• 1

    Kremsner P, Krishna S, 2004. Antimalarial combinations. Lancet 364 :285–294.

  • 2

    Woodrow CJ, Haynes RK, Krishna S, 2005. Artemisinins. Postgrad Med J 81 :71–78.

  • 3

    Vennerstrom J, Arbe-Barnes S, Brun R, Charman S, Chlu F, Chollet J, Dong Y, Dorn A, Hunziker D, Matile H, McIntosh K, Padmanilayam M, Santo-Tomas J, Scheurer C, Scorneaux B, Tang Y, Urwyler H, Wittlin S, Charman W, 2004. Identification of an antimalarial synthetic trioxolane drug development candidate. Nature 430 :900–904.

    • Search Google Scholar
    • Export Citation
  • 4

    Churchill F, 1989. Field adapted assays for chloroquine and its metabolites in urine and blood. Parasitol Today 5: 116, 121–126.

  • 5

    Desjardins RE, Canfield CJ, Haynes JD, Chulay JD, 1979. Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique. Antimicrob Agents Chemother 16 :710–718.

    • Search Google Scholar
    • Export Citation
  • 6

    Huber W, Koella J, 1993. A comparison of three methods of estimating EC50 in studies of drug resistance of malaria parasites. Acta Trop 55 :257–261.

    • Search Google Scholar
    • Export Citation
  • 7

    Kreidenweiss A, Mordmüller B, Krishna S, Kremsner PG, 2006. Antimalarial activity of a synthetic endoperoxide (RBx-11160/ OZ277) against Plasmodium falciparum isolates from Gabon. Antimicrob Agents Chemother 50 :1535–1537.

    • Search Google Scholar
    • Export Citation
  • 8

    Basco L, 2004. Molecular epidemiology of malaria in Cameroon. XX. Experimental studies on various factors of in vitro drug sensitivity assays using fresh isolates of Plasmodium falciparum.Am J Trop Med Hyg 70 :474–480.

    • Search Google Scholar
    • Export Citation
  • 9

    Verdier F, Le Bras J, Clavier F, Hatin I, Blayo M-C, 1985. Chloroquine uptake by Plasmodium falciparum-infected human erythrocytes during in vitro culture and its relationship to chloroquine resistance. Antimicrob Agents Chemother 27 :561–564.

    • Search Google Scholar
    • Export Citation
  • 10

    Vyas N, Avery B, Avery M, Wyandt C, 2002. Carrier-mediated partitioning of artemisinin into Plasmodium falciparum-infected erythrocytes. Antimicrob Agents Chemother 46 :105–109.

    • Search Google Scholar
    • Export Citation
  • 11

    Gu H, Warhurst D, Peters W, 1984. Uptake of [3H]dihydroartemisinin by erythrocytes infected with Plasmodium falciparum in vitro. Trans R Soc Trop Med Hyg 78 :265–270.

    • Search Google Scholar
    • Export Citation
  • 12

    Maerki S, Brun R, Charman S, Dorn A, Matile H, Wittlin S, 2006. In vitro assessment of the pharmacodynamic properties and the partitioning of OZ277/RBx-11160 in cultures of Plasmodium falciparum.J Antimicrob Chemother 58 :52–58.

    • Search Google Scholar
    • Export Citation
  • 13

    Cerutti C Jr, Marques C, Alencar FE, Durlacher RR, Alween A, Segurado AA, Pang LW, Zalis MG, 1999. Antimalarial drug susceptibility testing of Plasmodium falciparum in Brazil using a radioisotope method. Mem Inst Oswaldo Cruz 94 :803–809.

    • Search Google Scholar
    • Export Citation
  • 14

    Akoachere M, Buchholz K, Fischer E, Burhenne J, Haefeli W, Schirmer R, Becker K, 2005. In vitro assessment of methylene blue on chloroquine-sensitive and -resistant Plasmodium falciparum strains reveals synergistic action with artemisinins. Antimicrob Agents Chemother 49 :4592–4597.

    • Search Google Scholar
    • Export Citation
  • 15

    Brockman A, Price R, van Vugt M, Heppner D, Walsh D, Sookto P, Wimonwattrawatee T, Looareesuwan S, White N, Nosten F, 2000. Plasmodium falciparum antimalarial drug susceptibility on the north-western border of Thailand during five years of extensive use of artesunatemefloquine. Trans R Soc Trop Med Hyg 94 :537–544.

    • Search Google Scholar
    • Export Citation
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

 

 

 

IN VITRO SUSCEPTIBILITY OF P. FALCIPARUM POPULATIONS FROM COLOMBIA AND TANZANIA TO A NEW SYNTHETIC PEROXIDE (OZ277)

View More View Less
  • 1 International Center for Medical Research and Training (CIDEIM), Cali, Colombia; Ifakara Health Research & Development, Ifakara, Tanzania; Swiss Tropical Institute (STI), Basel, Switzerland; F. Hoffmann-La Roche Ltd., Basel, Switzerland
Restricted access

Sensitivity of Plasmodium falciparum populations from Colombia (N = 38) and Tanzania (N = 45) to the newly developed, fully synthetic peroxide OZ277 was investigated using a standard isotopic microtest. OZ277 showed excellent activity against chloroquine-resistant isolates in Colombia with median IC50 [range] values of 2.5 ng/mL [0.34–8] (4.4 nM [0.6–14]) and Tanzania with 1.5 ng/mL [0.22–10] (2.65 nM [0.4–17.7]). The potency of OZ277 was similar to artesunate, showing median IC50 values of 1.5 ng/mL [0.42–8.6] (3.8 nM [1.1–22.3]) and 1.8 ng/mL [0.2–10] (4.7 nM [0.5–26.04]) in Colombia and Tanzania, respectively. These results support the development of this new antimalarial compound.

Author Notes

Reprint requests: Lyda Osorio, CIDEIM Avenida 1 Norte #3-03 Cali, Colombia.
Save