Phentolamine

As a commonly used α-adrenoceptor blocker in clinical practice, phentolamine exerts the effects of dilating blood vessels, reducing peripheral resistance and exciting myocardium by non-selectively blocking α1 and α2 receptors before and after synapses, and indirectly promoting the release of catecholamines at the same time. In clinical practice, in addition to being used for the diagnosis of pheochromocytoma and the control of hypertensive episodes caused by it, it is also widely used in the treatment of left heart failure and peripheral vasospastic diseases, and can also assist in counteracting local tissue necrosis caused by extravasation of norepinephrine. The applicable population covers patients of different ages in multiple departments such as cardiovascular, endocrinology and surgery.

At present, the global market size of phentolamine is stable at around USD 120 million, with a compound annual growth rate of approximately 3.2%. The growth driver mainly comes from the increasing demand for vasoactive drugs in primary medical scenarios. The domestic market is currently dominated by generic drug supply, and relevant preparations have been included in the national centralized volume-based procurement. The average price reduction of the selected products exceeds 65%, the accessibility of drugs in public medical institutions has been greatly improved, and the market demand for upstream API has also maintained a steady growth of around 8% annually.

The original research enterprise of phentolamine is Novartis, and the original research trade name is "Regitine". Its core compound patent expired worldwide in the 1970s. At present, the main dosage form of the original research product on the market is injection, with a specification of 10mg/1ml, which has been included in the *Catalogue of Chemical Reference Preparations* of China and the FDA reference preparation catalogue. In terms of domestic API registration, more than 10 enterprises have obtained A status for their phentolamine APIs after registration with CDE. The domestically approved preparation varieties cover multiple dosage forms such as phentolamine mesylate for injection, phentolamine mesylate injection and tablets. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO can provide a full set of impurity reference standards for phentolamine, most of which are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. The products fully comply with the compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA, and can fully meet the full-process needs of API enterprises in quality research, impurity calibration and declaration and registration.