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Chemical Compound Review

Tafenoquine     N-[2,6-dimethoxy-4-methyl-5- [3...

Synonyms: CHEMBL298470, SureCN347388, AC1L3GZN, LS-172012, WR-238605, ...
 
 
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Disease relevance of AIDS006901

 

High impact information on AIDS006901

 

Chemical compound and disease context of AIDS006901

 

Biological context of AIDS006901

  • First-time-in-humans safety and pharmacokinetics of WR 238605, a new antimalarial [11].
  • The metabolism of WR 238605 involved the expected metabolic pathways, such as O-demethylation, N-dealkylation, N-oxidation, and oxidative deamination [12].
  • This study was conducted to assess the in vitro blood schizontocidal activity of tafenoquine, the most advanced candidate drug of the 8-aminoquinolines, and of its 1:1 combination with artemisinin in fresh isolates of Plasmodium falciparum in an area with multi-drug resistance, measuring the inhibition of schizont maturation [13].
 

Anatomical context of AIDS006901

  • After incubation of WR 238605 with rat liver microsomes, the metabolites were isolated either by direct solvent extraction or by extraction in the presence of ethyl chloroformate [12].
  • Uptake of WR-238605 6 or 12 days after mosquitoes were infected with P. berghei had no effect on the percentage of mosquitoes with oocysts or the mean number of oocysts produced per mosquito [3].
  • Halofantrine, primaquine, WR-182393, and WR-238605 were ineffective at clearing P. berghei ANKA from circulating erythrocytes at the doses tested; however, mice survival time increased markedly with these compounds when compared with the controls [14].
  • A two-compartment pharmacokinetic model, linked to a sigmoid Emax pharmacodynamic model, was developed to predict the MHb levels after administration of 8-[(4-amino-1-methylbutyl)amino]-2,6-dimethoxy-4-methyl-5-[(3- trifluoromethyl)phenoxy] quinoline succinate (WR 238605 succinate), a primaquine analogue [15].
 

Associations of AIDS006901 with other chemical compounds

 

