Table 7.
Artesunate and DHA AUC and Cmax values following oral artesunate administration.
| Ref. | Subjects | Oral AS regimen | AUC (ng*hr/mL) | Cmax (ng/mL) |
|---|---|---|---|---|
| [29] | 10 healthy male Vietnamese adults | 200 mg once daily × 5 days | ASa Day 1: 67 Day 5: 60 |
ASa Day 1:67 Day 5: 58 |
| DHAa Day 1:1158 Day 5:1300 |
DHA Pooled:654 |
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| [30] | 12 healthy male Malaysian adults | 200 mg AS once | AS 119 |
AS 256.3 |
| DHA AUC0-t:1331 |
DHA 873.7 |
|||
| [27] | 13 healthy adults in Africa | Mean dose: 4.26 mg/kg with (ACT) or without (AS only) amodiaquine single dose | AS AS only: 206.4 ACT: 183.3 |
AS AS only: 231.8 ACT: 141.6 |
| DHA AS only: 2044.4 ACT: 1410.5 |
DHA AS only: 844.5 ACT: 446.2 |
|||
| [28] | 8 healthy male Thai adults | 300 mg AS (Guilin and Arenco formulations) |
AS Guilin: 406 Arenco: 190.8 |
AS Guilin: 397 Arenco: 194 |
| DHA Guilin: 1630 Arenco: 2600 |
DHA Guilin: 500 Arenco:928 |
|||
| [6] | 8 healthy adults in Australia | 150 mg once | AS AUC0-6 hr:154 (n = 6) |
ASa 111 (n = 6) |
| DHA AUC0-6 hr: 824 |
DHAa 546 |
|||
| [26] | 23 healthy Malaysian adults | 200 mg once with amodiaquine as fixed or non-fixed product | AS† Fixed: 391.1 Non-fixed: 213.2 |
AS† Fixed: 333 Non-fixed: 444 |
| DHA† Fixed: 1468.9 Non-fixed: 1656.0 |
DHA† Fixed: 609.8 Non-fixed:874.5 |
|||
| [34] | 86 acute uncomplicated falciparum malaria patients from Malawi and Gambia | 1, 2, or 4 mg/kg AS with chlorproguanil and dapsone once daily × 3 days | ASb 1 mg/kg: 64.6 (n = 16) 2 mg/kg:151(n = 19) 4 mg/kg: 400(n = 23) |
ASb 1 mg/kg: 48.9 2 mg/kg: 106 4 mg/kg: 224 |
| DHAb 1 mg/kg: 538 (n = 24) 2 mg/kg: 1445(n = 29) 4 mg/kg: 383(n = 23) |
DHAb 1 mg/kg: 228 2 mg/kg: 581 4 mg/kg: 1414 |
|||
| [39] | 21 children (5 - 13 years) with uncomplicated malaria in Uganda | 4 mg/kg once daily with amodiaquine × 3 days | AS 113 (data pooled from all subjects) |
AS 51 (data pooled from all subjects) |
| DHAa 1404 |
DHAa 473 |
|||
| [32] | 43 adults with uncomplicated falciparum malaria in Thailand | 200 mg/day for fixed dose AS-mefloquine tablet (n = 20) or 4 mg/kg/day as nonfixed (n = 23) AS-mefloquine | AS AUC0-t: Fixed:310 (n = 19) Nonfixed: 419 (n = 21) |
AS Fixed:255 (n = 19) Nonfixed:451 (n = 23) |
| DHA AUC0-t: Fixed:3027 Nonfixed: 3633 |
DHA Fixed:1234 Nonfixed:2043 |
|||
| [35] | 6 male Thai adults with uncomplicated falciparum malaria and 6 healthy male adults | 100 mg AS once | AS AUC0-12 hr Healthy: 97 Patients: not determined |
AS Healthy: 114 Patients: not determined |
| DHA AUC0-12 hr Healthy: 501 Patients: 1144 |
DHA Healthy: 339 Patients: 554 |
|||
| [36] | 57 children (2-14 years) with uncomplicated falciparum malaria in Gabon | AS dose (mg/kg) Group A:2.1(1.4-2.4) Group B:3.3(2.4 - 3.9) Group C:4.8(3.0 - 6.1) Group D: 3.8(3.0-4.3) |
AS Group A: 104 (n = 12) Group B: 154 (n = 12) Group C:232 (n = 10) Group D: 179 (n = 13) |
AS Group A: 93 Group B:154 Group C: 287 Group D: 171 |
| Administered with pyronaridine | DHA Group A: 1055 Group B: 1989 Group C: 2961 Group D: 2245 |
DHA Group A:479 Group B: 940 Group C:1186 Group D:792 |
||
| [37] | 40 children and adults with uncomplicated falciparum malaria in Pailin, Cambodia and 40 adults with uncomplicated falciparum malaria in Wang Pha, Thailand | At each site: Group 1: AS monotherapy: 2 mg/kg/day × 7 days Group 2: AS 4 mg/kg/day × 3 days + mefloquine |
AS†a AUC0-24 hr Thailand: Group 1: 128 Group 2: 237 Cambodia: Group 1: 173 Group 2: 338 |
AS†a Thailand: Group 1: 171 Group 2: 200 Cambodia: Group 1: 270 Group 2: 316 |
| DHA†a AUC0-24 hr Thailand: Group 1: 1308 Group 2: 2957 Cambodia: Group 1: 1382 Group 2: 4123 |
DHA†a Thailand: Group 1: 859 Group 2: 1191 Cambodia: Group 1: 802 Group 2: 1590 |
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Values given as mean unless otherwise specified.
†Units converted to uniform scale a. Median b. Geometric mean