In vivo selection of Plasmodium falciparum pfmdr1 86N coding alleles by artemether-lumefantrine (Coartem)

J Infect Dis. 2005 Mar 15;191(6):1014-7. doi: 10.1086/427997. Epub 2005 Feb 8.

Abstract

Artemisinin derivative-based combination therapy is expected to suppress the development of Plasmodium falciparum drug resistance in Africa. We have performed an artemether-lumefantrine (Coartem; Novartis) follow-up clinical trial in Zanzibar, in which pfcrt K76T and pfmdr1 N86Y frequencies were determined before drug administration and in all recurrent parasites during a follow-up period of 42 days. A significant increase in pfmdr1 86N was observed after exposure to the drug. This points to 86N as a potential marker of lumefantrine resistance in vivo, while suggesting that Coartem is not robust enough to avoid selection of resistance-associated mutations in some malarial settings.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP-Binding Cassette Transporters / genetics*
  • Alleles
  • Animals
  • Antimalarials / pharmacology*
  • Antimalarials / therapeutic use
  • Artemether
  • Artemisinins / pharmacology*
  • Artemisinins / therapeutic use
  • Child
  • Drug Resistance / genetics
  • Drug Therapy, Combination
  • Ethanolamines / pharmacology*
  • Ethanolamines / therapeutic use
  • Fluorenes / pharmacology*
  • Fluorenes / therapeutic use
  • Genes, MDR
  • Humans
  • Infant
  • Lumefantrine
  • Malaria, Falciparum / drug therapy
  • Malaria, Falciparum / parasitology
  • Plasmodium falciparum / drug effects*
  • Plasmodium falciparum / genetics
  • Polymorphism, Single Nucleotide
  • Protozoan Proteins / genetics*
  • Selection, Genetic*
  • Sesquiterpenes / pharmacology*
  • Sesquiterpenes / therapeutic use

Substances

  • ATP-Binding Cassette Transporters
  • Antimalarials
  • Artemisinins
  • Ethanolamines
  • Fluorenes
  • Protozoan Proteins
  • Sesquiterpenes
  • mdr gene protein, Plasmodium
  • Artemether
  • Lumefantrine