Discovery of AZD2716: A Novel Secreted PhospholipaseA2 (sPLA2) Inhibitor for the Treatment of CoronaryArtery Disease

摘要

Expedited structure-based optimization of the initial fragment hit >1 led to the design of (R)->7 (AZD2716) a novel, potent secreted phospholipase A2 (sPLA2) inhibitor with excellent preclinical pharmacokinetic properties across species, clear in vivo efficacy, and minimized safety risk. Based on accumulated profiling data, (R)->7 was selected as a clinical candidate for the treatment of coronary artery disease.