Steroidal and Non-steroidal Mineralocorticoid Receptor Antagonists in Cardiorenal Medicine

Rajiv Agarwal; Peter Kolkhof; George Bakris; Johann Bauersachs; Hermann Haller; Takashi Wada; Faiez Zannad


Eur Heart J. 2021;42(2):152-161. 

In This Article

Steroidal and Nonsteroidal Antagonism in the Steroid Hormone Receptor Family

Following ligand binding, steroid hormone receptors interact with cofactors, including transcriptional cofactors that affect gene transcription. Over 300 different cofactors interact with members of the nuclear hormone superfamily in a ligand- and cell type-specific way, resulting in different physiological responses.[55] These differences translate into clinically meaningful differences between steroidal and nonsteroidal ligands. Even within the class of non-steroidal antagonists, remarkably different effects on the androgen receptors have been observed, for example the nonsteroidal anti-androgen drugs enzalutamide and bicalutamide; in recent trials, these molecular pathways translate to meaningful differences in important patient outcomes.[56,57]