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Osugacestat is a small-molecule gamma secretase (GS) inhibitor and pan-Notch antagonist with potential antineoplastic activity. It binds to the gamma secretase complex, blocking activation of Notch receptors, which may inhibit proliferation of tumor cells with an overactive Notch pathway. Osugacestat has been investigated primarily for cancers such as adenoid cystic carcinoma and triple negative breast cancer, especially in tumors driven by activating mutations in the NOTCH signaling pathway. The drug was originally developed by Bristol Myers Squibb and later by Ayala Pharmaceuticals, with clinical development reaching Phase II for certain indications[1][3][6].
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