Isometheptene

As a common primary headache disorder, migraine has a global prevalence rate of over 10%. The throbbing pain during attacks, accompanied by symptoms such as nausea and photophobia, will seriously affect patients' daily work and life, and there has been a long-term unmet clinical demand for rapid symptom relief. Isometheptene is a sympathomimetic drug, which can reduce the pulsation amplitude of blood vessels by constricting the intracranial dilated blood vessels, and also has a mild analgesic effect. It is often formulated into compound preparations with paracetamol, caffeine and other ingredients for acute relief of migraine during the attack period, and can also be used to relieve the discomfort symptoms of tension headache. The applicable population is patients with headache attacks who have no serious cardiovascular and cerebrovascular diseases or underlying hypertension.

Driven by the increase in the diagnosis rate of migraine and the expansion of demand for acute symptomatic medication, the market of compound preparations containing isometheptene maintains a steady growth trend. At present, the market size of this type of drugs in China is approximately RMB 230 million, and the compound annual growth rate in the past three years has remained at around 6.8%. In terms of the competitive landscape, the original research products have not yet entered the Chinese market, and the existing marketed preparations are all generic drugs produced by domestic pharmaceutical companies. There is no record of related varieties included in the centralized drug procurement, and the supply of API is still dominated by small-scale commercial production, with an overall low market concentration.

The original research enterprise of isometheptene is Teva Pharmaceutical Industries Ltd. from Israel, and the commercial name of its original research compound preparation is "Midrin", which is composed of isometheptene, dichloralphenazone and paracetamol. Its core compound patent expired globally in 2001. At present, the main dosage form of the original research marketed product is oral capsule, each containing 65 mg of isometheptene. This product is not included in the *Catalogue of Reference Preparations of Chemical Drugs* of China, and the original research preparation has not been approved for marketing in China. Up to now, there is no A-status registration number of isometheptene available for preparation use on the API registration platform of China's Center for Drug Evaluation (CDE). There are a total of 2 isometheptene-related preparations approved for marketing in China, all of which are compound oral preparations. (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 isometheptene API. The core impurities have all completed structural confirmation and calibration, which can meet the process R&D needs of different enterprises. Most products are in sufficient stock, and orders placed before 16:00 can be shipped on the same day. All products meet the quality requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can provide reliable reference standard support for customers' links such as impurity research, quality standard establishment, and registration and declaration.