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Synonyms: Aralen® | chloraquine | Malaquin®
chloroquine is an approved drug (FDA (1949), UK (2000))
Compound class: Synthetic organic
Comment: Chloroquine is a 4-aminoquinoline and used primarily as an antimalarial drug.
The approved drug is a racemic mixture and we show the chemical structure without stereochemistry to represent the mixture. The non-isomeric structure is also represented in the PubChem, ChEMBL and ChEBI entries listed in the links table below, while the two enantiomers forming the racemate are represented by PubChem CID 444810 and PubChem CID 639540. The PDB entry listed in the links table is for (R)-chloroquine.
Marketed formulations may contain chloroquine phosphate (PubChem CID 64927).
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.✖
|No information available.|
|Summary of Clinical Use|
|Chloroquine is one of the antimalarials listed in the World Health Organisation's 21st Essential Medicines List (2019), with its recommended use restricted to the prevention and treatment of P. vivax infection in areas where resistance has not yet developed.
It is also used off-label for other conditions/diseases, including treatment of autoimmune disorders (rheumatoid arthritis and lupus erythematosus), as an antiretroviral (HIV-1/AIDS and chikungunya fever) and as a radiosensitizing/chemosensitizing agent benefitting cancer therapies.
|Mechanism Of Action and Pharmacodynamic Effects|
|Chloroquine inhibits ferriprotoporphyrin IX (FP, a heme detoxifying enzyme) found in Plasmodium species. Chloroquine kills the malarial parasite by causing a build up of toxic heme by inhibiting the enzyme that normally converts it to non-toxic hamazion. Chloroquine may also form a complex with FP which is additionally highly toxic to the organism.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)