Drug intelligence / Profile preview

chloroquine + tafenoquine

Development stage
Phase 4
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Chloroquine + tafenoquine is a combination of two antimalarial drugs used primarily for the radical cure and prevention of malaria, especially caused by *Plasmodium vivax*. Chloroquine is a 4-aminoquinoline that interferes with the growth of malaria parasites in red blood cells, while tafenoquine is an 8-aminoquinoline that targets both blood and liver stages (including dormant hypnozoites) of the parasite. Tafenoquine requires metabolic activation, likely involving cytochrome P450 enzymes such as CYP2D6, to exert its antiplasmodial effects. This combination is indicated for patients aged 16 years or older to prevent relapse after initial treatment with chloroquine[1][2][5][6][8]. Tafenoquine has a long half-life and can be given as a single dose for radical cure.

02

Targets

PfLDH (Plasmodium falciparum lactate dehydrogenase)CYP2D6 (Cytochrome P450 2D6)

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