Labetalol

Cardiovascular disease is the leading cause of death globally. Among cardiovascular diseases, the prevalence of hypertension continues to rise, and the medication options for some populations with refractory hypertension and gestational hypertension have been limited for a long time. As an antihypertensive drug with dual α-receptor and β-receptor blocking effects, labetalol can selectively block α1 receptors to dilate peripheral blood vessels and reduce peripheral resistance, while non-selectively blocking β receptors to inhibit sympathetic nerve excitation and reduce cardiac output, without causing reflex tachycardia. It is currently one of the few clinically available antihypertensive drugs that can be safely used for gestational hypertension, and can also be used for patients with pheochromocytoma and angina pectoris complicated with hypertension. Its applicable population covers patients with common hypertension, pregnant women, and people requiring perioperative blood pressure control.

At present, the global market size of antihypertensive drugs has exceeded 55 billion US dollars, among which α/β receptor blockers account for about 8% of the overall antihypertensive drug market. As a core basic drug in this category, labetalol has maintained a market growth rate of 4.7% in recent years. In terms of the domestic market, the annual sales of labetalol in public medical institutions exceed 1.2 billion yuan. After the implementation of centralized drug procurement, the market penetration rate of generic preparations has increased to 78%, and the demand for APIs has grown steadily accordingly. At present, the domestic supply of labetalol API is dominated by local enterprises, and the top 3 enterprises account for more than 65% of the total market share.

The original research enterprise of labetalol is GlaxoSmithKline, with the original brand name Trandate. The core compound patent expired globally in 1998, and there is no core patent restriction at present. The main dosage forms approved for the original drug include tablets (100mg, 200mg, 300mg) and injections (5mg/mL). The original tablets have been included in the FDA Reference Listed Drug Catalog. The original preparation is not imported into China, and the reference preparation is included in the *Catalog of Reference Preparations for Chemical Drugs (9th Batch)*, with domestically marketed generic drugs selected as the reference. Up to now, 14 domestic enterprises have obtained A status for their labetalol API through CDE registration, and the registration applications of another 3 enterprises are under the review stage. The domestically approved labetalol preparations include labetalol hydrochloride tablets and labetalol hydrochloride for injection, with a total of more than 40 approval numbers. (Data as of June 2025, please refer to the official CDE website for the latest information)

CATO provides a full set of impurity reference standards for labetalol API, covering all research dimensions such as process impurities and degradation impurities. All products meet the compliance requirements of multiple regulations including the Chinese Pharmacopoeia and FDA. Most products are in stock, and in-stock products ordered before 16:00 can be shipped on the same day, which can effectively support the needs of pharmaceutical enterprises in API R&D, quality research and daily production quality control.