Table 3.
In vitro susceptibility of P. falciparum, parental (B5), pfexo-modified (B5-rexo-E415G-B8) and adapted clinical parasites to dihydroartemisinin (DHA), artesunate (AS), mefloquine (MQ), quinine (QN), chloroquine (CQ), atovaquone (ATQ), lumefantrine (LUM), doxycycline (DOX), tafenoquine (TQ), cycloguanil (CYC), primaquine (PQ), proguanil (PG), and pyronaridine (PND). (mean ± SD, nM)
| Drug | IC50 (nM) | ||||
|---|---|---|---|---|---|
| B5 | B5-r exo-E415G-B8 | ASAP-21 | ASAP-168 | P-value | |
| DHA | 9 ± 4 | 14 ± 6 | 5 ± 0.2 | 2 ± 1 | 0.1213 |
| AS | 7 ± 5 | 4 ± 1 | 3 ± 0.4 | 3 ± 1 | – |
| MQ | 161 ± 58 | 82 ± 37 | 61 ± 23 | 50 ± 20 | 0.0483 |
| QN | 546 ± 180 | 564 ± 165 | 71 ± 3 | 138 ± 32 | 0.0172,3 |
| CQ | 562 ± 218 | 416 ± 219 | 64 ± 12 | 256 ± 59 | 0.0172 |
| ATQ | 48 ± 38 | 114 ± 1 | 5 ± 0.6 | 4 ± 1 | 0.0171,2,3 |
| LUM | 10 ± 8 | 4 ± 1 | 2 ± 0.2 | 3 ± 1 | – |
| DOX | 13,523 ± 2337 | 14,649 ± 1071 | 8527 ± 349 | 10,920 ± 1061 | 0.0242 |
| TQ | 263 ± 143 | 315 ± 45 | 189 ± 13 | 274 ± 554 | – |
| CYC | 2063 ± 2703 | 705 ± 15 | 7183 ± 388 | N.D. | – |
| PQ | 3094 ± 2015 | 6387 ± 218 | 5720 ± 1160 | 2458 ± 61 | – |
| PG | 12,522 ± 7247 | 23,816 ± 3786 | 2114 ± 243 | 3643 ± 473 | 0.0331 |
| PND | 28 ± 16 | 25 ± 4 | 50 ± 2 | 12 ± 6 | 0.0332 |
P-value calculated by Mann–Whitney U Test
1,2,3Significant differences between data from B5-rexo-E415G-B8, ASAP-21, and ASAP-168 compared to B5 line, respectively
N.D. for not determined