Drug intelligence / Profile preview

tafenoquine

Development stage
Approved
Lead developer
GSK
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tafenoquine is an oral antimalarial drug belonging to the 8-aminoquinoline class, structurally related to primaquine. It is used for both the prevention and radical cure (prevention of relapse) of malaria, particularly caused by Plasmodium vivax. Tafenoquine acts against multiple stages of the malaria parasite lifecycle, including liver (pre-erythrocytic), blood (asexual), gametocyte forms, and notably the dormant hypnozoite stage responsible for relapses. Its long half-life allows for single-dose therapy in radical cure settings. The precise molecular mechanism is not fully established but involves redox cycling that disrupts parasite metabolism and survival in both hepatic and erythrocytic stages[1][3][5][10]. Tafenoquine was discovered at Walter Reed Army Institute of Research in 1978 and further developed by GlaxoSmithKline in collaboration with Medicines for Malaria Venture[3][4].

Brand names
ArakodaKrintafel
Other names
tafenoquine succinate
02

Targets

SLC47A1 (Multidrug and toxin extrusion transporter 1)OCT2 (Organic cation transporter 2)

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