The G protein-coupled receptor, APJ (APLNR), and its endogenous peptidic ligand (apelin) have been implicated in mediating multiple beneficial effects on cardiovascular function. Efforts to employ apelin peptides therapeutically have been hindered by their very short half-lives. This presentation will describe the small molecule drug discovery process from optimizing a small molecule high-throughput screening hit through to the identification of the APJ agonist AMG 986. A phase 1 clinical trial is currently underway evaluating AMG 986 in healthy volunteers and heart failure patients.

Discovery of AMG986, a potent, selective and orally bioavailable APJ agonist for the treatment of heart disease

256th National Meeting (2018)

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