Excessive MR activation is implicated in the pathogenesis of cardiovascular disease. MR antagonists (MRA) are effective and key guideline-directed therapy in patients with heart failure (HF) with reduced ejection fraction. However, clinical adverse events due to hyperkalaemia and a decline in renal function significantly restricts the treatment. AZD9977 is a novel, non-steroidal selective MR modulator that, compared with MRA, displays a differentiated MR-binding pattern and cofactor recruitment profile, and exerts similar organ protective effects to eplerenone with minimal effects on urinary electrolyte handling.
Authors: A Whittaker, A Kragh, J Hartleib-Geschwindner, A Backlund, P Greasley, M Heijer, M Kjaer, R Unwin, L Wernevik, A Gabrielsen, H Ericsson
Keywords: non-steroidal, MRA, mineralocorticoid receptor modulator
DOI Number: 10.1093/eurheartj/ehz746.0654 Publication Year: 2019
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