Opicapone

As a common degenerative disease of the central nervous system, Parkinson's disease is prone to complications such as "on-off phenomenon" and motor fluctuations in patients after long-term treatment with levodopa, and there is an urgent clinical demand for long-acting, highly selective catechol-O-methyltransferase (COMT) inhibitors. As the third-generation peripheral COMT inhibitor, opicapone reversibly and specifically blocks the metabolism of levodopa by peripheral COMT, prolongs the half-life and bioavailability of levodopa, and reduces the fluctuation of drug efficacy during administration. It is mainly used clinically as an adjuvant therapeutic drug for levodopa/carbidopa in adult Parkinson's disease patients with end-of-dose phenomenon. Compared with the first two generations of COMT inhibitors, it has a lower risk of hepatotoxicity, only needs to be administered once a day, and has a significant advantage in patient compliance.

At present, the number of Parkinson's disease patients worldwide has exceeded 10 million, of which Chinese patients account for nearly 30%. With the acceleration of the aging process, the market for related therapeutic drugs continues to expand. Data show that the global opicapone market size was approximately USD 120 million in 2023, with a compound annual growth rate of 18% in the past three years. The growth momentum mainly comes from the increased penetration rate in emerging markets and the upward adjustment of the recommendation level of the third-generation COMT inhibitors in clinical guidelines. In terms of the competitive landscape, the original research products still account for nearly 75% of the global market share at present, and only a small number of domestic enterprises have started the research and development of generic drugs, and no generic products have been approved for marketing, so the market competition is relatively moderate.

The original research enterprise of opicapone is Bial, a Portuguese company, with the original research trade name Ongentys. The expiration time of its core compound patent in Europe is 2027, and the expiration time of the compound patent in the US market is 2028. The main dosage form approved by the original research is oral tablet, with specifications of 25mg and 50mg. The original research preparation has been included in the FDA Reference Listed Drug Catalog, and has not yet been included in the *Catalogue of Chemical Pharmaceuticals* of China. In terms of the domestic market, no opicapone API has obtained an A-status registration number at present, and only 3 enterprises have submitted API DMF registration applications which are in the review stage. The original research preparation was approved by NMPA for import and marketing in 2021, and no generic preparation of domestic enterprises has been approved yet. (Data as of October 2024, please refer to the official website of CDE for the latest information)

In response to the R&D and quality control needs of opicapone, CATO provides a full set of impurity reference standards for this API, which can cover the whole process of impurity qualitative and quantitative research and stability investigation. 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 including the Chinese Pharmacopoeia and FDA, and can provide reliable material basis support for pharmaceutical R&D enterprises and inspection institutions.