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Drug intelligence / Profile preview
artesunate + pyronaridine + atovaquone + proguanil
- Development stage
- Unknown
- Lead developer
- Bernhard Nocht Institute for Tropical Medicine
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Artesunate + pyronaridine + atovaquone + proguanil (APAP) is a novel four-drug antimalarial combination therapy being developed to treat uncomplicated *Plasmodium falciparum* malaria and combat the emergence and spread of drug resistance. The combination brings together the rapid-acting artemisinin derivative artesunate, the long-acting benzonaphthyridine derivative pyronaridine, the mitochondrial electron transport inhibitor atovaquone, and the folate synthesis inhibitor proguanil. By targeting multiple distinct biological pathways in the parasite simultaneously and matching the pharmacokinetic half-lives of the partner drugs, the APAP regimen aims to prevent the selection of resistant mutants and provide high cure rates. In a Phase II clinical trial (MultiMal) conducted in Gabon and Ghana, the APAP regimen was shown to be safe, well-tolerated, and highly efficacious.
- Other names
- APAPAPAP regimenartesunate-pyronaridine-atovaquone-proguanilartesunate-pyronaridine-atovaquone/proguanil
02
Targets
DHFR-TS (Bifunctional dihydrofolate reductase-thymidylate synthase)Heme
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