Cinepazide
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| Clinical data | |
|---|---|
| ATC code | C04AX27 (WHO) |
| Identifiers | |
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| PubChem (CID) | 5282459 |
| ChemSpider | 4445611 |
| UNII |
67Y4P5C84X  |
| ChEMBL | CHEMBL1874750 |
| ECHA InfoCard | 100.041.739 |
| Chemical and physical data | |
| Formula | C22H31N3O5 |
| Molar mass | 417.49864 |
| 3D model (Jmol) | Interactive image |
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| (verify) | |
Cinepazide or cinepazide maleate[1] (Kelinao or Anjieli in China[2][3]) is a vasodilator used in China for the treatment of cardiovascular and cerebrovascular diseases, and peripheral vascular diseases.[4] It appears to work by potentiating A2 adenosine receptors.[5]
History
Cinepazide was discovered by scientists at Laboratoires Delalande (now part of Sanofi) in 1969 in an effort to explore useful substituted cinnamoyl-piperazine compounds.[6][7] The drug, in the form of a pill taken orally, was launched by Delalande in 1976 under the tradename Vasodistal, for treatment of heart failure, balance disorders, cerebrovascular disease, and vascular complications of diabetes.[6][8] In 1988 the drug was withdrawn from the market in Spain due to risk of agranulocytosis; other countries where the drug was available added warnings to the label.[8][9][10] It was withdrawn from the market in France in 1992.[11] The drug had also been marketed in Japan by Daiichi under the brand name "Brindel"[2] for dementia, but was withdrawn in 1999, following a review by the Japanese regulatory authorities of dementia drugs after a drug, calcium hopantenate, that had been considered the standard of care and against which cinepazide and other dementia drugs had been compared, had failed to demonstrate efficacy in a re-evaluation.[12]
In 2002 Sihuan Pharmaceutical brought an injectable form of the drug to market in China;[13] Sihuan had acquired the drug from a military hospital in China that had developed the formulation.[14] In 2010 it was the highest selling drug in China, with about 1 billion RMB in sales in the 3rd quarter, outselling Plavix in China.[13][3] This made Sihuan Pharm the largest company in China in the cardio-cerebral vascular drug market in 2010.[3] In 2014 it was the tenth highest-selling drug in China.[14]
References
- ↑ "Anjieli, Kelinao, cinepazide maleate - Product Profile - BioCentury". www.biocentury.com. Retrieved 2015-08-04.
- 1 2 Drugs.com Drugs.com International listings for cinepazide Page accessed Aug 3, 2015
- 1 2 3 20 Oct 2010Sihuan Pharm – China's leading player in cardio-cerebral vascular drug – IPO Report
- ↑ Sihuan Pharmaceutical Kelinao/Anjieli official site Page accessed Aug 3, 2015
- ↑ Ruffolo RR Jr, et al. Drug receptors and control of the cardiovascular system: recent advances. Prog Drug Res. 1991;36:117-360. Review. PMID 1876708 p 304
- 1 2 Johnson Sun for Guotai Junan International. Sept 28, 2011. Company Report: Sihuan Pharmaceuticals
- ↑ Cameron BD, et al The metabolic fate of the coronary vasodilator 4-(3,4,5-Trimethoxycinnamoyl)-1-(N-pyrrolidinocarbonylmethyl)piperazine (cinepazide) in the rat, dog and man. Xenobiotica. 1976 Jul;6(7):441-55. PMID 997590
- 1 2 Reactions Weekly 305(1):1. June 1990 Cinepazide-related agranulocytosis
- ↑ Laporte JR, Capellà D, Juan J.Agranulocytosis induced by cinepazide. Eur J Clin Pharmacol. 1990;38(4):387-8. PMID 2344862
- ↑ Department of Economic and Social Affairs of the United Nations Secretariat Consolidated List of Products Whose Consumption and/or Sale Have Been Banned, Withdrawn, Severely Restricted or not Approved by Governments Twelfth Issue: Pharmaceuticals United Nations – New York, 2005
- ↑ Sidney M. Wolfe, M.D. for the Public Citizen's Health Research Group. February 2, 1995. Differences in the Number of Drug Safety Withdrawals: United States, United Kingdom, Germany and France 1970-1992
- ↑ Takeda M, Tanaka T, Okochi M. New drugs for Alzheimer's disease in Japan. Psychiatry Clin Neurosci. 2011 Aug;65(5):399-404. PMID 21851448
- 1 2 Lefei Sun, Jinsong Du, and Iris Wang for Credit Suisse. October 6 2011 China Pharma Sector
- 1 2 Su Zhang for Standard Chartered Bank (HK) Limited. June 27, 2014 China health care: Pharma sector comes of age