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Atovaquone / Proguanil

Radboud University Medical Center · FDA-approved active Small molecule

Atovaquone inhibits parasite mitochondrial electron transport while proguanil inhibits dihydrofolate reductase, together disrupting nucleotide synthesis and energy production in malaria parasites.

Atovaquone inhibits parasite mitochondrial electron transport while proguanil inhibits dihydrofolate reductase, together disrupting nucleotide synthesis and energy production in malaria parasites. Used for Malaria prophylaxis in travelers to endemic areas, Acute uncomplicated malaria treatment.

At a glance

Generic nameAtovaquone / Proguanil
SponsorRadboud University Medical Center
Drug classAntimalarial combination
TargetMitochondrial electron transport chain (atovaquone); dihydrofolate reductase (proguanil)
ModalitySmall molecule
Therapeutic areaInfectious Disease
PhaseFDA-approved

Mechanism of action

Atovaquone acts as an ubiquinone analog that disrupts the mitochondrial electron transport chain in Plasmodium species, collapsing the proton gradient needed for ATP synthesis. Proguanil is a prodrug converted to cycloguanil, which inhibits dihydrofolate reductase and blocks folate-dependent nucleotide synthesis. The combination provides synergistic activity against both erythrocytic and exoerythrocytic stages of the parasite.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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