pf-06282999

Description: PF-06282999 is a novel, potent and selective myeloperoxidase (MPO) inhibitor with the potential for the treatment of cardiovascular diseases. Robust inhibition of plasma MPO activity was demonstrated with PF-06282999 upon oral administration to lipopolysaccharide-treated cynomolgus monkeys. On the basis of its pharmacological and pharmacokinetic profile, PF-06282999 has been advanced to first-in-human pharmacokinetic and safety studies. Myeloperoxidase (MPO) is a heme peroxidase that catalyzes the production of hypochlorous acid. Clinical evidence suggests a causal role for MPO in various autoimmune and inflammatory disorders including vasculitis and cardiovascular and Parkinson's diseases, implying that MPO inhibitors may represent a therapeutic treatment option.

References: J Med Chem. 2015 Nov 12; 58(21):8513-28.