Analytical, diagnostic and therapeutic context of AIDS006901

References

  1. Randomized dose-ranging study of the safety and efficacy of WR 238605 (Tafenoquine) in the prevention of relapse of Plasmodium vivax malaria in Thailand. Walsh, D.S., Looareesuwan, S., Wilairatana, P., Heppner, D.G., Tang, D.B., Brewer, T.G., Chokejindachai, W., Viriyavejakul, P., Kyle, D.E., Milhous, W.K., Schuster, B.G., Horton, J., Braitman, D.J., Brueckner, R.P. J. Infect. Dis. (1999) [Pubmed]
  2. Prophylaxis of Plasmodium falciparum infection in a human challenge model with WR 238605, a new 8-aminoquinoline antimalarial. Brueckner, R.P., Coster, T., Wesche, D.L., Shmuklarsky, M., Schuster, B.G. Antimicrob. Agents Chemother. (1998) [Pubmed]
  3. Sporontocidal activity of the antimalarial WR-238605 against Plasmodium berghei ANKA in Anopheles stephensi. Coleman, R.E. Am. J. Trop. Med. Hyg. (1990) [Pubmed]
  4. WR 238605, chloroquine, and their combinations as blood schizonticides against a chloroquine-resistant strain of Plasmodium vivax in Aotus monkeys. Obaldia, N., Rossan, R.N., Cooper, R.D., Kyle, D.E., Nuzum, E.O., Rieckmann, K.H., Shanks, G.D. Am. J. Trop. Med. Hyg. (1997) [Pubmed]
  5. Blood schizontocidal activity of WR 238605 (Tafenoquine) against Plasmodium cynomolgi and Plasmodium fragile infections in rhesus monkeys. Puri, S.K., Dutta, G.P. Acta Trop. (2003) [Pubmed]
  6. Modern malaria chemoprophylaxis. Shanks, G.D., Edstein, M.D. Drugs (2005) [Pubmed]
  7. Efficacy of monthly tafenoquine for prophylaxis of Plasmodium vivax and multidrug-resistant P. falciparum malaria. Walsh, D.S., Eamsila, C., Sasiprapha, T., Sangkharomya, S., Khaewsathien, P., Supakalin, P., Tang, D.B., Jarasrumgsichol, P., Cherdchu, C., Edstein, M.D., Rieckmann, K.H., Brewer, T.G. J. Infect. Dis. (2004) [Pubmed]
  8. 8-Aminoquinolines from Walter Reed Army Institute for Research for treatment and prophylaxis of Pneumocystis pneumonia in rat models. Bartlett, M.S., Queener, S.F., Tidwell, R.R., Milhous, W.K., Berman, J.D., Ellis, W.Y., Smith, J.W. Antimicrob. Agents Chemother. (1991) [Pubmed]
  9. Malaria prophylaxis/radical cure: recent experiences of the Australian Defence Force. Edstein, M.D., Walsh, D.S., Eamsila, C., Sasiprapha, T., Nasveld, P.E., Kitchener, S., Rieckmann, K.H. Médecine tropicale : revue du Corps de santé colonial. (2001) [Pubmed]
  10. 8-Aminoquinolines: future role as antiprotozoal drugs. Tekwani, B.L., Walker, L.A. Curr. Opin. Infect. Dis. (2006) [Pubmed]
  11. First-time-in-humans safety and pharmacokinetics of WR 238605, a new antimalarial. Brueckner, R.P., Lasseter, K.C., Lin, E.T., Schuster, B.G. Am. J. Trop. Med. Hyg. (1998) [Pubmed]
  12. Metabolism of a candidate 8-aminoquinoline antimalarial agent, WR 238605, by rat liver microsomes. Idowu, O.R., Peggins, J.O., Brewer, T.G., Kelley, C. Drug Metab. Dispos. (1995) [Pubmed]
  13. In vitro activity of tafenoquine alone and in combination with artemisinin against Plasmodium falciparum. Ramharter, M., Noedl, H., Thimasarn, K., Wiedermann, G., Wernsdorfer, G., Wernsdorfer, W.H. Am. J. Trop. Med. Hyg. (2002) [Pubmed]
  14. Gametocytocidal and sporontocidal activity of antimalarials against Plasmodium berghei ANKA in ICR Mice and Anopheles stephensi mosquitoes. Coleman, R.E., Clavin, A.M., Milhous, W.K. Am. J. Trop. Med. Hyg. (1992) [Pubmed]
  15. Simultaneous modeling of the pharmacokinetics and methemoglobin pharmacodynamics of an 8-aminoquinoline candidate antimalarial (WR 238605). Brueckner, R.P., Fleckenstein, L. Pharm. Res. (1991) [Pubmed]
  16. Randomized trial of 3-dose regimens of tafenoquine (WR238605) versus low-dose primaquine for preventing Plasmodium vivax malaria relapse. Walsh, D.S., Wilairatana, P., Tang, D.B., Heppner, D.G., Brewer, T.G., Krudsood, S., Silachamroon, U., Phumratanaprapin, W., Siriyanonda, D., Looareesuwan, S. Clin. Infect. Dis. (2004) [Pubmed]
  17. Malaria chemoprophylaxis with tafenoquine: a randomised study. Lell, B., Faucher, J.F., Missinou, M.A., Borrmann, S., Dangelmaier, O., Horton, J., Kremsner, P.G. Lancet (2000) [Pubmed]
  18. Evaluation of selected antiprotozoal drugs in the Babesia microti-hamster model. Marley, S.E., Eberhard, M.L., Steurer, F.J., Ellis, W.L., McGreevy, P.B., Ruebush, T.K. Antimicrob. Agents Chemother. (1997) [Pubmed]
  19. Population pharmacokinetics of the new antimalarial agent tafenoquine in Thai soldiers. Edstein, M.D., Kocisko, D.A., Brewer, T.G., Walsh, D.S., Eamsila, C., Charles, B.G. British journal of clinical pharmacology. (2001) [Pubmed]
  20. Measurement of tafenoquine (WR 238605) in human plasma and venous and capillary blood by high-pressure liquid chromatography. Kocisko, D.A., Walsh, D.S., Eamsila, C., Edstein, M.D. Therapeutic drug monitoring. (2000) [Pubmed]
 
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