molecules of the month

APJ compound 14

oral apelin receptor GPCR agonist

completed Ph. I for heart failure, discontinued

from cell-based HTS and opt.

J. Med. Chem., Mar. 19, 2021

Bristol Myers Squibb, Princeton, NJ

1 min read

The Bristol Myers Squibb apelin receptor (APJ) GPCR agonist (“compound 14”) is a clinical candidate for heart failure which completed a Ph. I study. Endogenous pyroglutamated apelin-13 peptide has been shown to be beneficial in cardiovascular disease models, and this small molecule agonist was intended to treat heart failure by mimicking apelin-13 peptide without the stability and delivery issues of a peptide approach. This drug candidate has impressive PK in preclinical species despite its structure containing several groups that can be difficult to deal with, including a phenol, pyridine, several ethers, a pyridine, and two benzylic positions. In a rat model, compound 14 treatment results in an increase in cardiac output without significant increase in heart rate in contrast to…

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