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Drug intelligence / Profile preview
artemether-lumefantrine + atovaquone-proguanil
- Development stage
- Unknown
- Lead developer
- Bernhard Nocht Institute for Tropical Medicine
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
artemether-lumefantrine + atovaquone-proguanil is an experimental triple-therapy antimalarial regimen (triple artemisinin-based combination therapy, or T-ACT) being developed to treat uncomplicated *Plasmodium falciparum* malaria and mitigate the risk of artemisinin resistance in sub-Saharan Africa. The regimen combines the standard artemisinin-based combination therapy (ACT) artemether-lumefantrine (AL) with atovaquone-proguanil (AP). Artemether is an artemisinin derivative that induces heme-activated radical damage to parasite proteins. Lumefantrine is a long-acting partner drug that inhibits heme detoxification. Atovaquone is a mitochondrial electron transport inhibitor targeting the cytochrome bc1 complex, and proguanil (via its active metabolite cycloguanil) inhibits dihydrofolate reductase. This combination is being evaluated in Phase II and Phase III clinical trials (such as the ASAAP project) in African children, adolescents, and adults to assess its safety, tolerability, efficacy, and transmission-blocking potential.
- Other names
- AL+APAL-APartemether + lumefantrine + atovaquone + proguanilartemether-lumefantrine and atovaquone-proguanilartemether-lumefantrine plus atovaquone-proguanilASAAP tri-therapyASAAP triple therapy
02
Targets
CYTB (Plasmodium falciparum cytochrome bc1 complex (qi site))DHFR (Dihydrofolate reductase)
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