Rivaroxaban

Venous thromboembolism is the third leading cardiovascular cause of death worldwide, second only to myocardial infarction and stroke. Traditional anticoagulants have clinical limitations such as narrow therapeutic window and the need for frequent coagulation function monitoring. The advent of rivaroxaban provides a better option for anticoagulant therapy. As the world's first oral direct factor Xa inhibitor, it highly selectively blocks the active site of factor Xa and inhibits thrombin generation, thereby blocking the core link of thrombosis. At present, this drug has been approved for multiple indications, including prevention of venous thromboembolism after hip or knee replacement surgery, treatment of deep vein thrombosis and pulmonary embolism, and prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation, covering the full age range of adult anticoagulation populations. The feature of no need for routine coagulation monitoring greatly improves patients' medication compliance.

In 2023, the global market size of rivaroxaban exceeded 7 billion US dollars, and the market size in China exceeded 9 billion RMB, maintaining an overall compound annual growth rate of 3%. With the implementation of the centralized procurement policy, the market share of domestic generic drugs has exceeded 70%, and the market share of the original drug is gradually shifting to generic drug enterprises, driving the continuous rise in demand for upstream APIs. The total annual production capacity of domestic API enterprises has exceeded 1,000 tons. At present, there are more than 30 domestic enterprises registered for rivaroxaban APIs, and the export market is mainly emerging pharmaceutical markets such as Southeast Asia, South America and Eastern Europe. Leading enterprises have passed FDA and CEP certifications and are capable of supplying regulated markets.

The original research enterprise of rivaroxaban is Bayer HealthCare Co., Ltd., and the original research trade name is Xarelto®. Its core compound patent expired in China in December 2020, and the crystal form patent expired in July 2024. The main dosage forms approved for the original drug include tablets, with three specifications of 10mg, 15mg and 20mg, which have been included in the Chinese *Catalogue of Reference Preparations of Chemical Drugs* and the FDA reference preparation catalogue. Up to now, there are more than 30 rivaroxaban API registration records on the CDE API registration platform, of which more than 20 are in the status of "A" (already used in marketed preparations), and more than 20 domestic enterprises have obtained approval for marketing of rivaroxaban tablets. (Data as of November 2024, please refer to the official CDE website for the latest information)

CATO provides a full set of impurity reference standards for rivaroxaban APIs, covering the full-link demands of synthetic starting materials, intermediates, process impurities and degradation impurities. Most products are in stock, and orders placed before 16:00 can be shipped on the same day. All products comply with the regulatory requirements of the Chinese Pharmacopoeia, FDA and other regulations, and can fully meet the demands of enterprises in all stages of API R&D, quality research and registration application.