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 ChartsThese 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 |
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Guide to Malaria Pharmacology Comments |
Pyrimethamine was developed at the beginning of the 1950s and was part of the work that led to the 1988 Nobel Prize in Physiology or Medicine being awarded to Gertrude Elion and George Hitchings for their discoveries of "important principles for drug treatment" [3]. Resistance to the antifolate class of antimalarial drugs, including pyrimethamine, emerged soon after their clinical introduction and arisies from mutations in PfDHFR-TS [4]. Potential Target/Mechanism Of Action: Pyrimethamine inhibits Plasmodium dihydrofolate reductase-thymidylate synthase (DHFR-TS). |