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In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure.

Gargalovic P, Wong P, Onorato J, Finlay H, Wang T, Yan M, Crain E, St-Onge S, Héroux M, Bouvier M, Xu C, Chen XQ, Generaux C, Lawrence M, Wexler R, Gordon D

Bristol Myers Squibb, Drug Discovery, Princeton, NJ (P.G., P.W., J.O., H.F., T.W., M.Y., E.C., C.X., X.-Q.C., C.G., M.L., R.W., D.G.).

New heart failure therapies that safely augment cardiac contractility and output are needed. Previous apelin peptide studies have highlighted the potential for APJ (apelin receptor) agonism to enhance cardiac function in heart failure. However, apelin's short half-life limits its therapeutic utility. Here, we describe the preclinical characterization of a novel, orally bioavailable APJ agonist, BMS-986224.

Circ Heart Fail 2021;14(3):e007351.

Pubmed ID: 33663236

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