Table 3.
In vitro and in vivo antitrypanosomal activity of DB829 and pentamidine against different T. brucei strains
| Organism and drug regimen (no. of doses × mg/kg i.p.) | DB829 |
Pentamidine |
||
|---|---|---|---|---|
| Mean IC50 ± SD (nM) | No. cured/no. infected (MRDa) | Mean IC50 ± SD (nM) | No. cured/no. infected (MRD) | |
| T. b. rhodesiense STIB900b | 20 ± 4 | 3 ± 0.8 | ||
| 1 × 5 | 2/4 (53.5) | NDd | ||
| 1 × 20 | 4/4 | 2/4 (22.5) | ||
| 4 × 5 | 4/4 | 1/4 (23) | ||
| 4 × 20 | ND | 2/4 (28.5) | ||
| T. b. gambiense ITMAP141267 | 69 ± 17 | 6 ± 1.2 | ||
| 1 × 5 | 3/3c | 3/4c (48) | ||
| 1 × 20 | 4/4 | 4/4 | ||
| 4 × 5 | 4/4 | 4/4 | ||
| 4 × 20 | ND | ND | ||
| T. b. gambiense STIB930 | 304 ± 87 | 2 ± 1.1 | ||
| 1 × 5 | 4/4 | 3/4 (59) | ||
| 1 × 20 | 4/4 | 4/4 | ||
| 4 × 5 | 4/4 | 4/4 | ||
| 4 × 20 | ND | ND | ||
| T. b. gambiense 130R | 99 ± 23 | 53 ± 28 | ||
| 1 × 5 | ND | ND | ||
| 1 × 20 | 4/4 | 4/4 | ||
| 4 × 5 | 4/4 | 2/3 (60) | ||
| 4 × 20 | ND | 4/4 | ||
| T. b. gambiense 45R | 302 ± 113 | 81 ± 8 | ||
| 1 × 5 | ND | ND | ||
| 1 × 20 | 4/4 | 4/4 | ||
| 4 × 5 | 4/4 | 3/3 | ||
| 4 × 20 | ND | ND | ||
a
MRD, mean relapse time in days.
b
DB829 also cured 3/4 mice at 4 × 50 mg/kg administered orally, 4/4 mice at 1 × 10 mg/kg i.p. or 1 × 10 mg/kg i.v., and 1/4 mice at 4 × 5 mg/kg i.v. for STIB900-infected animals.
c
The experiment was terminated on day 60 postinfection, instead of day 90 for other experiments with T. b. gambiense.
d
ND, not done.