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Synonyms: Arakoda® | etaquine | Krintafel® | WR238605
tafenoquine is an approved drug (FDA (2018))
Compound class: Synthetic organic
Comment: Tafenoquine is an 8-aminoquinoline derivative that has potent antimalarial activity and is a synthetic analogue of primaquine.
The INN record for tafenoquine indicates that it is a racemic mixture. We show the chemical structure without stereochemistry to represent the mixture. The non-isomeric structure is also represented in the PubChem and ChEMBL entries listed in the links table below, while the two enantiomers forming the racemate are represented by PubChem CID 76969187 and PubChem CID 76969188.
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|
|Tafenoquine was identified by researchers at the Walter Reed Army Institute of Research during an antimalarial drug discovery programme that ran from 1963 until the late 1970s. It is, with primaquine, one of only two licensed drugs available for terminal prophylaxis to prevent relapse or delayed-onset clinical presentation of P. vivax malaria. Tafenoquine has a significantly longer elimination half-life than primaquine and is the first drug to be approved for single-dose treatment of relapsing P. vivax malaria.
The compound was awarded MMV Project of the Year (2013).
Potential Target/Mechanism Of Action: As the precise mechanism of action of tafenoquine is not yet known, we do not have a molecular target for this compound.
|Target Candidate Profiles|
|Profile||Intended Use||Target Stage||Comment||References|
|TCP-3||prevention of relapse||hypnozoites|