Tafenoquine

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Tafenoquine
Systematic (IUPAC) name
N-[2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)
phenoxy]quinolin-8-yl]pentane-1,4-diamine
Identifiers
CAS number 106635-80-7
ATC code  ?
PubChem 115358
Chemical data
Formula C24H28F3N3O3 
Mol. mass 463.493 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

Tafenoquine (also called WR-238605 or SB-252263) is an 8-aminoquinoline drug manufactured by GlaxoSmithKline that is currently being investigated as a potential treatment for malaria, as well as for malaria prevention.[1][2]

The main advantage of tafenoquine is that it has a long half-life and therefore does not need to be taken as frequently as primaquine. Like primaquine, tafenoquine causes haemolysis in people with G-6-PD deficiency.[1]

The dose of tafenoquine has not been firmly established, but for the treatment of Plasmodium vivax malaria, a dose of 800 mg over three days has been used.[3]

[edit] References

  1. ^ a b Shanks GD, Oloo AJ, Aleman GM, et al. (2001). "A New Primaquine Analogue, Tafenoquine (WR 238605), for prophylaxis against Plasmodium falciparum malaria.". Clin Infect Dis 33: 1968–74. 
  2. ^ Lell B, Faucher JF, Missinou MA, et al. (2000). "Malaria chemoprophylaxis with tafenoquine: a randomised study.". Lancet 355 (9220): 2041–5. PMID 10885356. 
  3. ^ Nasvelda P, Kitchener S. (2005). "Treatment of acute vivax malaria with tafenoquine.". Trans R Soc Trop Med Hyg 99 (1): 2–5. DOI:10.1016/j.trstmh.2004.01.013.