Tizanidine

Centrally acting muscle relaxants are the core clinical choice for improving spastic movement disorders. As a second-generation α2 adrenergic receptor agonist, tizanidine selectively agonizes the α2 receptors on the presynaptic membrane of spinal motor neurons, reduces the release of excitatory amino acids, inhibits polysynaptic reflexes, and lowers excessively high skeletal muscle tension, without obvious risk of respiratory depression. Clinically, it is mainly used to relieve chronic muscle spasm caused by spinal cord injury, stroke, multiple sclerosis, amyotrophic lateral sclerosis and other diseases, and can also be used for muscle spasm accompanied by local pain such as neck and shoulder pain, low back and leg pain, covering a wide range of medication users in neurology, orthopedics, rehabilitation and other departments.

The current global tizanidine market size is approximately USD 1.27 billion, with a compound annual growth rate maintained at 5.8%. The growth momentum mainly comes from the rising prevalence of central nervous system injuries and the increased consultation rate of myospasm-related diseases among the elderly population. The growth rate of the Chinese market is higher than the global average, with a compound annual growth rate of 7.2%, and the sales in domestic sample hospitals exceeded RMB 210 million in 2023. In terms of the competitive landscape, the original research product accounts for about 32% of the market share. More than 10 domestic generic pharmaceutical companies have obtained approval for their preparations, and this variety has been included in the fifth batch of national centralized volume-based procurement. The average price reduction of the winning products has reached 71% compared with that before the centralized procurement, and the accessibility for patients has been greatly improved.

The original research enterprise of tizanidine is Novartis Pharma Schweiz AG, and the original brand name is "Kaitong". Its core compound patent expired globally in 2018. The main dosage form approved for the original research product is tablet, with conventional specifications including 2mg and 4mg. It has now been included in the *Catalogue of Chemical Reference Preparations* of China, and is also listed in the FDA Reference Preparation Catalogue. Up to now, 8 domestic enterprises have obtained A status for their tizanidine API after registration with CDE, which can be associated with the declaration of preparations. The domestically approved tizanidine preparations include two categories, tablets and capsules, with a total of 22 approval numbers. (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 tizanidine API, covering all categories such as process impurities and degradation impurities. Most products are in sufficient stock. Spot orders placed before 16:00 can be shipped on the same day. All products meet the requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can fully support customers' needs in API R&D, quality research and compliance declaration.