Drug intelligence / Profile preview

osugacestat

Development stage
Phase 2
Lead developer
Ayala Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

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].

Other names
osugacestat
02

Targets

NOTCH (Neurogenic locus notch homolog protein 3)GSEC (Gamma-Secretase Complex)

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