Rezvilutamide

Prostate cancer is a high-incidence malignant tumor of the male genitourinary system. Among patients with metastatic hormone-sensitive prostate cancer, the prognosis is generally poor, and traditional second-generation androgen receptor (AR) inhibitors have the risk of central nervous system-related adverse reactions. As a second-generation AR inhibitor independently developed in China, rezvilutamide greatly reduces the penetration rate of the blood-brain barrier by optimizing the molecular structure, can highly selectively block the activation of AR signaling pathways and inhibit the proliferation of tumor cells. Currently, its approved indication is metastatic hormone-sensitive prostate cancer with high tumor burden, which can significantly prolong the radiographic progression-free survival of patients, and reduce the incidence of adverse reactions such as fatigue and rash, providing a better treatment option for this type of patients.

The prevalence of prostate cancer in China is increasing year by year, driving the continuous expansion of the related therapeutic drug market. In 2023, the overall market size of second-generation AR inhibitors in China has exceeded 9 billion yuan, with a compound annual growth rate of more than 35%. As the first domestic second-generation AR inhibitor included in the National Medical Insurance Catalog, rezvilutamide has rapidly realized the replacement of original imported products by virtue of clear clinical benefits and price advantages. In the first half of 2024, its sales share in public medical institutions reached 22% in the same therapeutic field. At present, a number of domestic pharmaceutical companies have laid out the generic drug R&D track, and the market competition will further intensify after the expiration of the core patent.

The original research enterprise of rezvilutamide is Hengrui Medicine, with the trade name of Aixuerui®. Its core compound patent will expire in China in 2037. The main dosage form approved by the original research is tablet, with the specification of 80mg, which has been included in the *Catalogue of Reference Preparations of Chemical Drugs* issued by the National Medical Products Administration. At present, only the original research enterprise holds the A-status registration number of rezvilutamide API, and there is no API registration information of other enterprises. All rezvilutamide preparations approved for marketing in China are original research products. (Data as of June 2025, please refer to the official website of CDE for the latest information.

CATO provides a full set of impurity reference standards for rezvilutamide API. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day, which can meet the compliance requirements of multiple regulations such as Chinese Pharmacopoeia, FDA and others, and provide stable and reliable reference standard support for the whole process of pharmaceutical companies' R&D, quality research and production.