Compound name | Cmax (ng/mL)a
| Cmax (µM) | Unbound fraction | IC50 (µM) | DDI indexb
|
---|
Amodiaquine | 5.2c [45] | 0.015 | 0.1 [46] | 11 | 0.0001 |
Proguanil | 306d [47] | 1.2 | 0.25 [39] | 13 | 0.02 |
Pyrimethamine | 281e [48] | 1.1 | 0.06 [49] | 1.6 | 0.04 |
Quinine | 11430f [50] | 35 | 0.11g [36] | 3.4 | 1.1 |
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a(Geometric) mean or median maximum plasma concentrations as determined in in vivo pharmacokinetic studies
-
bDDI index calculated by dividing the unbound Cmax by the IC50 concentration. A DDI index cut-off value ≥ 0.1 is believed to indicate the requirement for future in vivo pharmacokinetic studies [18]
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cIn Ugandan children aged 5–13 years with uncomplicated malaria
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dIn Thai children with uncomplicated multidrug-resistant falciparum malaria
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eIn patients with acute falciparum malaria
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fIn adult patients with uncomplicated falciparum malaria
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gIn Thai patients with falciparum malaria