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Drug intelligence / Profile preview
artesunate + atovaquone + proguanil
- Development stage
- Phase 4
- Lead developer
- Liu Xu
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Artesunate + atovaquone + proguanil is a triple combination antimalarial therapy used primarily for the treatment of uncomplicated and multidrug-resistant *Plasmodium falciparum* malaria. Artesunate is an artemisinin derivative that rapidly reduces parasite biomass by generating reactive oxygen species within infected erythrocytes. Atovaquone inhibits the mitochondrial electron transport chain in the parasite, while proguanil acts as a dihydrofolate reductase inhibitor, disrupting folate synthesis essential for DNA replication. The combination aims to enhance efficacy and reduce resistance development; however, studies indicate that adding artesunate to atovaquone-proguanil provides little additional blood-stage efficacy but does reduce post-treatment gametocyte carriage compared to dual therapy[1][2][3]. The regimen has been well tolerated in clinical trials[3].
- Other names
- artesunate plus atovaquone-proguanilASAP
02
Targets
DHFR-TS (Bifunctional dihydrofolate reductase-thymidylate synthase)Neuraminidasebc1 complex (Cytochrome bc1 complex (plasmodium))
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