molecules of the month


oral nonsteroidal MR antagonist

Ph. II candidate in DN and NASH (discontinued)

previous literature and hypothesis-driven opt.

J. Med. Chem.

Mitsubishi Tanabe Pharma Corporation, Yokohama, JP

Apararenone Chemical Structure oral nonsteroidal MR antagonist - Mitsubishi Tanabe Pharma Corporation, Yokohama, JP
5 mins read

Context. Apararenone (Mitsubishi Tanabe) is an oral nonsteroidal mineralocorticoid receptor (MR) antagonist. Agents with the ability to modulate the nuclear receptor MR have been pursued for at least 80 years. Spironolactone, the first-in-class MR (steroidal) antagonist, was approved in 1960, with the more selective eplerenone (also steroidal) being approved in 2002, 42 years later. Since steroidal MR antagonists (MRAs) are known to distribute primarily to the kidneys and have been associated with an increased risk of hyperkalemia, attention has shifted to nonsteroidal MR antagonists. Research efforts in this regard culminated in the approval of the first nonsteroidal MR antagonist finerenone (Kerendia) for CKD associated with type 2 diabetes in 2021. Another agent, Sankyo’s esaxerenone, is approved in Japan for hypertension…

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