Vorapaxar

Cardiovascular disease is the leading cause of death worldwide, among which arterial thrombosis is the core inducement of severe adverse cardiovascular events such as acute coronary syndrome and myocardial infarction. As the first-in-class protease-activated receptor 1 (PAR-1) antagonist, vorapaxar can selectively block thrombin-mediated platelet aggregation and inhibit thrombosis from the upstream of the coagulation pathway without significantly affecting bleeding time, providing a differentiated antiplatelet treatment option for people at high risk of thrombosis. Currently, this drug is mainly indicated for patients with a history of myocardial infarction or peripheral arterial disease, and can be combined with standard antiplatelet therapy to reduce the risk of the composite endpoint of cardiovascular death, myocardial infarction and stroke.

The global market size related to vorapaxar was approximately USD 320 million in 2023. Driven by the improvement of the diagnosis and treatment rate of peripheral arterial disease and the popularization of combination medication regimens, the compound annual growth rate from 2024 to 2029 is expected to be 4.7%. At present, the market is still dominated by the original research product, with the United States and the European Union as the main consumption regions, accounting for 72% of the global market share. In terms of the domestic market, no generic drug has been approved for marketing so far, and the market is in the stage of exclusive possession by the original research product. With the continuous release of demand for cardiovascular disease prevention and control, there is broad space for import substitution in the future.

The original research enterprise of vorapaxar is Merck & Co., Inc., and the original trade name is Zontivity. The core compound patent of the drug expires in 2024 in the United States, and the core compound patent in China expires in 2023. The main dosage form approved for the original research product is tablet, with a specification of 2.08 mg. The original research tablet has been included in the FDA Reference Listed Drug Catalog, and has not been included in the *Chinese Catalogue of Chemical Drugs* at present. In China, there is no vorapaxar API that has been registered with A status for the time being, and only several enterprises have submitted DMF applications which are under the review stage. The original research preparation was approved by the National Medical Products Administration for import and marketing in 2021. (Data as of October 2024, please refer to the official website of CDE for the latest information)

In response to the demand for qualitative and quantitative research on impurities in the development process of vorapaxar generic drugs, CATO can provide a full set of impurity reference standards for this API. Most products are in stock, and in-stock products ordered before 16:00 will be shipped on the same day. All products meet the compliance requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can fully support the whole-process R&D and production scenarios such as application document preparation, quality research and routine batch testing.