Table 3.
Tafenoquine (TQ) wild-type (WT) dose-ranging studies using C57BL/6 mice
| Day dose administereda | PQ dose (mg/kg) | No hepatic IVIS signalb | No asexual erythrocytic infection (parasitemia)c | No sexual erythrocytic infection (gametocytemia)c |
|---|---|---|---|---|
| Causal prophylactic model | ||||
| D1 | 2.5 | 0/5 (D1), 0/5 (D2) | 0/5 | NA |
| 5 | 3/5 (D1), 2/5 (D2) | 0/5 | NA | |
| 10 | 5/5 (D1), 5/5 (D2) | 4/5 | NA | |
| 20 | 5/5 (D1), 5/5 (D2) | 5/5 | NA | |
| D0 | 2.5 | 0/5 (D1), 0/5 (D2) | 0/5 | NA |
| 5 | 4/5 (D1), 4/5 (D2) | 3/5 | NA | |
| 10 | 3/5 (D1), 4/5 (D2) | 2/5 | NA | |
| 20 | 5/5 (D1), 5/5 (D2) | 5/5 | NA | |
| D1 | 20 | 0/5 (D1), 0/5 (D2) | 5/5 | NA |
| Erythrocytic treatment model | ||||
| D4 | 5 | NA | 0/5 | 0/5 |
| 10 | NA | 0/5 | 0/5 | |
| 20 | NA | 4/5 | 4/5 | |
TQ tafenoquine, mg/kg milligrams free base of drug per kg body weight, NA not applicable, IVIS in vivo imaging system
aDay of drug administration relative to intravenous sporozoite (IV SPZ) challenge (day 0) using C57BL/6 wild-type mice
bNumber of animals without an IVIS signal (indicates no hepatic infection). D1 = day 1 (relative to IV SPZ challenge day 0). D2 = day 2 (relative to IV SPZ challenge day 0)
cNumber of animals without parasitemia (flow cytometry) or gametocytemia (microscopy) day 29. N = 5 animals per cohort