Riluzole

Amyotrophic lateral sclerosis is a progressive neurodegenerative disease, and patients with this disease have an average survival period of only 3 to 5 years. The clinical practice has long faced the dilemma of extremely limited treatment options. Riluzole, a benzothiazole anti-excitatory neurotoxic drug, is the first specific drug approved for the treatment of amyotrophic lateral sclerosis. Its mechanism of action is to block the release of glutamate from the presynaptic membrane, inhibit the activity of voltage-dependent sodium channels and N-methyl-D-aspartic acid receptors, and reduce neuronal damage induced by excitatory amino acids. It can effectively delay the progression of the patient's disease, prolong the survival period and the survival time before tracheotomy. It is currently a basic treatment drug for amyotrophic lateral sclerosis recommended by domestic and foreign guidelines, and is suitable for all adult patients without clear contraindications.

The global market size of riluzole has maintained steady growth for a long time. In 2023, the market size was approximately USD 720 million, and the market size in China was approximately RMB 390 million, with a compound annual growth rate maintained at around 5.1%. In terms of the competitive landscape, the original research product still occupies a dominant position in the mid-to-high-end market, and domestic generic drug companies have gradually completed the replacement. As of 2024, more than 8 local enterprises have obtained marketing approval for riluzole preparations, and riluzole has been included in the National Medical Insurance Catalog (Class B). The medication burden on patients has decreased by more than 80% compared with that in the initial stage of marketing, and the accessibility at the primary level continues to improve.

The original research enterprise of riluzole is Aventis Pharma (later merged into Sanofi Group), and the original research brand name is Rilutek. The core compound patent of the original research product expired in the United States in 2015, and the compound patent in China expired in 2017. The original research dosage form is oral tablet with a specification of 50mg, which has been included in the *Catalog of Reference Preparations of Chemical Drugs* of China and is also a reference preparation recognized by the FDA. Currently, there are more than 12 riluzole API registration numbers (status A) in China, and domestic APIs can fully meet the demand of domestic preparation production. The riluzole preparations approved in China cover two dosage forms: tablets and capsules. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO can provide a full set of impurity reference standards for riluzole to support the quality research needs of the whole process of R&D and production. 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 compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA, and can be directly used in scenarios such as method validation, stability study and registration declaration.