TABLE 3.
Average (± S.D.) PK parameters following single i.v. or s.c. dose administration at 10 mg/kg in cynos
The following abbreviations are used: t½β = terminal half-life; CL = non-specific clearance; AUC = area under the concentration time curve from time 0 to time of last measurable concentration; V1 = volume of distribution of the central compartment; %F = bioavailability; ka = absorption rate constant; tmax = time to maximum serum concentration; Cmax = maximum serum concentration; i.v. = intravenous; s.c. = subcutaneous.
| Parameter | Anti-LTαparental | Anti-LTα+3 | Anti-LTα−4 | HumAb4D5-8 parental | HumAb4D5-8 +5 | HumAb4D5-8 −4 |
|---|---|---|---|---|---|---|
| t½β day | 4.62 ± 1.09 | 3.23 ± 0.766 | 7.33 ± 0.846 | 7.06 ± 0.917 | 8.50 ± 0.372 | 7.57 ± 2.05 |
| CL ml/day/kg | 14.9 ± 2.53 | 59.3 ± 7.51 | 5.78 ± 0.415 | 6.22 ± 0.607 | 51.1 ± 5.42 | 6.63 ± 0.559 |
| AUC (i.v.) day·μg/ml | 671 ± 114 | 169 ± 21.4 | 1730 ± 124 | 1610 ± 157 | 196 ± 20.8 | 1510 ± 127 |
| V1 ml/kg | 88.1 ± 18.0 | 69.7 ± 14.4 | 50.4 ± 4.57 | 58.7 ± 7.39 | 97.3 ± 20.9 | 66.3 ± 7.33 |
| %F | 59.9 ± 14.3 | 31.4 ± 5.23 | 69.9 ± 7.62 | 71.5 ± 10.2 | 82.7 ± 11.9 | 117 ± 14.5 |
| ka 1/day | 0.970 ± 0.370 | 0.921 ± 0.213 | 1.09 ± 0.204 | 0.555 ± 0.126 | 0.384 ± 0.0916 | 0.454 ± 0.0869 |
| tmax (s.c.) day | 1.00 ± 0 | 0.833 ± 0.333 | 2.50 ± 1.00 | 3.00 ± 0 | 1.50 ± 1.00 | 2.5 ± 1.00 |
| Cmax (s.c.) μg/ml | 55.3 ± 17.8 | 17.0 ± 10.4 | 143 ± 5.52 | 88.0 ± 9.25 | 16.2 ± 4.78 | 118 ± 20.5 |