The following classes of drugs are currently available for the treatment of Parkinson’s disease:
Anticholinergics: Antan
Antihistamines: Diphenhydramine, Amantadine
L-dopa analogues: Medobar, Xanax, Cilymet Dopamine agonists: Tysudar, Xelianxing, Cripa, Bromocriptine
Monoamine oxidase B inhibitors: Seguin, Kingspin
Catecholamine oxy-methyltransferase inhibitors: Entocapone (Kodan)
I. Levodopa and compound preparations.
1. Levodopa: After clinical application in 1967 and its success, it also brought a fundamental turn in the treatment of Parkinson’s disease, and is still the basic drug in this field. The market share of levodopa is only 0.3.
Since the early 1980s, oral preparations have been produced by Jiangsu Kanyi Pharmaceutical and Wuhan Zhonglian Pharmaceutical, and there are now 30 enterprises holding SFDA-issued preparation production licenses. Levodopa API was firstly approved by Guangxi He Feng Pharmaceutical, currently there are 13 enterprises with production approvals issued by SFDA, due to the limited sales of levodopa alone, at present most of the levodopa and peripheral dopa decarboxylase inhibitor benserazide in a 4:1 ratio to make a compound preparation, in addition to the compound preparation carbidopa/levodopa.
2.Dobutamine: Dobutamine is a compound preparation of levodopa and benserazide, which has high bioavailability and is the leading variety in the world anti-Parkinson’s disease drug market. It was first developed by Roche in Switzerland and approved by FDA in 1973 under the trade name Madopar (Medopar). In 1998, Shanghai Roche has been approved to produce dobutamine tablets in China, and Roche’s dobutamine dispersible tablets were approved to be imported for clinical use in 1999.
In 2003, it ranked 285th in the world prescription drug market, with sales revenue of $179 million, up 20 from $148 million in 2000, an increase of 0.8. Medobar is the main product in the domestic anti-Parkinson’s disease drug market, and from the domestic market in 2002, the drug not only dominates the hospital Parkinson’s drug, but also performs well in the retail market, according to SFDA Southern Institute of national retail drug statistics show that in 2002, Medobar ranked first in the neurological drugs, sales share of neurological drugs accounted for 5.49, sales in key hospitals accounted for 3.6 of the performance income of Shanghai Roche.
Dobutamine was developed earlier in China. In 1993, Shanghai No.2 Pharmaceutical Factory had developed dobutamine tablets and obtained the production approval, and in 1995, Shanghai Oriental Pharmaceutical, Shanghai Sanxin Pharmaceutical and Shanghai Fuda Pharmaceutical had developed dobutamine capsules. Now the domestic production approval of Guangzhou Qiao Guang Pharmaceutical, Guangzhou Huan Ye Pharmaceutical and Hangzhou Aida Pharmaceutical, the domestic has formed by the pattern of imported drugs, joint venture drugs and domestic drugs, China Pharmaceutical Business Association recently reported that in 2003 in China’s wholesale field leading the top 200 drugs, dobutamine ranked 84th, the sales amount has reached 93.07 million yuan, becoming an important anti-Parkinson’s disease drug market. It has become an important product in the anti-Parkinson’s disease market.
3, carbidopa-levodopa: This product is another leading variety of levodopa-based combination drugs, which has a good market performance in the global market. This product passed the U.S. FDA in May 1991, with the trade name Sinemet (restorative), ranked 269th among the world’s leading 500 drugs in 2000, with sales of $170 million, and in 2003 the world prescription drug Bristol-Myers Squibb’s carbidopa-levodopa sales were $108 million in the market, an increase of 11.3 from the previous year, but its performance in the domestic market was not outstanding.
In 1995, Nantong Pharmaceutical General Factory received approval for the production of carbidopa-levodopa under the trade name “Cilamet”. At present, in the domestic carbidopa/levodopa market, mainly the imported drugs of Merzadone Italy and the controlled-release tablets of Merzadone Hangzhou, which occupy more than 90 shares.
Second, dopamine agonists.
Dopamine agonists are a relatively important class of drugs in the anti-Parkinson’s disease drug market, usually used for initial treatment, their efficacy alone is not as significant as levodopa, when levodopa is not effective enough as an adjuvant to reduce the impact of high doses of levodopa on its neurons.
1.Bromocriptine, approved by FDA in March 1982, was marketed in the United States under the trade name of Parlodel, whose bromocriptine occupies a major market in the world, with sales revenue of $134 million in 2000, and is currently one of the products of Novartis.
Bromocriptine is mainly sold in the domestic market by Novartis, followed by Swiss Serono’s drugs and “Bemotin”, a product of Hungary’s Geri Grand Pharmacy, which ranked 142nd among the top 200 drugs in China’s wholesale sector in 2003, with sales amounting to 52.56 million yuan. Bromocriptine API and its capsule are domestic products under research and development, and have entered the clinical research schedule, after the domestic drug market, will change the status quo of high drug prices.
2.Pegolit. Developed by Elan Corporation, trade name Permax, approved by FDA in December 1988 and marketed in the U.S., with a market share of 0.53 billion USD in 2000. Currently a product of Eli Lilly and Company, the trade name Celance (Xie Liang Xing). Pergolide mesylate API and tablets have been developed by Tianjin Central Pharmaceuticals, which received manufacturing approval for marketing in 1999, and its efficacy is superior to that of bromocriptine and lysergic acid.
The relevant patent JP-1513267 submitted by Eli Lilly Japan expired on December 9, 2003. According to the Regulations on Administrative Protection of Pharmaceuticals, the administrative protection of the product in China has been terminated, and the imported drug in the domestic market is the product of Eli Lilly UK.
3.Ropinirole: The drug was developed by the UK’s Shik Bicheng, first marketed in the UK in September 1996 under the trade name Requip, and approved by the FDA for marketing in the US on September 19, 1997. Product for clinical use, the market continues to advance, in 2001 than the previous year, an increase of 31.8, sales revenue of £ 0.75 billion, the last two years in a rising trend, global revenue of £ 0.99 billion in 2003 (equivalent to $162 million).
4. Pramipexole: It is a product developed by Farmacia and Boehringer Ingelheim, and was first marketed in the United States in July 1997 after being approved by the FDA under the trade name Senfro. After the product market growth rate is relatively fast, in 2000, Senfuro sales revenue has reached 133 million euros, the next two years have been increasing at a rate of more than 30, but in 2003, basically the same as the previous year, for 232 million euros.