Table 2.
Pharmacokinetic parameters and ratio estimates of idrabiotaparinux vs. idraparinux after subcutaneous equimolar dosing in healthy volunteers (n = 24 per treatment group) or patients in the EQUINOX bioequipotency substudy at month 6 (n = 114 per treatment group)
| Parameter* | Idrabiotaparinux (3.0 mg***) | Idraparinux (2.5 mg***) | Ratio (90% CI) ** idrabiotaparinux vs. idraparinux |
|---|---|---|---|
| After single dosing in healthy volunteers | |||
| Cmax (μmol l−1) | 0.368 ± 0.0257 (7) [0.367] | 0.401 ± 0.0513 (13) [0.397] | 0.92 (0.87, 0.98) |
| AUC(0,tlast) (μmol l−1 h) | 21.8 ± 3.87 (18) [21.5] | 23.9 ± 6.57 (27) [22.9] | 0.94 (0.83, 1.07) |
| After repeated dosing in patients in the EQUINOX substudy at month 6 | |||
| Cmax (μmol l−1) | 0.525 ± 0.152 (29) [0.505] | 0.544 ± 0.107 (20) [0.534] | 1.06 (1.00, 1.11) |
| AUC (μmol l−1 h) | 50.2 ± 14.3 (29) [48.4] | 51.6 ± 13.2 (26) [50.1] | 1.04 (0.98, 1.10) |
*
All values are quoted in mean ± SD (%CV) [Geometric mean].
**
Calculated using log transformed values.
***
Equimolar dose of idraparinux and idrabiotaparinux. AUC, area under the curve; AUC(0,tlast), AUC up to the last concentration; CI, confidence interval; Cmax, maximal concentration; SD, standard deviation.