Mean AUC values for lesogaberan and its metabolites in human studies
| AUC Value Measured | Lesogaberan Dose | Dosing Regimen | Total Radioactivity AUC | AUC (% Parent; % Total DRM) | ||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Lesogaberan | M1 | M2 | M3 | M4 | M5 | M6 | ||||
| mg | µmol × h/liter | |||||||||
| AUC0–24 h | 100 | Single dose | 28.100 | 17.7 (100.0; 59.7) | 2.56 (14.5; 8.6) | 0.145 (0.8; 0.5) | — | 3.66 (20.7; 12.4) | 5.56 (31.4; 18.8) | — |
| AUC0–∞ | 400 | Single dose | — | 87.9 (100.0; 52.8) | 10.5 (11.9; 6.3) | 3.41 (3.9; 2.0) | <2.40 | 17.8 (20.3; 10.7) | 47.0 (53.5; 28.2) | <2.40 |
| AUCτ × 2 | 400 | Twice daily for 5 days | — | 171 (100.0; 61.8) | 19.6 (11.5; 7.1) | 4.66 (2.7; 1.7) | <2.40 | 29.2 (17.1; 10.6) | 52.2 (30.5; 18.9) | <2.40 |
—, not measured; AUC, area under curve; DRM, drug-related material (expressed as the sum of the AUCs for parent compound and measured metabolites).