Clinical utility of tafenoquine in the prevention of relapse of Plasmodium vivax malaria: a review on the mode of action and emerging trial data

Infection and Drug Resistance
Aurore B HounkpatinJana Held

Abstract

Tafenoquine is an 8-aminoquinoline with activity against all human life cycle stages of Plasmodium vivax, including dormant liver stages - so called hypnozoites. Its long half-life of ~15 days is allowing for a single exposure regimen. It has been under development since 1980 and received approval by the US Food and Drug Administration in summer 2018 as an anti-relapse drug for P. vivax malaria in patients aged 16 years and older and for prophylaxis of malaria caused by any Plasmodium species in adults. Prior to tafenoquine administration, glucose-6-phosphate dehydrogenase (G6PD) deficiency needs to be excluded by testing. Individuals with a deficient G6PD activity are at risk of tafenoquine-induced hemolysis - as is the case for primaquine, the mainstay drug for P. vivax radical cure. A wealth of clinical studies have been conducted and are still ongoing to assess the safety, tolerability, and efficacy of tafenoquine. This review focuses on data emerging from the latest clinical trials on P. vivax radical cure with tafenoquine, the key studies for regulatory approval of tafenoquine, and elucidates the latest hypothesis on the mode of action.

Citations

Nov 29, 2019·Journal of Travel Medicine·Jelena LewisJeff Goad
Jul 7, 2019·Scientific Reports·Tamirat Gebru WoldearegaiJana Held
Jun 24, 2020·Malaria Journal·Pradeep A SubramaniVaradharajan Sundaramurthy
Feb 20, 2020·Biochemistry·Kuan-Yi Lu, Emily R Derbyshire
May 1, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Lais Pessanha de CarvalhoJana Held

Methods Mentioned

BETA
genotyping
flow cytometry

Clinical Trials Mentioned

NCT01376167
NCT02216123
NCT02658435
NCT02802501
NCT02563496
NCT02488980
NCT03320174

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