Valproate

As a classic anti-epileptic spectrum drug, valproic acid is a fatty acid anticonvulsant that exerts effects through multiple mechanisms including increasing the concentration of γ-aminobutyric acid (GABA) in the brain and blocking voltage-dependent sodium channels. It is currently one of the few broad-spectrum neurotherapeutic drugs that can cover generalized seizures, partial seizures and manic episodes associated with bipolar disorder. It is a first-line option for long-term control and treatment of epilepsy in both pediatric and adult patients, and is also a priority recommended medication for patients with epilepsy comorbid with migraine. Its clinical demand covers neurology diagnosis and treatment scenarios for all age groups.

The annual global market size of valproic acid preparations is approximately USD 2.3 billion, with a compound annual growth rate of around 2.1% from 2023 to 2028. China accounts for approximately 18% of the global market, and the proportion of medication used in primary medical institutions is increasing year by year. As the compound patent has expired for many years, the current market presents a pattern of coexistence of originator drugs and generic drugs. More than 30 domestic enterprises have obtained approval for generic preparations, among which 12 enterprises have passed the consistency evaluation for their oral dosage forms. In the 7th round of national centralized drug procurement, the average price reduction of valproate oral regular-release dosage forms was 47%, and their accessibility at the primary level has been greatly improved.

The originator enterprise of valproic acid is Sanofi, with the originator brand name "Depakine". Its core compound patent expired globally in 1973, and the core domestic preparation patent expired in 2004. Currently, the dosage forms of the originator drug approved in China include oral solution (12g/300ml), sustained-release tablets (0.5g) and powder for injection (0.4g), all of which have been included in the China Listed Drug Catalog as reference preparations. According to the domestic API registration platform, 17 enterprises have obtained A-status registration numbers for valproic acid APIs so far, and the corresponding domestically approved preparation varieties cover all dosage forms including oral regular-release dosage forms, sustained and controlled-release dosage forms and injections. (Data as of October 2024, please refer to the official CDE website for the latest information)

CATO provides a full set of valproic acid impurity reference standards, which can meet the impurity research requirements under different process routes and fully comply with the regulatory requirements of multiple countries including the Chinese Pharmacopoeia and FDA. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day, which can efficiently support the quality research and consistency evaluation work of API enterprises.