TABLE 3.
QN254 antimalarial activity in the P. berghei murine malaria modela
| Dosing regimen (agent and dose [mg/kg])b | Parasitemia reduction (%) | Avg mouse survival (days) | Cure rate (%) | Toxicity rate (%)c |
|---|---|---|---|---|
| QN254 | ||||
| 1 × 10 | 59 | 6.0 | 0 | 0 |
| 1 × 15 | 73 | 6.0 | 0 | 0 |
| 1 × 30 | >99.99 | 8.1 | 0 | 0 |
| 1 × 60 | >99.99 | 12.0 | 0 | 0 |
| 1 × 100 | >99.99 | 23.4 | 50 | 0 |
| 3 × 30 | >99.99 | 28.4 | 80 | 0 |
| 3 × 60 | >99.99 | NAd | 60 | 40* |
| 3 × 100 | >99.99 | NA | 20 | 80* |
| Artesunate | ||||
| 1 × 100 | 98 | 7.0 | 0 | 0 |
| 3 × 30 | 98.7 | 12.2 | 0 | 0 |
| Chloroquine | ||||
| 1 × 100 | 99.6 | 12.5 | 0 | 0 |
| 3 × 30 | 99.8 | 14.3 | 0 | 0 |
| Mefloquine | ||||
| 1 × 100 | 89 | 25.5 | 0 | 0 |
| 3 × 30 | 98.8 | 22.1 | 0 | 0 |
a
Results represent the percent inhibition of parasitemia compared to untreated controls. QN254 was prepared in 0.5% carboxymethyl cellulose. The mean survival of control animals was 5.6 to 6.2 days.
b
The solution formulation for artesunate, chloroquine, and mefloquine consisted of 10% ethanol, 30% PEG 400 (polyethylene glycol 400), and 60% of a 10% vitamin-ETPGS solution.
c
*, Mice died around day 10 and were parasite-free. There were 10 mice per test group except for the “3 ×” treatment with QN254 because of ethical reasons due to the observed toxicity.
d
NA, not available.