Siponimod

Multiple sclerosis is a chronic inflammatory demyelinating disease of the central nervous system, which has a high incidence among young adults and a high disability rate. The advent of siponimod has brought a new option for long-term disease course management for patients with relapsing forms. As a new generation of selective sphingosine-1-phosphate receptor modulator, it can bind to S1P1 and S1P5 receptors on the surface of lymphocytes, prevent lymphocytes from migrating to the central nervous system, and reduce inflammatory damage. At the same time, it can also promote the maturation of oligodendrocytes and potentially delay neurodegenerative lesions. Currently, it is approved for the treatment of relapsing forms of multiple sclerosis in adults, including clinically isolated syndrome, relapsing-remitting disease and active secondary progressive disease. It is the first oral disease-modifying therapy approved specifically for active secondary progressive multiple sclerosis.

At present, there are more than 2.8 million patients with multiple sclerosis worldwide, among which about 30% will progress to the secondary progressive form. With its unique dual mechanism of action, the global market size of siponimod had exceeded 1.2 billion US dollars in 2023, with a compound annual growth rate remaining above 18%. In terms of the Chinese market, following the official approval for marketing and inclusion in the National Reimbursement Drug List in 2020, the payment threshold for patients has been significantly reduced, and the market size growth rate has exceeded 40% in the past three years. The current competitive landscape is still dominated by the originator drug. Three domestic enterprises have submitted marketing applications for generic drugs, and no generic varieties have been approved yet, leaving a broad potential market space.

The originator enterprise of siponimod is Novartis Pharma, with the original brand name of Mayzent. The core compound patent of the originator drug will expire in 2027 in the United States, and the Chinese compound patent will expire in 2025. The main formulation approved for the originator drug is tablet, with specifications including 0.25mg and 2mg, which has been included in the *Catalogue of Chemical Drugs* of China and the FDA Reference Listed Drug Catalogue. In terms of domestic API registration, currently only the imported API of the originator enterprise has obtained Class A registration status, and the API registrations of another 4 domestic enterprises are in the review and approval stage. The originator formulation has been approved for marketing in China, and no generic formulation has been approved yet. (Data as of October 2024, please refer to the official website of CDE for the latest information)

In response to the R&D and production needs of siponimod, CATO can provide a full set of impurity reference standards for this API. Most products are in stock. Orders for in-stock products 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 fully support pharmaceutical enterprises in the whole-process quality research work from API R&D to registration.