Heart failure (HF) and related complications constitute a major health burden in developed countries. Despite considerable advances in recent decades, a clear unmet medical need for the development of novel treatment options for HF still exists. APJ receptor (APLNR) and its endogenous peptidic ligand (apelin) have been implicated as important modulators of cardiovascular function. However, the use of apelin peptides as therapeutic reagents is very challenging due to their short in vivo half-lives. Herein we report the discovery of a novel series of potent, selective, orally bioavailable small molecule agonists of APJ, exemplified by <b>AM-2995</b>, which improved cardiovascular function in rodent models.

Discovery of AM-2995, a potent, selective and orally bioavailable APJ agonist for the treatment of heart disease

256th National Meeting (2018)

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