30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development

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   Figure 1

   Important steroidal MRAs. Chemical structures of the most important 17-spirolactone derivatives, which were discovered and published between 1957 (beginning on top of the figure) and 1987 are shown. Launched drug compounds are highlighted by a white background. Open-ring potassium salt derivatives are highlighted by a light grey background (note that potassium canrenoate is both, a launched drug and a potassium salt derivative). Active metabolites are highlighted by a darker grey background. Arrows indicate either the generation of respective active metabolites from spironolactone (to different quantitative amounts, indicated by respective arrow sizes) or the equilibrium of the open-ring potassium salts with the respective lactone metabolite. Note the structural similarities of several stacked derivatives, e.g. mexrenone and eplerenone, or spironolactone and mespirenone.
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   Figure 2

   Novel non-steroidal MRAs in clinical development. Chemical structures of the three clinically most advanced non-steroidal MRAs apararenone, esaxerenone and finerenone are shown (from left to right).
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   Figure 3

   60 years of research and development on MRAs. The time bar highlights relevant publications on the discovery of MRAs or important clinical trial results with MRAs (RALES, EPHESUS, EMPHASIS-HF, ARTS, ARTS-DN and ARTS-HF) in a given year. Note that cloning of MR was at midway within the 60 years of R&D on MRAs.

• © 2017 The authors