Tafenoquine is an antiparasitic agent used for the treatment and prevention of relapse of Vivax malaria. Tafenoquine is an 8-aminoquinoline analogue of primaquine which varies only on the presence of a 5-phenoxy group.
- Mechanism
- Curator reviewed · 3 references
The mechanism of action of tafenoquine is not well established but studies have reported a longer and more effective action when compared to primaquine. The active moiety of tafenoquine, 5,6 ortho quinone tafenoquine, seems to be redox cycled by P. falciparum which are upregulated in gametocytes and liver stages. Once inside, the oxidated metabolite produces hydrogen peroxide and hydroxyl radicals. It is thought that these radicals produce leads to the parasite death.
On the other hand, tafenoquine inhibits heme polymerase in blood stage of parasites which explains the activity against blood stages of parasites.
- Primary indication
- Tafenoquine is used for the treatment and prevention of relapse of Vivax malaria in patients 16 years and older.Curator reviewed · 1 structured indication
- Formula / weight
- C24H28F3N3O3 · 463.501 g/mol (avg)
- First approval
- United States, 2018
- Code names
- SB 252263 · SB-252263-AAB
- Brand names
Resolves to
LBHLFPGPEGDCJG-UHFFFAOYSA-NSMILESCOC1=CC(C)=C2C(OC3=CC=CC(=C3)C(F)(F)F)=C(OC)C=C(NC(C)CCCN)C2=N1What you can answer from here — as of September 23, 2026
Which drugs share a target with Tafenoquine, and which of those have an active Phase 3 trial?
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