Piperaquine

Piperaquine
Systematic (IUPAC) name
1,3-bis[4-(7-chloroquinolin-4-yl)piperazin-1-yl]propane
Clinical data
Identifiers
4085-31-8 Yes
PubChem CID 122262
ChemSpider 109031 
UNII A0HV2Q956Y 
ChEMBL CHEMBL303933 
Chemical data
Formula C29H32Cl2N6
535.51
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Piperaquine is an antimalarial drug, a bisquinoline first synthesised in the 1960s, and used extensively in China and Indochina as prophylaxis and treatment during the next 20 years. Usage declined in the 1980s as piperaquine-resistant strains of P. falciparum arose and artemisinin-based antimalarials became available. However, Chinese scientists have been studying whether piperaquine can still be used therapeutically in combination with artemisinin.[1]

Piperaquine is characterized by slow absorption and a long biological half-life,[2] making it a good partner drug with artemisinin derivatives which are fast acting but have a short biological half-life.[3]

The fixed-dose combination dihydroartemisinin-piperaquine (Eurartesim) was submitted for approval to the European Medicines Agency in 2009.[4]


References

  1. Davis TM, Hung TY, Sim IK, Karunajeewa HA, Ilett KF (2005). "Piperaquine: a resurgent antimalarial drug". Drugs 65 (1): 75–87. doi:10.2165/00003495-200565010-00004. PMID 15610051.
  2. D'alessandro U. (2009). "Progress in the development of piperaquine combinations for the treatment of malaria". Curr Opin Infect Dis 22 (6): 588–92. doi:10.1097/QCO.0b013e328332674a. PMID 19773652.
  3. http://apps.who.int/prequal/info_applicants/Guidelines/Nonclinical_Overview_Artemisinin-Derivatives.pdf"
  4. Medicines for Malaria. "Registration". Retrieved 2010-06-20.