Table 1.
Pharmacodynamic 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 (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 | |||
| Amax (%) | 9.93 ± 1.64 (17) [9.79] | 10.1 ± 2.03 (20) [9.95] | 0.96 (0.89, 1.04) |
| AAUC(0,tlast), (% h) | 359 ± 69.5 (19) [352] | 369 ± 84.4 (23) [359] | 0.95 (0.87, 1.04) |
| After repeated dosing in patients in EQUINOX substudy at month 6 | |||
| Amax (%) | 18.8 ± 8.84 (47) [17.16] | 17.6 ± 9.77 (56) [15.52] | 1.11 (1.00, 1.22) |
| AAUC (% h) | 1213 ± 670 (55) [1086] | 1135 ± 566 (50) [1027] | 1.06 (0.96, 1.16) |
| After repeated dosing in patients in EQUINOX substudy at steady-state | |||
| Amax (%) | 20.0 ± 10.7 (53) [17.9] | 19.2 ± 11.1 (58) [16.8] | 1.07 (0.96, 1.19) |
| AAUC (% h) | 1286 ± 800 (62) [1130] | 1261 ± 672 (53) [1133] | 1.00 (0.90, 1.10) |
*
All values are quoted in mean ± SD (%CV) [Geometric mean].
**
Calculated using log transformed values.
***
Equimolar dose of idraparinux and idrabiotaparinux. AAUC, area under the anti-Xa activity vs. time over the dosing interval; AAUC(0,tlast), AAUC from time 0 to the time corresponding to the last concentration above the limit of quantification; Amax, maximal activity; CI, confidence interval; SD, standard deviation.