Myocardial infarction (MI) is the most common cause of heart failure (HF) worldwide. Therapeutics, such as glucocorticoids and COX-2 inhibitors, that suppress inflammation have been unsuccessful at preventing progression to heart failure following an MI.  In contrast, our laboratories have shown that resolving inflammation by stimulation of the formyl peptide receptor 2 (FPR2) has the potential to promote myocardial healing, thereby preserving cardiac tissue and improving heart function. This disclosure will highlight the discovery, optimization and mechanistic studies of selective 4-phenylpyrrolidinone FPR2 agonists.  BMS-986235/LAR-1219 was nominated as a clinical candidate based on a compelling in vitro and in vivo profile, including efficacy in a mouse heart failure model. The molecule is currently in Phase 1 clinical development.<br/>

Discovery of clinical candidate, BMS-986235/LAR-1219: Selective FPR2 agonist for prevention of heart failure

2019 Fall National Meeting

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