Recently, the 12th Southwest Forum of Chronic Cardiovascular Disease was successfully held in Chongqing, China, which formally opened the national academic journey of Limeitong Eplerenone tablets. In August 2023, the new generation of selective aldosterone receptor antagonist, eplerenone tablets, which is the first generic drug in China, was approved for marketing by China’s National Medicines Agency (NMPA) in cooperation between China’s Grand Pharma and Nanjing Cavendish Bio-engineering Technology Co., Ltd.. It is the first of its kind in China, and its successful approval has made up for the gap of second-generation MRA drugs in China. According to the new registration classification, it is regarded as having passed the consistency evaluation and is suitable for the treatment of hypertension and can be used alone or in combination with other antihypertensive drugs.
Professor Luo Suxin from the First Affiliated Hospital of Chongqing Medical University was invited to give a lecture on “Application of New Generation Selective Aldosterone Receptor Antagonists in Cardiovascular Diseases”, which comprehensively analyzed the application and advantages of aldosterone receptor antagonists such as eplerenone in the clinic.
Heart failure is economically burdensome, combinations are a cornerstone and a new generation of MRA drugs is urgently needed in the clinic
Four-drug combinations are the cornerstone of the treatment of heart failure as the standard pharmacologic regimen for chronic heart failure, and MRAs are one of the commonly used classes of drugs. However, according to current real-world studies and grassroots drug use data, the utilization rate of GDMT drugs related to heart failure treatment, especially MRAs, is relatively low and the dose compliance rate is low. In China, there are fewer types of MRA drugs available for clinical use, and spironolactone is the only commonly used drug. A retrospective study found that: the adherence to spironolactone is low, and the MRA utilization rate of patients with heart failure showed a significant decrease after discharge from the hospital with an increase in the risk of the patients; this is mainly related to the spironolactone’s adverse effects such as hyperkalemia, gynecomastia, sexual dysfunction, vaginal bleeding and other adverse effects, and the clinic is in urgent need of a new generation of MRA drugs. There is an urgent need for a new generation of MRA drugs.
Eplerenone, a new generation aldosterone receptor antagonist, with higher patient compliance
MR overactivation leads to a series of complications that are ultimately life-threatening. Modern medicine has confirmed the aldosterone escape phenomenon in the treatment of hypertension with ACEI/ARB, and the combination of MRA can inhibit MR over-activation, thus benefiting cardiovascular diseases. As a new generation MRA, eplerenone is fully upgraded compared to spironolactone; it has higher receptor selectivity, fewer active metabolites, absorption not affected by food, and lower adverse effects such as hyperkalemia, gynecomastia, sexual dysfunction, and vaginal bleeding in women. Large sample studies have confirmed that long-term patient treatment with eplerenone reduces disease-related hospitalization rates and improves compliance.
Eplerenone significantly improves cardiac remodeling and reduces adverse events
From animal studies to real-world clinical studies, it has been confirmed that: eplerenone plays an important role in preventing fibrosis and inhibiting adverse cardiac remodeling; and reduces cardiovascular disease mortality and readmission rates in patients with heart failure, with lower cardiovascular and all-cause mortality rates compared to spironolactone.
Multiple guidelines/consensus unanimously recommend aldosterone receptor antagonists for cardiovascular disease treatment
Research on aldosterone receptor antagonists has been going on for more than 70 years; in 1953, aldosterone crystals were extracted from bovine adrenal glands for the first time; in 1957, the first aldosterone receptor antagonist, spironolactone, was launched on the market; in 1962, Laragh found that plasma aldosterone levels were elevated in patients with congestive heart failure; in 1981, the concept of aldosterone escape was proposed; and in 1999, the RALES study was released, which was a landmark study evaluating spironolactone in the treatment of heart failure. In 1999, the RALES study was released, which was a landmark study evaluating spironolactone in the treatment of heart failure, marking the formal entry of MRA treatment of heart failure into the era of evidence-based medicine; in 2003, EPHESUS, EMPHASIS-HF and other studies were released, which established the status of eplerenone in the treatment of heart failure.
Many domestic and foreign guidelines/consensus recommend aldosterone receptor antagonists for the treatment of various chronic heart failure and cardiovascular diseases, and they are indispensable drugs for the treatment of cardiovascular diseases. It is believed that with the listing of eplerenone in China, it will bring more choices, which will be really beneficial to the clinic and the patients.
The national academic tour of eplerenone has been officially opened, and we hope that with the popularization of our products, we can benefit more patients and contribute to the development of China’s cardiovascular disease diagnosis and treatment “Grand” power!
