Drug intelligence / Profile preview

E2609 + itraconazole

Development stage
Phase 1
Lead developer
Eisai
Modality
Small Molecules
Administration
Oral
01

Overview

E2609 + itraconazole is a combination of two pharmaceutical agents investigated for potential drug-drug interactions. E2609 is an experimental small molecule developed as a BACE1 inhibitor for Alzheimer’s disease, while itraconazole is a triazole antifungal agent approved for treatment of fungal infections. The purpose of combining these drugs in clinical studies is to evaluate possible changes in pharmacokinetics, efficacy, or safety when both drugs are administered together. Itraconazole is a potent CYP3A4 inhibitor and can alter the plasma concentrations and metabolism of co-administered drugs, potentially impacting efficacy or causing adverse effects. E2609’s mechanism involves inhibition of beta-site amyloid precursor protein-cleaving enzyme 1 (BACE1), thereby reducing amyloid-beta production, whereas itraconazole inhibits cytochrome P450-dependent 14α-demethylase of lanosterol, blocking ergosterol synthesis and disrupting fungal cell membrane integrity[1][3][4][5][6].

02

Targets

BACE1 (Beta-site APP-cleaving enzyme 1)CYP51A1 (Sterol 14α-demethylase)

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