Ticagrelor

Acute coronary syndrome (ACS) is one of the diseases with high fatality rate in the field of cardiovascular diseases, and antiplatelet therapy is the core regimen for its whole-course management. As the first reversibly binding P2Y12 receptor antagonist, ticagrelor is an antiplatelet drug of the cyclopentyltriazolopyrimidine class. It can take effect directly without metabolic activation by the liver. Compared with clopidogrel, it has a faster onset of action, stronger platelet inhibitory effect and smaller individual differences. Clinically, it is mainly used for ACS patients and patients with ischemic heart disease receiving PCI treatment. It can significantly reduce the risk of the composite endpoint of cardiovascular death, myocardial infarction and stroke without increasing the overall risk of major bleeding, and is a first-line antiplatelet drug recommended by current domestic and foreign guidelines.

The global ticagrelor market size reached a peak of nearly 3 billion US dollars in 2021. After the expiration of the core patent, generic drugs have entered the market rapidly, and the current overall market size is stable at around 1.2 billion US dollars. China is the regional market with the fastest growth rate of ticagrelor. In 2023, the sales volume of ticagrelor in domestic sample hospitals exceeded 1.8 billion yuan, and the proportion of generic drugs in public medical institutions has exceeded 85%. At present, more than 20 domestic enterprises have obtained approval for ticagrelor generic drug preparations. The winning bid price in centralized procurement has dropped by more than 90% compared with the highest price of the original research drug, and the clinical accessibility has been greatly improved. The expansion of downstream preparation production capacity directly drives the continuous growth of demand for upstream API.

The original research enterprise of ticagrelor is AstraZeneca, and the original research brand name is "Brilinta". The core compound patent expired in 2019 in the United States and Europe, and the core compound patent in China expired in 2021. The main dosage form approved for the original research drug is tablet, with specifications of 90mg and 60mg. It has been included in the *Catalogue of Reference Preparations of Chemical Drugs* of China, and is also listed in the FDA Reference Preparations Catalogue. In terms of domestic API registration, there are currently more than 30 registration numbers of ticagrelor API, among which 17 have been publicized as Class A status, and ticagrelor tablets approved by multiple domestic enterprises have been launched on the market for sale. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of impurity reference standards for ticagrelor API. All products in the full series meet the compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA. Most products are in regular stock. Spot orders placed before 16:00 can be shipped on the same day, which can meet the reference standard use requirements of API R&D, consistency evaluation and commercial production at all stages.