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ISM6331 is a potent, non-covalent small molecule inhibitor with a novel scaffold that targets the transcriptional enhanced associate domain (TEAD) protein family. TEAD proteins are key regulators within the Hippo signaling pathway, which plays a critical role in tumor progression, metastasis, cancer metabolism, immunity, and drug resistance. Developed by Insilico Medicine using its AI-driven Chemistry42 platform for structure-based drug design, ISM6331 was selected from thousands of candidate molecules for its high potency, selectivity, favorable pharmacokinetic properties (including oral bioavailability), and safety profile. Preclinical studies have demonstrated broad anti-tumor activity across multiple cell lines and animal models at low doses. The compound has received FDA Orphan Drug Designation for mesothelioma and is currently being evaluated in Phase I clinical trials for mesothelioma and other solid tumors in both China and the United States[1][2][4][5][6][8][9].
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