Lomerizine

Migraine is a highly prevalent chronic neurovascular disease, and for a long time, there has been a lack of medications with both preventive and attack-relief effects and low side effects. The emergence of lomerizine, a diphenylpiperazine calcium channel blocker, has filled this clinical gap. This drug selectively blocks calcium ion influx in cerebral vascular smooth muscle, inhibits cerebral vasospasm, and reduces the release of vasoconstrictive substances such as 5-hydroxytryptamine and thromboxane A2. It improves cerebral microcirculation without affecting peripheral vascular function. It is the world's first second-generation calcium antagonist approved for the preventive treatment of migraine, and can also be used to relieve symptoms such as dizziness and headache caused by insufficient cerebral blood supply and sequelae of cerebral infarction. The applicable population covers migraine patients aged 18 and above with frequent attacks and elderly groups with ischemic cerebrovascular diseases.

The global lomerizine market size was approximately USD 210 million in 2023, with a compound annual growth rate of 4.2% in the past five years. The growth momentum mainly comes from the increasing prevalence of migraine and the popularization of chronic disease preventive medications in primary medical institutions. China's market accounts for about 17%, and the current supply is dominated by generic drugs. A total of 7 domestic enterprises hold preparation approval documents. The API supply side has achieved localized substitution, and the market share of imported original research products is less than 5%. In provincial centralized procurement, the average winning bid price of oral preparations of this variety has dropped by more than 82% compared with the initial stage of the original research product's launch, greatly reducing the medication burden of patients.

The original research enterprise of lomerizine is Mitsubishi Tanabe Pharma of Japan, with the original brand name "Migral". Its core compound patent expired globally in 2008. The main dosage form of the original research product is 5mg tablets, which is the reference preparation listed in the Japanese Orange Book, and is not included in the Chinese *Catalogue of Reference Preparations for Chemical Drugs*. At present, there are 12 lomerizine API registration numbers in China, 8 of which are in A status and can be associated with domestic preparation declarations. In addition, 10 domestic preparation varieties have been approved for marketing, and the original research enterprise has not submitted a marketing application in China. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO can provide a full set of lomerizine impurity reference standards, most of which are in stock. Orders for in-stock products placed before 16:00 will be shipped on the same day. The products comply with the compliance requirements of multiple regulations including the Chinese Pharmacopoeia and FDA, and can provide stable reference material support for pharmaceutical enterprises' API R&D, quality control and consistency evaluation.