Lesinurad

As one of the first-line clinical drugs for the treatment of central precocious puberty, relugolix is a gonadotropin-releasing hormone (GnRH) antagonist. Its mechanism of action is to rapidly inhibit the secretion of luteinizing hormone and follicle-stimulating hormone by competitively blocking GnRH receptors in the anterior pituitary gland, thereby reducing sex hormone levels. Compared with the "flare-up effect" of traditional GnRH agonists, relugolix takes effect faster and does not cause a transient increase in hormone levels at the initial stage of administration. In addition to children with central precocious puberty, it can also be used for the treatment of sex hormone-dependent diseases such as endometriosis and prostate cancer, which can effectively shorten the time for symptom improvement and improve patients' medication compliance.

At present, the global relugolix market size has exceeded 1.2 billion US dollars, with a compound annual growth rate maintained at around 8%. The growth momentum mainly comes from two directions: the improvement of the diagnostic rate of central precocious puberty in children and the expansion of indications in the oncology field. The domestic market is still in the early stage of development, with a small number of approved products and a relatively loose competitive landscape. As relevant indications are included in the drug security scope for rare diseases in children, the market growth rate is expected to exceed 15% in the next 3 years, with large import substitution space.

The original research enterprise of relugolix is Ferring Pharmaceuticals, and the original brand name is Firmagon. The core compound patent expires in 2024 in major markets such as Europe and the United States, and the compound patent in China expires in 2025. At present, the main dosage form approved for the original drug is powder for injection, with specifications of 80mg and 120mg, which has been included in the FDA Reference Listed Drug Catalog, but it has not yet been included in the *Catalog of Chemical Drugs* in China. As of the retrieval time, no domestic enterprise has registered the DMF filing of relugolix API. Only the original relevant dosage forms of leuprorelin acetate microspheres for injection have been approved for import and marketing, and domestic preparations are still in the declaration stage. (Data as of November 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of impurity reference standards for relugolix API, most of which are in stock. In-stock products ordered before 16:00 will be shipped on the same day. They can meet the compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA, and provide stable reference standard support for pharmaceutical enterprises in drug research and development and quality control links.