Drug intelligence / Profile preview

BMS-262084

Development stage
Discontinued
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Parenteral
01

Overview

BMS-262084 is a small molecule, azetidinone-based irreversible inhibitor developed by Bristol Myers Squibb. It acts as a potent and selective dual inhibitor of coagulation Factor XIa (IC50 of 2.8 nM) and human tryptase (IC50 of 5 nM). Chemically, it is a 4-carboxy-2-azetidinone (beta-lactam) derivative. The compound was investigated for its antithrombotic effects in cardiovascular diseases and thrombosis, with potential for both oral and parenteral administration. Furthermore, its tryptase inhibitory activity led to research into its use for asthma, where it demonstrated efficacy in reducing allergen-induced bronchoconstriction and inflammatory cell infiltration in preclinical guinea pig models.

02

Targets

Factor XIa

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