Aldosterone synthase (CYP11B2)

Class

Aldosterone synthase inhibitor

Aldosterone synthase, also known as CYP11B2, is an enzyme found in the outer layer of the adrenal gland (the zona glomerulosa) that produces aldosterone, a hormone that signals the kidney to retain sodium and water while excreting potassium. This process helps regulate blood volume and blood pressure. When aldosterone is produced in excess, either from adrenal tumors or from more diffuse overactivity of the adrenal gland, it drives persistent high blood pressure that often resists standard treatment, and it can independently promote scarring (fibrosis) of the heart and kidney. Inhibiting aldosterone synthase reduces aldosterone production at its source, offering an alternative to blocking the hormone's receptor. This mechanism is being explored mainly for treatment-resistant hypertension, primary aldosteronism, and conditions such as heart failure and chronic kidney disease where aldosterone-driven tissue damage contributes to disease progression. A central design challenge for drugs in this class is achieving selectivity for CYP11B2 over its close molecular relative, CYP11B1, which produces cortisol, the body's principal stress hormone, since unwanted inhibition of cortisol synthesis could cause its own health problems.