Osilodrostat

Osilodrostat is an inhibitor of aldosterone synthase (IC₅₀ = 0.7 nM for the recombinant human enzyme).¹ It is selective for human aldosterone synthase over rat aldosterone synthase (IC₅₀ = 160 nM). Osilodrostat inhibits increases in plasma aldosterone levels induced by angiotensin II or adrenocorticotropic hormone (ACTH) in rats (ED₅₀s = 0.6 and 1.1 mg/kg, respectively). It reduces mean arterial pressure and prolongs survival in rats expressing human renin and angiotensinogen, a double-transgenic model of angiotensin II-dependent hypertension, in a dose-dependent manner. Formulations containing osilodrostat have been used in the treatment of Cushing’s syndrome.

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1. Ménard, J., Rigel, D.F., Watson, C., et al. Aldosterone synthase inhibition: Cardiorenal protection in animal disease models and translation of hormonal effects to human subjects. J. Transl. Med. 12, 340 (2014).