Table 1 PK and PD parameters of OZ439 after oral delivery in fasted and fed patients as reported in the literature
Parameter | Estimated value | Reference | ||
|---|---|---|---|---|
Fasted (capsule) | Fed (oral dispersion) | Fasted (oral dispersion) | ||
Dose (mg) | 800–1200 | 800 | 800 |  |
Absorption rate (ka) | 0.72 | 0.72 | 1.5 | [31] |
Elimination half-life (h) | 27.9 | 31.7 (healthy) 58.0 (malaria) | 38.8 | [31] [32] |
Clearance (L/h/kg) | 2.43 | 0.48 (healthy) 0.58 (malaria) | 1.41 N/A | [31] [32] |
Parasite reduction rate (PRR) (/48Â h) | 3000 | 3000 | 3000 | Assumed to be similar to artemisinin |
IC50 (nM) | 4.5 | 4.5 | 4.5 | [30] |
Molecular weight (Da) | 469.6 | 469.6 | 469.6 | [30] |
Hill’s slope constant | 4 | 4 | 4 |  |