Table 4.
Summary of PK parameters for otlertuzumab (cycle 1)
| Dose (mg/kg) | No. of patients | Cmax (μg/mL) | Half-life (h) | CL (mL/h/kg) | AUC all (h⋅mg/mL) | ||||
|---|---|---|---|---|---|---|---|---|---|
| Mean | %CV | Mean | %CV | Mean | %CV | Mean | %CV | ||
| Dose-escalation cohorts | |||||||||
| 1 | 2 | 19.5 | 24.2 | 133.7 | 4.9 | 1.62 | 9.7 | 4 846 | 39.7 |
| 3 | 2 | 41.5 | 26.7 | 208.1 | 68.6 | 2.87 | 33.6 | 18 333 | 80.4 |
| 6 | 1 | 128.6 | 25.7 | 271.9 | 0 | 2.1 | 0 | 42 683 | 45.2 |
| 3* | 4 | 138.0 | 64.2 | 178.6 | 65.7 | 0.306 | 44.5 | 45 728 | 69.5 |
| 10 | 7 | 435.7 | 23.3 | 221.7 | 38.5 | 0.473 | 129.5 | 413 319 | 53.0 |
| 15 | 6 | 703.7 | 51.4 | 176.3 | 25.6 | 0.262 | 62.8 | 593 848 | 132.6 |
| 20 | 9 | 1 081.1 | 49.9 | 177.9 | 30.5 | 0.129 | 623 | 831 562 | 66.0 |
| 6* | 3 | 367.5 | 31.6 | 247.8 | 38.0 | 0.129 | 58.9 | 37 625 | 58.5 |
| 10* | 1 | 202 | 28.4 | 121.2 | 0 | 0.7 | 0 | 42 961 | 71.1 |
| Dose-expansion cohorts | |||||||||
| 10 | 3 | 461.5 | 30.2 | 236.7 | 24.6 | 1.32 | 157.7 | 602 581 | 69.4 |
| 20 | 2 | 1 175.6 | 18.4 | 129.7 | 0.5 | 0.05 | 33.5 | 857 111 | 50.0 |
| 30 | 6 | 1 756.5 | 36.2 | 217.0 | 39.6 | 0.53 | 113.8 | 2 025 904 | 41.9 |
AUC all, area under the concentration-time curve from time 0 to the last measurable time point; CL, serum clearance; Cmax, maximum observed concentration; CV, coefficient of variation. Cycle 1 AUC, area under the concentration-time curve from time 0 to approximately day 29.
*
Dosed days 1, 3, and 5, then weekly ×3.