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Chemical Compound Review

Wellvone     3-[4-(4- chlorophenyl)cyclohexyl]-4- hydroxy...

Synonyms: Malarone, ATOVAQUONE, Acuvel, Mepron, pron, ...
 
 
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Disease relevance of Mepron

 

High impact information on Mepron

 

Chemical compound and disease context of Mepron

 

Biological context of Mepron

 

Anatomical context of Mepron

 

Associations of Mepron with other chemical compounds

 

Gene context of Mepron

  • Atovaquone inhibits the bc1 complex competitively with apparent Ki = 9 nm, raises the midpoint potential of the Rieske iron-sulfur protein from 285 to 385 mV, and shifts the g values in the EPR spectrum of the Rieske center [23].
  • No synergy could be demonstrated between atovaquone and DHFR inhibitors or macrolides [27].
  • Using uptake of 3H-vinblastine in L-MDR1 cells, atovaquone was shown to inhibit P-glycoprotein with an apparent Ki of 95.6 microM [28].
  • CONCLUSIONS: Atovaquone is a relatively weak inhibitor of CYP2C9-mediated SMX-HA formation in vitro [29].
  • RESULTS: No in vitro atovaquone resistance (IC50 > 1900 nM) and no cytb mutation leading to the Y268S substitution were detected among 477 unexposed African P. falciparum isolates [30].
 

Analytical, diagnostic and therapeutic context of Mepron

References

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  16. Recapitulation in Saccharomyces cerevisiae of cytochrome b mutations conferring resistance to atovaquone in Pneumocystis jiroveci. Hill, P., Kessl, J., Fisher, N., Meshnick, S., Trumpower, B.L., Meunier, B. Antimicrob. Agents Chemother. (2003) [Pubmed]
  17. Mutations in Plasmodium falciparum cytochrome b that are associated with atovaquone resistance are located at a putative drug-binding site. Korsinczky, M., Chen, N., Kotecka, B., Saul, A., Rieckmann, K., Cheng, Q. Antimicrob. Agents Chemother. (2000) [Pubmed]
  18. Atovaquone as long-term suppressive therapy for toxoplasmic encephalitis in patients with AIDS and multiple drug intolerance. Atovaquone Expanded Access Group. Katlama, C., Mouthon, B., Gourdon, D., Lapierre, D., Rousseau, F. AIDS (1996) [Pubmed]
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  24. Prophylaxis for human immunodeficiency virus-related Pneumocystis carinii pneumonia: using simulation modeling to inform clinical guidelines. Goldie, S.J., Kaplan, J.E., Losina, E., Weinstein, M.C., Paltiel, A.D., Seage, G.R., Craven, D.E., Kimmel, A.D., Zhang, H., Cohen, C.J., Freedberg, K.A. Arch. Intern. Med. (2002) [Pubmed]
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  28. The effect of atovaquone on etoposide pharmacokinetics in children with acute lymphoblastic leukemia. van de Poll, M.E., Relling, M.V., Schuetz, E.G., Harrison, P.L., Hughes, W., Flynn, P.M. Cancer Chemother. Pharmacol. (2001) [Pubmed]
  29. Inhibition by atovaquone of CYP2C9-mediated sulphamethoxazole hydroxylamine formation. Miller, J.L., Trepanier, L.A. Eur. J. Clin. Pharmacol. (2002) [Pubmed]
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  31. Single-dose and steady-state pharmacokinetics of a novel microfluidized suspension of atovaquone in human immunodeficiency virus-seropositive patients. Dixon, R., Pozniak, A.L., Watt, H.M., Rolan, P., Posner, J. Antimicrob. Agents Chemother. (1996) [Pubmed]
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