TABLE 1.
In vitro drug testing of antimalarial activity of T3/SAR97276 and artesunate using different drug sensitivity tests
| Drug | Incubation period (h) | Geometric mean IC50 in nM against P. falciparum 3D7 (95% CI)a as determined by using: |
||||
|---|---|---|---|---|---|---|
| MIC | HX assay | SYBR green | pLDH ELISA | HRP2 ELISA | ||
| T3/SAR97276 | 48 | 5.6 | 4.6 (4-5.2) | 77.3 (25.7-232) | >1,000 | 18.5 (14.1-24.3) |
| 72 | 2 | 4.5 (3.7-5.6) | 2.3 (0.6-9.9) | 19.5 (15.3-24.7) | 99.3 (50.3-19.6) | |
| 72 (w/o drug)b | 7.2 | 8.1 (6.9-9.5) | 7.4 (5.9-9.2) | |||
| 96 h | 1.9 | 1.3 (1.2-1.4) | 3.9 (3.6-4.4) | |||
| 96 (w/o drug) | 7.4 | 5.3 (4.6-6.3) | 6.3 (5.7-7) | |||
| Artesunate | 48 | 3.7 | 1.1 (0.8-1.4) | 1.9 (1.2-2.8) | 2.4 (2.2-2.6) | 1.5 (1.4-1.7) |
| 72 | 1.6 | 1.2 (0.8-1.6) | 1.5 (1.3-1.8) | 2.0 (1.1-3.4) | 2.5 (1.9-3.3) | |
| 72 (w/o drug) | 1.8 | 1.4 (1-2.1) | 1.5 (1.4-1.7) | |||
| 96 | 1.8 | 1.1 (0.9-1.5) | 1.3 (1.1-1.5) | |||
| 96 (w/o drug) | 1.4 | 1.4 (1.1-1.8) | 1.6 (1.5-1.8) | |||
a
MIC, microscopy; HX, hypoxanthine. Values in boldface do not match the real IC50 (see the text).
b
w/o drug, without drug. In these cases, after 48 h of contact with the drug, infected erythrocytes were washed for drug clearance and then incubated in fresh drug-free culture medium.