Eplerenone

Excessive activation of the renin-angiotensin-aldosterone system is one of the core driving factors for the progression of cardiovascular diseases such as hypertension and heart failure. As the terminal effector hormone of this pathway, long-term excessive secretion of aldosterone can lead to pathological injuries such as myocardial fibrosis and water and sodium retention. Eplerenone is the first selective aldosterone receptor antagonist. By specifically blocking the binding of aldosterone to mineralocorticoid receptors, it can significantly reduce target organ damage while lowering blood pressure. Compared with the traditional non-selective spironolactone, it greatly reduces the risk of endocrine adverse reactions such as gynecomastia in men and menstrual disorders. Clinically, it is mainly used for the treatment of adult hypertension and heart failure after acute myocardial infarction, especially for high-risk cardiovascular patients with comorbid diabetes and chronic kidney disease.

The global market size of eplerenone preparations was approximately USD 1.47 billion in 2023, and it is expected to rise to USD 1.70 billion in 2028 with a compound annual growth rate of 2.9%. The growth momentum mainly comes from the increasing prevalence of heart failure and the improvement of the penetration rate of chronic disease management for cardiovascular diseases. The domestic market is still dominated by generic drugs at present. As of 2024, more than 30 enterprises have obtained marketing approval for eplerenone tablets. In the 7th batch of national centralized drug procurement in 2022, the average price cut of this variety reached 68%, which directly promoted the substantial improvement of clinical accessibility, and the demand for upstream API has also entered a rapid expansion stage.

The original research enterprise of eplerenone is Pfizer, and the original trade name is Inspra. Its US compound patent expired in 2012, and its core Chinese patent expired in 2013. The main dosage form approved for the original drug is tablet, with specifications of 25mg and 50mg. The original product has been included in the FDA Reference Listed Drug Catalog and China's *Catalog of Reference Preparations for Chemical Drugs*. In terms of domestic API registration, as of September 2024, there are 12 eplerenone API registration numbers, among which 8 have obtained A status through the joint review and approval with preparations, and a number of domestic enterprises have obtained marketing approval for eplerenone tablets. (Data as of September 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of eplerenone impurity reference standards, which fully cover all kinds of impurities in the synthesis process and degradation pathways. All products meet the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA. Most products are in stock regularly. Spot orders paid before 16:00 can be shipped on the same day, which can effectively support the quality control requirements of the whole process of API research and development, quality research and production.