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Synonyms: Daraprim® | GNF-Pf-5586 | TCMDC-125860
pyrimethamine is an approved drug (FDA (1953))
Compound class: Synthetic organic
Comment: Pyrimethamine is an antifolate compound with broad-spectrum antiprotozoal activity. It is used in the treatment and prevention of malaria as part of a combination therapy.
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.✖
View more information in the IUPHAR Pharmacology Education Project: pyrimethamine
|No information available.|
|Summary of Clinical Use|
|Pyrimethamine is used in the treatment of toxoplasmosis and acute malaria. Also used for the prevention of malaria in areas without resistance to pyrimethamine.
Pyrimethamine is listed in the World Health Organisation's 21st Essential Medicines List (2019) as a curative treatment for uncomplicated P. falciparum malaria in combination with sulfadoxine and artesunate. This is one of the artemisinin-based combination therapies (ACTs) recommended in the WHO's Guidelines for the treatment of malaria 
|Mechanism Of Action and Pharmacodynamic Effects|
|Interferes with the formation of malarial schizont in erthrocytes and the liver. This is via the inhibition of the dihydrofolate reductase-thymidylate synthase in plasmodia which blocks the biosynthesis of purines and pyrimidines, leading to failure of nuclear division.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)