Table 1 The causal prophylactic activities of tafenoquine (TQ) and primaquine (PQ) by using real time in vivo image system (IVIS) following single dose (-1 or 0 day after inoculation) or daily oral administrations for 3 days multiple doses (-1, 0, and 1 day after infection) against challenge with 50,000 sporozoites of the ANKA strain of P. berghei intravenously in male C57BL/6 albino mice with positive and negative controls (n = 5–20 each)
Test agents | Dose (mg/kg) | Oral dose | Date of dosing | Suppression rate (%) IVIS* | Blood Infection by FCM* | Number of C57BL/albino mice | Delay in patency (days after onset in controls) | Effects | ||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
24 h | 48 h | 72 h | Challenged | Protected completely | Causal prophylaxis | |||||||
Tafenoquine | 10 | 3 days | -1, 0, 1 | 100 | 100 | 100 | 0/5 | 5 | 5 | 5/5 | - | Full CP |
5 | 3 days | -1, 0, 1 | 90.4 | 100 | 100 | 0/13 | 13 | 13 | 13/13 | - | Full CP | |
2.5 | 3 days | -1, 0, 1 | 100 | 100 | 100 | 2/5 | 5 | 3 | 3/5 | - | Partial CP | |
1.25 | 3 days | -1, 0, 1 | 84.7 | 92.3 | 98.9 | 4/5 | 5 | 1 | 1/5 | 2,4,4,7 | Suppression | |
5 | Single | -1 | 68.7 | 98.6 | 100 | 0/10 | 10 | 10 | 10/10 | - | Full CP | |
5 | Single | 0 | 66.0 | 91.1 | 98.5 | 4/5 | 5 | 1 | 1/5 | 4,2,4,9 | Partial CP | |
Primaquine | 25 | 3 days | -1, 0, 1 | 100 | 100 | 100 | 0/10 | 10 | 10 | 10/10 | - | Full CP |
20 | 3 days | -1, 0, 1 | 100 | 100 | 100 | 1/10 | 10 | 9 | 9/10 | 6 | Partial CP | |
15 | 3 days | -1, 0, 1 | 100 | 100 | 100 | 4/20 | 20 | 16 | 16/20 | 2,2,2,1 | Partial CP | |
10 | 3 days | -1, 0, 1 | 100 | 97.6 | 100 | 5/10 | 10 | 5 | 5/10 | 2,4,2,2,4 | Partial CP | |
5 | 3 days | -1, 0, 1 | 82.4 | 77.5 | 89.4 | 5/5 | 5 | 0 | 0/5 | 2,2 | Suppression | |
25 | Single | -1 | 45.7 | 0 | 0 | 5/5 | 5 | 0 | 0/5 | - | Suppression | |
25 | Single | 0 | 11.2 | 0 | 0 | 5/5 | 5 | 0 | 0/5 | - | Suppression | |