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Exelixis and Insilico Medicine Enter into Exclusive Global License Agreement for ISM3091, a Potentially Best-in-Class USP1 Inhibitor
— ISM3091 is a highly selective, orally bioavailable small molecule inhibitor of USP1 identified through Insilico Medicine’s artificial intelligence (AI)

About this update from Exelixis, Inc.
[{"type":"text","content":"\n— ISM3091 is a highly selective, orally bioavailable small molecule inhibitor of USP1 identified through Insilico Medicine’s artificial intelligence (AI) platform, with potent activity in BRCA-mutated tumor models —\n\n\n— In April 2023, the U.S. Food and Drug Administration (FDA) cleared Insilico’s Investigational New Drug application (IND) for ISM3091 in patients with solid tumors —\n\n\n ALAMEDA, Calif. & NEW YORK--(BUSINESS WIRE)--\nExelixis, Inc. (Nasdaq: EXEL) and Insilico Medicine (“Insilico”) today announced that the companies have entered into an exclusive license agreement granting Exelixis global rights to develop and commercialize ISM3091, a potentially best-in-class small molecule inhibitor of USP1, which has emerged as a synthetic lethal target in the context of BRCA-mutated tumors.\n\nThis press release features multimedia. View the full release here: https://www.businesswire.com/news/home/20230912041846/en/\nUnder the terms of the agreement, Insilico granted Exelixis an exclusive, worldwide license to develop and commercialize ISM3091, and other USP1-targeting compounds, in exchange for an upfront payment to Insilico of $80 million anticipated in the third quarter 2023. Insilico is also eligible to receive future development, commercial, and sales-based milestone payments, as well as tiered royalties on net sales.\n\n\n“ISM3091 represents a potentially best-in-class approach to inhibiting USP1, an important oncology target with broad applicability in BRCA-mutant tumors,” said Dana Aftab, Ph.D., Executive Vice President, Discovery and Translational Research and Chief Scientific Officer, Exelixis. “We believe preclinical data on ISM3091’s potent anti-tumor activity, tolerability, and pharmacokinetics set the compound apart from competing USP1 inhibitors and make it an important addition to Exelixis’ growing clinical-stage pipeline. Following the FDA’s clearance of Insilico’s IND earlier this spring, we’re looking forward to accelerating phase 1 trial enrollment.”\n\n\n“ISM3091 is the third clinical-stage program made possible by Chemistry42, Insilico Medicine’s generative AI platform for small molecule drug discovery,” said Alex Zhavoronkov, Ph.D., founder and CEO of Insilico Medicine. “The compound’s novel structure, anti-tumor activity, and excellent drug-like properties give it significant potential as a diffe...