Selection of Cytochrome b Mutants Is Rare among Plasmodium falciparum Patients Failing Treatment with Atovaquone-Proguanil in Cambodia

Antimicrob Agents Chemother. 2021 Feb 17;65(3):e01249-20. doi: 10.1128/AAC.01249-20. Print 2021 Feb 17.

Abstract

Atovaquone-proguanil remains effective against multidrug-resistant Plasmodium falciparum in Southeast Asia, but resistance is mediated by a single point mutation in cytochrome b (cytb) that can arise during treatment. Among 14 atovaquone-proguanil treatment failures in a clinical trial in Cambodia, only one recrudescence harbored the cytb mutation Y268C. Deep sequencing did not detect the mutation at baseline or in the first 3 days of treatment, suggesting that it arose de novo Further sequencing across cytb similarly found no low-frequency cytb mutations that were up-selected from baseline to recrudescence. Copy number amplification in dihydroorotate dehydrogenase (DHODH) and cytb as markers of atovaquone tolerance was also absent. Cytb mutation played a minor role in atovaquone-proguanil treatment failures in an active comparator clinical trial.

Keywords: Malarone; Plasmodium falciparum; atovaquone-proguanil; cytochrome b; deep sequencing; drug resistance; malaria.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antimalarials* / therapeutic use
  • Atovaquone / therapeutic use
  • Cambodia
  • Cytochromes b / genetics
  • Drug Combinations
  • Humans
  • Malaria, Falciparum* / drug therapy
  • Naphthoquinones* / therapeutic use
  • Plasmodium falciparum / genetics
  • Proguanil / therapeutic use

Substances

  • Antimalarials
  • Drug Combinations
  • Naphthoquinones
  • atovaquone, proguanil drug combination
  • Cytochromes b
  • Proguanil
  • Atovaquone