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Synonyms: Aczone® | NSC-6091
dapsone is an approved drug (FDA (1979), UK (1988))
Compound class: Synthetic organic
Comment: Dapsone is a sulfonamide-related antibacterial, antimalarial and anti-inflammatory drug. In bacteria it inhibits dihydropteroate synthase-mediated production of folic acid, which has the effect of disrupting the availability of thymidylate for DNA synthesis.
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|Guide to Malaria Pharmacology Comments|
|Dapsone was used by the US Army during the Vietnam War as a prophylactic agent for malaria but was subsequently replaced by mefloquine . The spread of Plasmodium strains resistant to existing antimalarial drugs, led to the introduction of a combination therapy containing chlorproguanil and dapsone (marketed as LapDap™). This formulation was withdrawn in 2008 following concerns about haemolytic anaemia in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency . A combined prophylactic medicine with pyrimethamine (Maloprim®) has also been withdrawn in many jurisdictions .
Potential Target/Mechanism Of Action: dapsone is an inhibitor of P. falciparum hydroxymethyldihydropterin pyrophosphokinase-dihydropteroate synthase (PfPPPK-DHPS) .