Cinepazide Explained

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] 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balance disorders, cerebrovascular disease, and vascular complications of diabetes.[7] [8] In 1988 the drug was withdrawn from the market in Spain due to risk of agranulocytosis; other countries where the drug was available added warnings to the label.[9] [10] It was withdrawn from the market in France in 1992.[11] The drug had also been marketed in Japan by Daiichi Pharmeceutical Company under the brand name "Brindel"[2] for dementia, but was withdrawn in 1999, following a review by the Japanese regulatory authorities of dementia drugs after a drug, calcium hopantenate, that had been considered the standard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; Sihuan had acquired the drug from a military hospital in China that had developed the formulation.[13] 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.[14] [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.[13]

Notes and References

  1. Web site: Anjieli, Kelinao, cinepazide maleate - Product Profile - BioCentury. www.biocentury.com. 2015-08-04.
  2. Drugs.com Drugs.com International listings for cinepazide Page accessed Aug 3, 2015
  3. 20 Oct 2010 Sihuan Pharm – China's leading player in cardio-cerebral vascular drug – IPO Report
  4. Sihuan Pharmaceutical Kelinao/Anjieli official site Page accessed Aug 3, 2015
  5. Ruffolo RR, Hieble JP, Brooks DP, Feuerstein GZ, Nichols AJ . Drug receptors and control of the cardiovascular system: recent advances . Progress in Drug Research. Fortschritte der Arzneimittelforschung. Progrès des Recherches Pharmaceutiques . 36 . 117–360 . 1991 . 1876708 . 10.1007/978-3-0348-7136-5_4. 978-3-0348-7138-9 . subscription .
  6. Cameron BD, Chasseaud LF, Hawkins DR, Taylor T . The metabolic fate of the coronary vasodilator 4-(3,4,5-Trimethoxycinnamoyl)-1-(N-pyrrolidinocarbonylmethyl)piperazine (cinepazide) in the rat, dog and man . Xenobiotica; the Fate of Foreign Compounds in Biological Systems . 6 . 7 . 441–55 . July 1976 . 997590 . 10.3109/00498257609151657 .
  7. Johnson Sun for Guotai Junan International. Sept 28, 2011. Company Report: Sihuan Pharmaceuticals
  8. Reactions Weekly 305(1):1. June 1990 Cinepazide-related agranulocytosis
  9. Laporte JR, Capellà D, Juan J . Agranulocytosis induced by cinepazide . European Journal of Clinical Pharmacology . 38 . 4 . 387–8 . 1990 . 2344862 . 10.1007/bf00315580 . 19427552 .
  10. 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
  11. 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
  12. Takeda M, Tanaka T, Okochi M . New drugs for Alzheimer's disease in Japan . Psychiatry and Clinical Neurosciences . 65 . 5 . 399–404 . August 2011 . 21851448 . 10.1111/j.1440-1819.2011.02253.x . 21519637 .
  13. Su Zhang for Standard Chartered Bank (HK) Limited. June 27, 2014 China health care: Pharma sector comes of age
  14. Lefei Sun, Jinsong Du, and Iris Wang for Credit Suisse. October 6, 2011 China Pharma Sector

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