.Pharmacolibrary.Drugs.P_AntiparasiticProductsInsecticidesAndRepellents.P01B_Antimalarials.P01BA07_Tafenoquine.Tafenoquine

Information

Tafenoquine is an 8-aminoquinoline antimalarial drug used for the radical cure (prevention of relapse) and prophylaxis of Plasmodium vivax malaria. It is administrated orally and approved by regulatory authorities such as the US FDA for this indication. Its mechanism of action involves the inhibition of the parasite's mitochondrial electron transport.

Pharmacokinetics

Pharmacokinetic parameters reported for healthy adult subjects (both male and female) following a single oral dose administration.

References

1. Thakkar, N, et al., & Goyal, N (2018). Population Pharmacokinetics of Tafenoquine, a Novel Antimalarial. Antimicrobial agents and chemotherapy 62(11) –. DOI:10.1128/AAC.00711-18 PUBMED:https://pubmed.ncbi.nlm.nih.gov/30201820

2. Edstein, MD, et al., & Charles, BG (2001). Population pharmacokinetics of the new antimalarial agent tafenoquine in Thai soldiers. British journal of clinical pharmacology 52(6) 663–670. DOI:10.1046/j.0306-5251.2001.01482.x PUBMED:https://pubmed.ncbi.nlm.nih.gov/11736877

3. Vélez, ID, et al., & Goyal, N (2022). Tafenoquine exposure assessment, safety, and relapse prevention efficacy in children with Plasmodium vivax malaria: open-label, single-arm, non-comparative, multicentre, pharmacokinetic bridging, phase 2 trial. The Lancet. Child & adolescent health 6(2) 86–95. DOI:10.1016/S2352-4642(21)00328-X PUBMED:https://pubmed.ncbi.nlm.nih.gov/34871570

Revisions

• 06/2025 initial generated model