Table 2. Comparative PK parameters of ADCs at MTD or nearest dose level, at Cycle 1.
| ADC Name |
Dosing regimen |
Dose (mg/kg) |
MTD (mg/kg) |
Cytotoxin | Isotype | DAR | Cleavable | Cmax (µg/mL) |
AUC (µg.day/mL) |
CL (mL/day/kg) |
t½ (days) |
Vss (mL/kg) |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mylotarg® | q2w | 0.220 | 0.220 | calicheamicin | IgG4 | 2.5 | c | 2.86 | 5.13 | 90.8 | 3.02 | 300 |
| CMC544 | q4w | 0.045 | 0.040 | calicheamicin | IgG4 | 6 | c | 0.969 | 0.600 | 91.2 | 0.710 | 89.1 |
| IMGN901 | q1w | 2.77 | 2.77 | DM1 | IgG1 | 3.5 | c | 55.1 | 62.6 | 52.6 | 0.890 | 56.3 |
| HuC242-DM1 | q3w | 5.81 | 5.81 | DM1 | IgG1 | 3.5 | c | 241 | 285 | 24.3 | 2.02 | 42.7 |
| Kadcyla® | q3w | 3.60 | 3.60 | DM1 | IgG1 | 3.5 | ncl | 76.2 | 300 | 12.7 | 3.10 | 58.4 |
| MLN2704 | q3w | 8.48 | not reached | DM1 | IgG1 | 3.5 | c | 209 | 404 | 26.6 | 2.50 | nc |
| AVE9633 | q3w | 6.43 | not reached | DM4 | IgG1 | 3.5 | c | 119 | 468 | 12.6 | 3.93 | 68.1 |
| BT062 | q3w | 3.95 | 3.95 | DM4 | IgG4 | 3.5 | c | 89.4 | 183 | 24.0 | 2.12 | nc |
| SAR3419 | q3w | 3.95 | 3.95 | DM4 | IgG1 | 3.5 | c | 95.4 | 720 | 6.49 | 6.90 | 53.6 |
| Adcetris® | q3w | 1.80 | 1.80 | MMAE | IgG1 | 4 | c | 32.0 | 79.4 | 25.1 | 4.43 | 117 |
| CDX-011 | q3w | 1.88 | 1.88 | MMAE | IgG2 | 4 | c | 36.3 | 59.7 | 40.8 | 1.18 | 48.7 |
| PSMA-ADC | q3w | 2.20 | 2.50 | MMAE | IgG1 | 4 | c | 41.6 | 67.8 | 32.9 | 1.65 | 62.5 |
| MEDI-547 | q3w | 0.08 | 0.08 | MMAF | IgG1 | 4 | ncl | 2.14 | nc | nc | nc | nc |
q4w: every 4 wk ; q3w: every 3 wk; q2w: every 2 wk; c: cleavable; ncl: non-cleavable; DAR: drug-to-antibody ratio; Cmax: maximal observed concentration; AUC: area under curve; CL: clearance; t½: elimination half-life; Vss: volume of distribution at steady-state; nc: not calculated