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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.✖
|No information available.|
|Summary of Clinical Use|
|The FDA has approved, under Priority Review, single-dose tafenoquine for the radical cure of P. vivax malaria in adults. The compound is not indicated for the treatment of acute P. vivax infection and should be coadministered with an appropriate antimalarial partner. Tafenoquine had previously been granted a Breakthrough Therapy designation by the FDA (December 2013), followed in November 2017 by the submission of a New Drug Application (NDA). The approval was based on efficacy and safety data from a number of clinical trials including the randomised, double-blind, Phase 2b/3 studies: DETECTIVE (NCT01376167 [2-3]) and GATHER (NCT02216123 ). Click here to link to ClinicalTrials.gov's complete list of tafenoquine trials. In August 2018, the FDA expanded tafenoquine's approval status to allow use of Arakoda® tablets as a once weekly prophylactic for the prevention of malaria infection in people aged 18 years and older.
Testing for glucose-6-phosphate dehydrogenase (G6PD) deficiency is required before administration because tafenoquine, like primaquine, causes haemolysis in genetically sensitive individuals .
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT01376167||Ph 2B/3 Tafenoquine (TFQ) Study in Prevention of Vivax Relapse||Phase 2 Interventional||GlaxoSmithKline|
|NCT02216123||Study to Assess the Incidence of Hemolysis, Safety, and Efficacy of Tafenoquine (SB-252263, WR238605) Versus Primaquine in Subjects With Plasmodium Vivax Malaria||Phase 3 Interventional||GlaxoSmithKline|
|The terminal half-life of elimination of tafenoquine is 14 days .|
For extended ADME data see the following: