Inactivation of the miltefosine transporter, LdMT, causes miltefosine resistance that is conferred to the amastigote stage of Leishmania donovani and persists in vivo

Int J Antimicrob Agents. 2007 Sep;30(3):229-35. doi: 10.1016/j.ijantimicag.2007.05.007. Epub 2007 Jul 12.

Abstract

Miltefosine (hexadecylphosphocholine) is the first oral antileishmanial drug. In this study, we addressed the question whether miltefosine-resistant Leishmania donovani promastigotes transform to miltefosine-resistant amastigotes. A promastigote line, M-mutR, showed defective internalisation of miltefosine owing to mutations in LdMT, similar to previously described resistant lines. M-mutR parasites were infective to macrophages in vitro as well as in BALB/c mice in vivo. There was good correlation of in vitro resistance indices between promastigotes and intracellular amastigotes. Most importantly, M-mutR parasites retained the resistant phenotype in vivo, with no decrease of hepatic burden in BALB/c mice following miltefosine treatment up to 30 mg/kg (ca. 90% inhibition in wild-type infections). No cross-resistance to other antileishmanial drugs was observed in M-mutR amastigotes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphatases / genetics*
  • Adenosine Triphosphatases / physiology
  • Animals
  • Antiprotozoal Agents / metabolism*
  • Antiprotozoal Agents / pharmacology*
  • Drug Resistance
  • Female
  • Genotype
  • Leishmania donovani / drug effects*
  • Leishmaniasis, Visceral / drug therapy
  • Leishmaniasis, Visceral / microbiology
  • Membrane Transport Proteins / genetics*
  • Membrane Transport Proteins / physiology
  • Mice
  • Mice, Inbred BALB C
  • Mutation / physiology
  • Phenotype
  • Phosphorylcholine / analogs & derivatives*
  • Phosphorylcholine / metabolism
  • Phosphorylcholine / pharmacology
  • Protozoan Proteins / genetics*
  • Protozoan Proteins / physiology

Substances

  • Antiprotozoal Agents
  • Membrane Transport Proteins
  • Protozoan Proteins
  • Phosphorylcholine
  • miltefosine
  • Adenosine Triphosphatases
  • miltefosine transporter, Leishmania donovani