Keeping Heart Disease at BAY

Keeping Heart Disease at BAY

Author: Scott Williams

Chronic heart failure (CHF) is a disease that puts a heavy burden not only on patients, but also on healthcare resources. A validated treatment for CHF is blockade of the mineralocorticoid receptor (MR), but currently available MR antagonists suffer from two substantial drawbacks that limit their benefit in the clinic: lack of selectivity (in the case of spironolactone) and limited efficacy (in the case of eplerenone).

Lars Bärfacker and colleagues, Bayer Research Center in Wuppertal, Germany, revealed a novel series of non-steroidal MR antagonists based on a 1,4-dihydropyiridine scaffold. The authors provide a detailed structure–activity relationship as well as insight into the underlying pharmacophore model.

Their work has culminated in the identification of BAY 94-8862, a potent non-steroidal MR antagonist with outstanding selectivity. BAY 94-8862 is currently in phase II clinical trials for the treatment of CHF patients with renal impairment.


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