Benserazide

As Parkinson's disease is a common neurodegenerative disease among middle-aged and elderly people, levodopa replacement therapy is a clinically recognized core regimen. However, after oral administration, most of levodopa will be decomposed by decarboxylase in the periphery, and only a small amount can penetrate the blood-brain barrier to exert effects. It is also prone to cause adverse reactions such as gastrointestinal reactions and dyskinesia. Benserazide is a peripheral dopa decarboxylase inhibitor, which cannot penetrate the blood-brain barrier itself. When used in combination with levodopa, it can specifically inhibit the peripheral decarboxylation process of levodopa, greatly increase the concentration of levodopa entering the central nervous system, and reduce peripheral adverse reactions at the same time. It is a key component of compound levodopa preparations, and is mainly suitable for long-term treatment of patients with idiopathic Parkinson's disease and symptomatic Parkinson's syndrome.

At present, the global market size of anti-Parkinson's disease drugs has exceeded 4.5 billion US dollars, with a compound annual growth rate maintained at around 6.8%. Among them, compound levodopa preparations account for about 22% of the market share due to their clear clinical positioning and high cost performance. The domestic market size of anti-Parkinson's disease drugs has exceeded 8 billion yuan. With the acceleration of the aging process, the compound annual growth rate in the past five years has reached 9.2%. The domestic market of benserazide-related preparations has long been dominated by original research products. In recent years, with the advancement of the consistency evaluation of generic drugs, 3 enterprises have obtained marketing approval for levodopa and benserazide hydrochloride tablets. After centralized procurement, the price of relevant preparations has dropped by more than 70%, and the market demand for corresponding APIs continues to be released.

The original research enterprise of benserazide is Roche, and the trade name of its original research compound preparation is Madopar, which is composed of benserazide and levodopa in a ratio of 1:4. Its core compound patent expired relatively early in major global markets, and the compound patent in China expired in 2004. At present, the originally researched dosage form approved in China is tablet, with the specification of 50mg benserazide/200mg levodopa. This preparation has been included in the Chinese Chemical Reference Preparation Catalogue and is also listed as an FDA reference preparation. Up to now, 7 enterprises' benserazide APIs have obtained A-status registration on the CDE API registration platform, and a total of 8 domestic enterprises have obtained marketing approval for levodopa and benserazide hydrochloride tablets, among which 5 have passed the consistency evaluation. (Data as of October 2024, please refer to the official CDE website for the latest data)

CATO can provide a full set of benserazide impurity standard substances, covering all research impurity reference substances related to the synthesis process and degradation pathways, and most products are available in stock. All standard substances comply with the relevant regulatory requirements of the Chinese Pharmacopoeia and FDA, and complete structure confirmation and purity testing reports are provided. In-stock products ordered before 16:00 can be shipped on the same day, which can fully meet the research needs of different stages such as API R&D, quality research, and consistency evaluation.