Drug intelligence / Profile preview

bms-986141 + itraconazole

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

Overview

A combination product consisting of **BMS-986141**, an orally bioavailable small-molecule antagonist of protease-activated receptor 4 (PAR4), with **itraconazole**, an antifungal agent and strong inhibitor of cytochrome P450 3A4 (CYP3A4). BMS-986141 selectively inhibits PAR4-mediated platelet aggregation, resulting in antithrombotic effects with reduced bleeding risk compared to other antiplatelet agents. It demonstrated robust inhibition of PAR4-induced platelet aggregation, and its use is being explored for cardiovascular and thrombotic diseases[1][2][3][4][5]. The combination with itraconazole was specifically studied to assess the impact of CYP3A4 inhibition on the pharmacokinetics of BMS-986141; co-administration increases BMS-986141 exposure up to 8-fold and prolongs half-life 3-fold, due to inhibition of CYP3A4-mediated metabolism[3]. No brand or trade name is associated with this combination; it exists as an investigational interaction for drug-drug interaction assessment and pharmacokinetic studies.

Other names
bms-986141 + itraconazole
02

Targets

PAR4 (Protease-activated receptor 4)SMO (Smoothened)CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)

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