Drug intelligence / Profile preview

BMS-708163 + fluconazole

Development stage
Phase 1
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

BMS-708163 (avagacestat) is a potent, selective, and orally bioavailable small molecule inhibitor of γ-secretase. It was developed by Bristol Myers Squibb for the potential treatment of Alzheimer's disease. The drug works by inhibiting γ-secretase-mediated cleavage of amyloid precursor protein (APP), thereby reducing the production of amyloid β-peptides (Aβ40 and Aβ42), which are implicated in the pathogenesis of Alzheimer's disease. Avagacestat shows high selectivity for APP processing over Notch signaling, aiming to minimize side effects associated with Notch inhibition[6][8]. Fluconazole is a triazole antifungal agent used to treat various systemic and superficial fungal infections such as candidiasis and cryptococcal meningitis. It acts as a selective inhibitor of fungal cytochrome P450-dependent 14α-lanosterol demethylation, an essential step in ergosterol biosynthesis required for maintaining fungal cell membrane integrity[1][2][3]. Fluconazole is marketed under the brand name Diflucan.

Other names
fluconazoleavagacestat
02

Targets

GSEC (Gamma-Secretase Complex)CYP51A1 (Sterol 14α-demethylase)

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