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varegacestat
- Development stage
- Phase 3
- Lead developer
- Immunome
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Varegacestat is an orally bioavailable small molecule that acts as a gamma secretase and pan-Notch inhibitor, with potential antineoplastic activity. By binding to gamma secretase, varegacestat blocks the proteolytic cleavage and release of the Notch intracellular domain (NICD), preventing its translocation to the nucleus and subsequent activation of Notch-regulated genes. This inhibition leads to apoptosis and reduced proliferation in tumor cells that overexpress Notch signaling pathways. Varegacestat has been investigated primarily for cancer indications, including fibroma and solid tumors, with orphan drug designation for solid tumors. The drug was originally developed by Bristol-Myers Squibb and is currently being developed by Ayala Pharmaceuticals, Novartis, and Immunome[1][5].
- Other names
- Notch inhibitor 1
02
Targets
GSEC (Gamma-Secretase Complex)NOTCH (Neurogenic locus notch homolog protein 3)
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