aldosterone synthase inhibitors

Aldosterone synthase inhibitors (ASIs) are a novel pharmacological class of small molecule therapeutics designed to treat hypertension and other conditions characterized by aldosterone excess. These agents work by selectively inhibiting the enzyme CYP11B2 (aldosterone synthase), which catalyzes the final steps of aldosterone biosynthesis in the adrenal cortex, including the conversion of 11-deoxycorticosterone to aldosterone. This mechanism is distinct from mineralocorticoid receptor antagonists (MRAs), which block the action of aldosterone at the receptor level; ASIs instead reduce the systemic production of the hormone itself. Clinical development has primarily focused on resistant and uncontrolled hypertension, where candidates such as baxdrostat, lorundrostat, and vicadrostat have demonstrated significant efficacy in reducing blood pressure. However, the class requires careful monitoring for hyperkalemia and potential off-target inhibition of CYP11B1, which could impact cortisol synthesis.

Other names

aldosterone synthase inhibitorsASIsCYP11B2 inhibitorsCYP-11B2 inhibitorsCYP 11B2 inhibitors