Table 3.
Summary of Enavatuzumab Pharmacokinetic Parameters (Mean [± SD])
| Enavatuzumab Dose | ||||||
|---|---|---|---|---|---|---|
| Pharmacokinetic Parameter Mean (SD) | 0.1 mg/kg (n = 5) |
0.3 mg/kg (n = 4) |
0.5 mg/kg (n = 1) |
0.7 mg/kg (n = 3) |
mg/kg (n = 5) |
1.5 mg/kg (n = 1) |
| Cycle 1 (28 days) | ||||||
| Tmax (h) | 1.0 (0.00) |
1.57 (1.51) |
1.80 (1.79) |
2.33 (2.31) |
3.86 (1.95) |
1.0 (NA) |
| C1max (μg/mL) | 2.32 (40.71) |
7.56 (3.19) |
12.74 (4.02) |
13.03 (3.11) |
28.09 (5.87) |
26.54 (NA) |
| C1max/D (μg/mL/mg/kg) | 23.16 (7.14) |
25.19 (10.63) |
25.48 (8.04) |
18.61 (4.45) |
28.09 (5.87) |
17.69 (NA) |
| AUCcycle1 (mg•h/mL) | 0.70 (0.11) |
2.33 (0.66) |
1.85 (NA) |
4.32 (0.25) |
10.59 (0.48) |
NA |
|
AUCcycle1/2xD (mg•h/mL/mg/kg) |
3.48 (0.54) |
3.89 (1.09) |
1.85 (NA) |
3.08 (0.18) |
5.29 (0.24) |
NA |
| Troughcycle1 (mcg/mL) | 0.32 | 0.79 | 1.81 | 2.56 | 4.21 | N/A |
| Troughcycle2-6 (mcg/mL) | 0.27 | 1.26–1.57 | 0.46–0.48* | 1.98–2.34 | 6.50–7.49 | N/A |
AUCcycle 1 = area under the drug concentration-time curve for Cycle 1; C1max = maximum serum concentration following the first dose; D = dose of enavatuzumab; h = hour; NA = not applicable; SD = standard deviation; Tmax = time to maximum serum concentration;
*
represents results from a single patient.