Drug intelligence / Profile preview

BMS-986177 + itraconazole

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

Overview

BMS-986177 + itraconazole is a combination of two drugs: **BMS-986177** (also known as milvexian) and **itraconazole**. BMS-986177 is an orally administered, investigational small molecule anticoagulant that selectively inhibits **Factor XIa**, thereby aiming to reduce thrombus formation without significantly impacting hemostasis. It is being developed to prevent thromboembolic events, particularly ischemic stroke, acute coronary syndromes, and atrial fibrillation, with clinical studies showing a favorable safety profile and a reduction in recurrent symptomatic ischemic strokes. Itraconazole is a well-established oral triazole antifungal agent widely used to treat systemic and superficial fungal infections; it inhibits the synthesis of ergosterol by blocking cytochrome P450-dependent 14α-demethylase in fungi. The specific rationale for the BMS-986177 + itraconazole combination is likely to assess drug–drug interactions, particularly the impact of itraconazole (a strong CYP3A4 inhibitor) on the pharmacokinetics of BMS-986177.

Other names
milvexian + itraconazole
02

Targets

CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)ABCG2 (Breast cancer resistance protein)Factor XIaABCB1 (P-glycoprotein)

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