Baxdrostat(CAS:1428652-17-8)

Baxdrostat, CAS number 1428652-17-8, is the first first-in-class aldosterone synthase inhibitor API owned by AstraZeneca, officially approved by FDA in 2026. It fills the long-standing therapeutic gap for resistant hypertension and owns extreme scarcity value in global new drug R&D and high-end generic drug industries, listed as core fourth-line combination therapeutic raw material in hypertension guidelines of multiple countries. It appears as white crystalline powder with strictly controlled chiral purity, and limits of related substances, heavy metals and residual solvents fully comply with USP and EP pharmacopoeia standards. Featuring stable chemical structure and mild storage requirements, it supports mass industrial production of 1mg and 2mg oral film-coated tablets, and meets diversified purchasing demands including new drug application, pharmacological research and custom synthesis.

In terms of core pharmacological mechanism, excessive aldosterone secretion serves as the key pathogenic pathway of resistant hypertension in obese, salt-sensitive, elderly and diabetic nephropathy patients. Traditional RAAS inhibitors, calcium channel blockers and beta blockers fail to suppress aldosterone production fundamentally, while spironolactone and eplerenone merely compete for mineralocorticoid receptors without lowering total hormone volume, accompanied by risks of sex hormone-related side effects. Baxdrostat delivers fully differentiated efficacy: it highly selectively binds CYP11B2, the rate-limiting enzyme of adrenal aldosterone synthesis, directly blocking the final step of aldosterone generation, reducing plasma aldosterone concentration by up to 70% after administration. It barely inhibits cortisol synthetase CYP11B1, so basic human glucocorticoid secretion remains intact, completely avoiding adverse reactions such as adrenal hypofunction and endocrine disorders. Reduced aldosterone significantly cuts renal reabsorption of sodium and chloride to excrete excess water and lower blood volume; meanwhile it suppresses vascular smooth muscle proliferation, delays arterial fibrosis and reverses myocardial remodeling, achieving triple target organ protection for blood pressure reduction, renal protection and myocardial preservation. Baxdrostat owns outstanding pharmacokinetic profiles: peak plasma concentration reaches within 2–4 hours after oral intake, half-life ranges from 26 to 30 hours, once-daily dosing maintains stable 24-hour blood pressure control with minimal drug-drug interaction risks, compatible with nearly all mainstream antihypertensive agents.

Clinically, Baxdrostat’s primary indication is adult resistant hypertension, defined as patients failing blood pressure targets after standardized full-dose triple therapy including diuretics. Landmark Phase 3 BaxHTN and BrigHTN trials verified that adding Baxdrostat to original triple regimens generates significant systolic blood pressure reduction within 4 weeks, with placebo-adjusted drop up to 14 mmHg, delivering superior efficacy for hypertensive patients complicated with diabetes, chronic kidney disease and obesity. Besides hypertension, clinical trials are ongoing for primary aldosteronism, CKD combined hypertension and heart failure prevention for high-risk populations to expand cardiorenal comorbidity treatment scenarios. Different from endothelin receptor antagonists limited to pulmonary arterial hypertension and aprocitentan solely for resistant hypertension, Baxdrostat targets aldosterone synthesis at source with wider applicable population and excellent clinical combination compatibility.

Regarding industrial production and clinical safety, Baxdrostat adopts patent-optimized full synthetic technology with uniform batch purity and ultra-low impurities, enabling controllable mass production costs and sustainable bulk supply for pharmaceutical factories. Standard clinical daily doses are 1mg and 2mg with favorable overall tolerance; only mild hyperkalemia occurs in a small number of patients, which can be well managed via regular blood potassium and renal function monitoring, without severe hepatotoxicity or hormonal disturbance. As a landmark new-mechanism blockbuster antihypertensive API developed in the past decade, Baxdrostat breaks through the treatment bottleneck of traditional hypotensive drugs. With continuously expanding global patient base of resistant hypertension, it holds irreplaceable competitiveness in innovative preparations, generic drug export and cardiovascular basic research, promising broad and long-term market development prospects in the global pharmaceutical industry.