Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.
The mineralocorticoid receptor (MR) is a member of the nuclear receptor superfamily and is essential for controlling sodium transport in epithelial tissues such as the kidney and colon[2]. Apararenone is a novel non-steroidal MR antagonist in late-stage clinical trials in patients with heart failure, chronic kidney disease (CKD), hypertension and liver disease[3]. In patients with stage 2 diabetic nephropathy (DN), mean urine albumin to creatine ratio (UACR), as a percentage of baseline, decreased to 62.9%, 50.8%, and 46.5% in the 2.5 mg, 5 mg, and 10 mg apararenone groups, respectively, at week 24. UACR remission rates at week 24 were 0.0%, 7.8%, 29.0%, and 28.1% in the placebo and apararenone 2.5 mg, 5 mg, and 10 mg groups, respectively. Estimated glomerular filtration rate (eGFR) tended to decrease and serum potassium tended to increase[4].
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