Increased systemic exposures of artemether and dihydroartemisinin in infants under 5 kg with uncomplicated Plasmodium falciparum malaria treated with artemether-lumefantrine (Coartem®)

Malar J. 2015 Apr 15:14:157. doi: 10.1186/s12936-015-0682-7.

Abstract

Background: Artemether-lumefantrine (AL) dispersible formulation was developed for the treatment of uncomplicated Plasmodium falciparum malaria in infants and children weighing 5 to <35 kg. However, there are no clinical studies with artemisinin-based combination therapy in infants <5 kg.

Methods: This multicentre, open-label, single-arm study evaluated the efficacy, safety and pharmacokinetics of AL dispersible in infants aged >28 days and <5 kg of body weight, who were treated with one AL dispersible tablet (20 mg artemether/120 mg lumefantrine) given twice-daily for three days and followed up for six weeks (core follow-up) and at 12 months of age (long-term follow-up).

Results: A total of 20 patients were enrolled and completed the six-week core study follow-up. In the per protocol population, PCR-corrected cure rate at days 28 and 42 was 100% (95% CI: 79.4, 100). AL dispersible was well tolerated with reported adverse events of mild to moderate severity. Pharmacokinetic data showed that lumefantrine levels were similar, however, artemether and dihydroartemisinin levels were on average two- to three-fold greater than historical values in infants and children ≥5 kg.

Conclusions: A three-day regimen of AL dispersible formulation was efficacious and generally well tolerated in infants weighing <5 kg with uncomplicated P. falciparum malaria, but artemether and dihydroartemisinin exposures could not be supported by the preclinical safety margins for neurotoxicity. Hence, dosing recommendations cannot be made in infants <5 kg as implications for toxicity are unknown.

Trial registration: Clinicaltrials.gov NCT01619878.

Publication types

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

MeSH terms

  • Antimalarials / administration & dosage
  • Antimalarials / adverse effects
  • Antimalarials / pharmacokinetics*
  • Artemether, Lumefantrine Drug Combination
  • Artemisinins / administration & dosage
  • Artemisinins / adverse effects
  • Artemisinins / pharmacokinetics*
  • Drug Combinations
  • Drug-Related Side Effects and Adverse Reactions / epidemiology
  • Ethanolamines / administration & dosage
  • Ethanolamines / adverse effects
  • Ethanolamines / pharmacokinetics*
  • Female
  • Fluorenes / administration & dosage
  • Fluorenes / adverse effects
  • Fluorenes / pharmacokinetics*
  • Humans
  • Infant
  • Malaria, Falciparum / drug therapy*
  • Male
  • Treatment Outcome

Substances

  • Antimalarials
  • Artemether, Lumefantrine Drug Combination
  • Artemisinins
  • Drug Combinations
  • Ethanolamines
  • Fluorenes
  • artenimol

Associated data

  • ClinicalTrials.gov/NCT01619878