HRS-2430

HRS-2430 is a potent and highly selective small molecule inhibitor of aldosterone synthase (Cytochrome P450 11B2; CYP11B2), currently under development by Jiangsu Hengrui Pharmaceuticals. Aldosterone synthase is the terminal enzyme in the biosynthetic pathway of aldosterone, a mineralocorticoid hormone that regulates blood pressure and electrolyte balance. Excessive aldosterone levels are implicated in the pathogenesis of hypertension, primary aldosteronism, and progressive cardiovascular and renal diseases. HRS-2430 is designed to lower plasma aldosterone levels while maintaining high selectivity over CYP11B1 (11β-hydroxylase), an enzyme sharing 93% sequence identity with CYP11B2 that is essential for cortisol synthesis. By avoiding CYP11B1 inhibition, the drug aims to treat mineralocorticoid-related conditions without inducing adrenal insufficiency. As of 2024, HRS-2430 is undergoing Phase 1 clinical trials in healthy volunteers to evaluate its safety, tolerability, and pharmacokinetic profile.