Metoprolol

Cardiovascular diseases are chronic diseases with high incidence worldwide. As the cornerstone drugs for the treatment of hypertension, coronary heart disease and other diseases, β-blockers have been used in clinical practice for decades. Metoprolol is a highly selective β1-adrenergic receptor blocker. By blocking cardiac β1 receptors, it reduces myocardial contractility, slows heart rate and decreases cardiac output, thus exerting the effects of lowering blood pressure, resisting myocardial ischemia and improving cardiac function. It is mainly used clinically to treat hypertension, angina pectoris, myocardial infarction, hypertrophic cardiomyopathy, aortic dissection, arrhythmia, hyperthyroidism and other diseases. It is also one of the core drugs for the long-term management of patients with chronic heart failure. Its applicable population covers adult patients with hypertension, coronary heart disease and chronic heart failure, and the clinical demand is very large.

At present, the global market size of metoprolol has exceeded 3 billion US dollars, and the domestic market size has also exceeded 5 billion yuan. In recent years, with the continuous rise in the prevalence of cardiovascular diseases, the market has maintained a compound annual growth rate of about 4%. In terms of the competitive landscape, the original research products still occupy the main share of the mid-to-high-end market. Dozens of domestic generic drug enterprises have been approved for production. Among them, the oral conventional-release dosage forms have been included in the national centralized volume-based procurement, and the winning bid price has dropped by more than 90% compared with the original research products, which has greatly improved the accessibility of the drug and also driven the steady growth of the demand for upstream active pharmaceutical ingredients.

The original research enterprise of metoprolol is AstraZeneca, with the trade name of Betaloc. The core compound patent expired in the 1990s, and the domestic core preparation patent also expired in 2021. At present, the mainstream marketed dosage forms include metoprolol tartrate conventional tablets (25mg, 50mg, 100mg) and metoprolol succinate sustained-release tablets (47.5mg, 95mg). Both types of dosage forms have been included in the *Catalogue of Reference Preparations of Chemical Drugs* of China and the FDA Reference Preparation Catalogue. In terms of domestic API registration, more than 20 enterprises have obtained A status for their metoprolol APIs through CDE registration, and more than 30 domestic enterprises have been approved for marketing of the corresponding oral preparations, which fully meets the clinical medication demand. (Data as of September 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of metoprolol impurity reference standards. Most of the products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. They fully comply with the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, and can fully meet the demand for impurity reference substances in the process of API R&D, quality research and production.