Drug intelligence / Profile preview

BMS-708163 + ketoconazole

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

BMS-708163 (also known as avagacestat) is a potent and selective small molecule inhibitor of γ-secretase, an enzyme involved in the cleavage of amyloid precursor protein (APP) to produce amyloid β-peptides implicated in the pathogenesis of Alzheimer's disease. It was developed by Bristol Myers Squibb and advanced to Phase II clinical trials for Alzheimer's disease. Avagacestat is designed to reduce the production of Aβ40 and Aβ42 peptides while sparing Notch signaling to minimize side effects[6][8]. Ketoconazole is an imidazole antifungal agent used primarily for serious systemic fungal infections when other treatments are not available or tolerated. It works by inhibiting ergosterol synthesis in fungi, disrupting cell membrane integrity[1][7]. Ketoconazole also has significant drug-drug interaction potential due to its inhibition of cytochrome P450 enzymes[2][7].

Brand names
Nizoral
Other names
ketoconazoleavagacestatBMS-708163BMS708163BMS 708163
02

Targets

GSEC (Gamma-Secretase Complex)CYP3A4 (Cytochrome P450 3A4)CYP51A1 (Sterol 14α-demethylase)

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