TABLE 1.
In vivo efficacy of antimalarials, including BH267.meta, against P. berghei
| Compounda | Dosing regimen (mg kg−1 day−1)b |
||||||||
|---|---|---|---|---|---|---|---|---|---|
| 30 |
10 |
3 |
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| Activity (%) | Survival (d) | Parasite-free mice (n/total) | Activity (%) | Survival (d) | Parasite-free mice (n/total) | Activity (%) | Survival (d) | Parasite-free mice (n/total) | |
| Chloroquine | 99.9 | 21.2 | - | 99.9 | 15.5 | - | 99.0 | 11.0 | - |
| Mefloquine | 99.9 | 29.1 | 4/5 | 99.9 | 21.0 | 1/5 | 93.0 | 13.0 | - |
| Artesunate | 99.0 | 9.2 | - | 99.1 | 8.1 | - | 85.0 | 8.8 | - |
| BH267.meta | 99.8 | 13.0 | - | 99.9 | 10.7 | - | 99.7 | 8.0 | - |
a
BH267.meta was dissolved (3 mg kg−1 dose) or suspended (all higher doses) in 70/30 Tween 80/ethanol diluted 10-fold with water. The control compounds chloroquine, artesunate, and mefloquine were dissolved or suspended in a non-solubilizing, standard suspension vehicle (0.5% [wt/vol] carboxymethylcellulose, 0.5% [vol/vol] benzyl alcohol, 0.4% [vol/vol] Tween 80, and 0.9% [wt/vol] NaCl in water).
b
Once per day on 4 consecutive days (4, 24, 48, and 72 h after infection; n = 3; LOQ = 0.1%). Mice with <40 parasitemia reduction were euthanized on day 4 in order to prevent death that would otherwise occur on day 6.