Thiocolchicoside

Musculoskeletal pain is a high-prevalence chronic disease affecting more than 1.5 billion people worldwide. Long-term use of traditional non-steroidal anti-inflammatory drugs is prone to cause gastrointestinal and cardiovascular adverse reactions, so there is an urgent clinical need for alternatives with both analgesic effect and safety. Thiocolchicoside is a semi-synthetic colchicine derivative, which exerts anti-inflammatory and analgesic effects by inhibiting microtubule polymerization and blocking the release of inflammatory factors, while it does not affect the mitosis of normal cells, with significantly better safety than natural colchicine. It is mainly used clinically to treat acute musculoskeletal pain episodes such as low back pain, sciatica and arthritis, and can also be used for the auxiliary relief of acute gout attacks. The applicable population covers pain patients over 18 years old without severe hepatic and renal insufficiency.

The global thiocolchicoside market size was approximately USD 210 million in 2023, with a compound annual growth rate of 4.7% from 2019 to 2023, and the growth mainly comes from the continuous increase in demand for chronic pain management. At present, Europe is the largest consumer market, accounting for 58% of the global share, while the domestic market is still in the introduction period. The sales volume in sample hospitals in 2023 was approximately RMB 12 million, with an annual growth rate of more than 30%. In terms of the competitive landscape, European pharmaceutical enterprises occupy the leading position in original research and high-end generic drugs. At present, only a small number of domestic enterprises have started generic application, and there is no large-scale local supply.

The original research enterprise of thiocolchicoside is France's Pharmascience Laboratory, with the original brand name HiQur®. Its core compound patent in the EU expired in 2017, and there is no public authorization record for the Chinese compound patent. The dosage form approved for the original drug is oral tablet, with the main specification of 4mg per tablet. It has been included in the EU EMA reference preparation catalogue, but has not yet been included in the *Catalogue of Reference Preparations for Chemical Drugs* issued by China NMPA. At present, there is no valid A-status registration number of thiocolchicoside under evaluation or approved on the domestic API registration platform. Only 1 enterprise has submitted an I-status registration application, and there is no approved and marketed preparation product of this variety in China. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO can provide a full set of thiocolchicoside impurity reference standards, covering the whole chain of synthetic starting materials, intermediates and degradation impurities. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All reference standards meet the compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA, and can fully meet the needs of the whole stages of API R&D, quality research and application registration.