Mineralocorticoid receptor antagonists: a patent evaluation of US20150284376A1

ABSTRACT

Introduction: Recent clinical studies showed that mineralocorticoid receptor antagonists are able to markedly reduce the overall and cardiovascular mortality in patients with left ventricular systolic dysfunction and mild or severe symptoms of chronic heart failure (HF). Beyond cardiac diseases, new indications of MRAs increase exponentially, especially in patients with impaired renal function. Most of the developed mineralocorticoid receptor antagonists are now non-steroidal. Identifying so-called “kidney friendly” compounds (i.e. with less renal potassium sparing properties as compared to classical steroidal MRA and therefore better safety profile in at-risk patients) would represent a clear breakthrough and many companies have developed intense patent activities in the field.

Area covered: The present article provides an analysis of US20150284376 patent application which discloses non-steroidal compounds.

Expert opinion: Of US20150284376 discloses a new class of MRA for which it is too early for determining the relevance in the absence of preclinical studies.

KEYWORDS:

• Mineralocorticoid receptor antagonist
• aldosterone
• non-steroidal compounds

Article highlights

• Addition of mineralocorticoid receptor antagonists (MRAs) to standard care reduced the overall and cardiovascular mortality in patients suffering from heart failure.

• Beyond cardiac diseases, new indications of MRAs have been described including vascular, metabolic, renal, ocular, or skin diseases.

• At least 5 pharmaceutical companies have non-steroidal MRAs in clinical development.

• Finerenone assigned to Bayer is most advanced compound investigated in clinical trials.

• US20150284376 patent application discloses a new class of non-steroidal compounds for which it is too early to determine their relevance in the absence of preclinical studies.

This box summarizes key points contained in the article.

Declaration of interest

The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Additional information

Funding

F Jaisser has received a grant sponsorship from Bayer. This paper was funded by the Centre de Recherche Industrielle et Technique (1138-FJ-2015) and the Institut National de la Santé et de la Recherche Médicale (1138-Team1-2016).