Table 3.
Pharmacokinetics of pyronaridine in whole blood in healthy adults
| Reference | n | Regimen | PYR daily dose (mg) |
C
max
(ng/mL) |
T
max
(h) |
AUC0−∞ (ng/mL day) |
t
1/2
(days) |
|---|---|---|---|---|---|---|---|
| Phase I dose ascending study54,a | 7 | PA 6:2 mg/kg single dose |
360 | 186 ± 84.5 | 2.19 ± 1.63 | 258.5 ± 218.2 | 10.29 ± 10.63 |
| Phase I dose ascending study54,a | 7 | PA 9:3 mg/kg single dose |
540 | 262 ± 84.7 | 2.05 ± 1.34 | 319.5 ± 103.4 | 7.83 ± 4.54 |
| Phase I dose ascending study54,a | 7 | PA 12:4 mg/kg single dose |
720 | 467 ± 217 | 1.62 ± 0.30 | 517.9 ± 170.3 | 6.25 ± 1.51 |
| Phase I dose ascending study54,a | 7 | PA 15:5 mg/kg single dose |
900 | 792 ± 321 | 4.83 ± 4.47 | 868.4 ± 201.6 | 7.00 ± 1.99 |
| Morris et al.60,b | 6 | PA 12:4 mg/kg single dose |
720 | 266 ± 89 | 3.4 ± 3.6 | 374 ± 75 | 5.03 ± 2.19 |
| Morris et al.63,c | 16 | PA 9:3 mg/kg 3 day course |
540 | 377.2 ± 160.7 | 1.42 ± 0.36 | 1248 ± 429 | 13.1 ± 2.68 |
| Morris et al.61,d | 13 | PA 9:3 mg/kg 3 day course |
540 | 307.6 ± 110.7 | 1.5 (1–12) | 988 ± 266 | 14.5 ± 6.23 |
| Jittamala et al.62,e | 15 | PA 9:3 mg/kg 3 day course |
540 | 341 [226, 571] |
1.50 [1.00, 6.00] |
579.2 [462.5, 1000] |
16.3 [10.9, 26.5] |
All values are expressed as mean ± SD unless indicated otherwise. PA, pyronaridine-artesunate tablet; PYR, pyronaridine tetraphosphate.
Phase I dose ascending study of pyronaridine-artesunate in Korean healthy volunteers (SP-C-001-03)64 reported in PhD dissertation of Wattanavijitkul.54 The sampling period in this study was 10 days.
Mass balance study of pyronaridine in healthy volunteers with a sampling period of 42 days.
A drug–drug interaction study between pyronaridine-artesunate and ritonavir.63 Parameters were based on the first pyronaridine-artesunate dosing period of the pyronaridine-artesunate alone arm. The sampling period in this study was 42 days.
A drug–drug interaction study between pyronaridine-artesunate and metoprolol.61 Parameters were based on the pyronaridine-artesunate alone arm. The sampling period in this study was 42 days.
A drug–drug interaction study between pyronaridine-artesunate and primaquine. Parameters were based on the pyronaridine-artesunate alone group. The sampling period in this study was 42 days. Values are reported for this study as median [minimum, maximum].