Cyclobenzaprine

Skeletal muscle spasm is a common concomitant symptom of musculoskeletal system diseases. Traditional therapeutic drugs are often accompanied by strong central sedative side effects, and there has been a long-standing clinical demand for safer muscle relaxant drugs. Cyclobenzaprine is a centrally acting muscle relaxant. By acting on α and 5-hydroxytryptamine receptors at the brain stem level, it inhibits the excessive discharge of motor neurons, relieves the pain and tenderness accompanied by muscle spasm without affecting the normal function of muscles, and improves local activity limitation at the same time. It is mainly used to relieve muscle spasm associated with acute, painful musculoskeletal diseases, and is suitable for short-term adjuvant treatment of adult patients, with the usual course of treatment not exceeding 2 to 3 weeks.

At present, the global market size of cyclobenzaprine is approximately USD 320 million, with the United States as the core consumer market, accounting for more than 85% of the global share. Due to the long clinical application history of this drug, generic drugs have flooded in rapidly after the expiration of the patent, and currently generic drugs account for more than 90% of the overall market share. The domestic market is still in the cultivation stage, with an annual growth rate maintained at around 11%, and it has not been included in the national centralized procurement scope. The application enthusiasm of local enterprises is increasing year by year.

The original research enterprise of cyclobenzaprine is Merck Sharp & Dohme, with the original trade name Flexeril, and its core compound patent expired globally in 2003. The main dosage form approved for the original product is tablet, and common specifications include 5mg and 10mg. The original product has been included in the FDA Orange Book Reference Listed Drug Catalog, but has not yet been included in the reference listed drug catalog marketed in China. At present, the original preparation has not been approved for marketing in China. In terms of API registration, there is no domestic or imported registration number that has obtained A status. Only 2 enterprises have submitted API registration applications, which are currently under the review and approval stage. (Data as of December 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of impurity reference standards for cyclobenzaprine API, supporting the full-process impurity research requirements from R&D to declaration. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. The products fully comply with the requirements of multiple national regulations such as the Chinese Pharmacopoeia and FDA, helping enterprises accelerate the R&D and declaration progress of related varieties.