Drug intelligence / Profile preview

PF-06282999

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PF‑06282999 is a potent and selective small molecule inhibitor of myeloperoxidase (MPO), an enzyme highly expressed in neutrophils and implicated in the pathogenesis of cardiovascular diseases such as heart failure and acute coronary syndromes. The compound acts as a mechanism-based irreversible inactivator of MPO, with high selectivity over related enzymes like thyroid peroxidase and cytochrome P450 isoforms. It was developed by Pfizer for potential use in treating cardiovascular conditions, including acute coronary syndromes and possibly overweight/obesity. Preclinical studies demonstrated good oral bioavailability, moderate plasma protein binding, resistance to metabolic turnover, minimal cytochrome P450 inhibition, and renal excretion as the principal clearance route. Clinical development reached Phase 1 trials but was subsequently discontinued[1][5][7][8].

Other names
1435467-37-02-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide2-[6-(5-chloro-2-methoxyphenyl)-4-oxo-2-sulfanylidenepyrimidin-1-yl]acetamideUNII-YO3O4Q2NC8UNII-YO-3O4Q2NC8UNII-YO 3O4Q2NC8
02

Targets

MPO (Myeloperoxidase)

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