimens at the forefront of cancer care. Powered by bi-coastal centers of discovery and development excellence, we are rapidly evolving our product portfolio to target an expanding range of tumor types and indications with our clinically differentiated pipeline of small molecules, antibody-drug conjugates and other biotherapeutics. This comprehensive approach harnesses decades of robust investment in our science and partnerships to advance our investigational programs and extend the impact of our flagship commercial product, CABOMETYX (cabozantinib). Exelixis is driven by a bold scientific pursuit to create transformational treatments that give more patients hope for the future. For information about the company and its mission to help cancer patients recover stronger and live longer, visit www.exelixis.com, follow @ExelixisInc on X, like Exelixis, Inc. on Facebook and follow Exelixis on LinkedIn.