Table 10 Physicochemical and pharmacokinetic properties for selected anti-malarials
From: An in vitro toolbox to accelerate anti-malarial drug discovery and development
Property | 8-Aminoquinolines | Peroxides | |||
|---|---|---|---|---|---|
Primaquinea | Tafenoquinea | DHAb | OZ277b | OZ439b | |
Log D7.4 | 0.54 | 4.24 | 2.3 | 2.6 | > 5 |
Plasma fu | 0.26 | 0.0007 | 0.21 | 0.086 | < 0.0001 |
FaSSGF solubility (µg/mL) | > 2000 | > 2000 | 140 | > 2000 | 79 |
FaSSIF solubility (µg/mL) | > 2000 | 15.8 | 159 | > 2000 | 40.6 |
FeSSIF solubility (µg/mL) | > 2000 | 1310 | 246 | > 2000 | 526 |
Half-life (h) | 7 | 360 | 1 | 3 | > 40 |
V/F (L) | 277 | 1600 | 385 | 929 | 1570 |
CL/F (L/h) | 28 | 3.0 | 272 | 184 | 41 |
Food effect | no | yes | no | no | yes |