Topiroxostat

Hyperuricemia and the onset of gout are closely related to excessive uric acid production and insufficient excretion. Xanthine oxidase is the key rate-limiting enzyme in the process of uric acid production, while the activity of renal tubular uric acid transporters also directly affects the efficiency of uric acid excretion. Topiroxostat is a new type of selective xanthine oxidase inhibitor, which also has a partial uricosuric effect. It strongly reduces the serum uric acid level through a dual mechanism of action. Clinically, it is mainly used for the treatment of hyperuricemia in patients with gout, and is also suitable for adult patients who are intolerant to allopurinol or have poor response to it. It has a low incidence of adverse reactions, and there is no need to adjust the dosage according to renal function, providing a safer medication option for people with hyperuricemia complicated with chronic kidney disease.

At present, the global anti-gout drug market size has exceeded 3.5 billion US dollars, with an annual compound growth rate of around 7%, among which xanthine oxidase inhibitors account for more than 60%. As a new generation of drugs in the same category, topiroxostat has seen particularly prominent growth in the East Asian market. In 2023, the sales of topiroxostat preparations at the terminal of China's public medical institutions exceeded 200 million yuan, with a year-on-year growth rate of over 120%. At present, more than 10 domestic enterprises have laid out the R&D of generic topiroxostat, among which 3 enterprises have obtained approval for the marketing of their preparation products. As more generic drugs pass the consistency evaluation in the future, there is still considerable room for improvement in market penetration.

The original research enterprise of topiroxostat is Fuji Yakuhin Co., Ltd. of Japan, with the original brand name TOPILORIC. The core compound patent will expire in Japan in 2026, and the compound patent in China expired in 2023. The main dosage form approved for the original drug is tablet, with specifications of 20mg and 40mg. The original topiroxostat tablet has been included in the Catalogue of Marketed Drugs in China and is used as a reference listed drug. As of now, 8 domestic enterprises have completed the registration of topiroxostat active pharmaceutical ingredients (APIs) at the Center for Drug Evaluation (CDE), and all the approved preparation products are topiroxostat tablets. (Data as of June 2025, please refer to the official CDE website for the latest information)

CATO can provide a full set of topiroxostat impurity reference standards, covering all categories such as synthetic process impurities and degradation impurities. Most of the products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All reference standards comply with the regulatory requirements of the Chinese Pharmacopoeia, FDA and other regulations, and can fully meet the use requirements of different stages such as API R&D, quality research, and registration and declaration.