Summary of PK exposure in serum of patients on the Q3W dosing regimen
| Cohort, µg/kg . | Arithmetic mean (CV%); n . | |||
|---|---|---|---|---|
| Cycle 1 . | Cycle 2 . | |||
| Cmax, µg/L* . | AUClast, d × µg/L . | Cmax, µg/L* . | AUClast, d × µg/L . | |
| Conjugated Ab | ||||
| 15 | 178 (72.0); 4 | 337 (193); 4 | 2150 (-); 1 | 1596 (—); 1 |
| 30 | 258 (62.9); 7 | 127 (180); 7 | 339 (81.5); 4 | 735 (190); 4 |
| 60 | 449 (62.7); 3 | 43.0 (86.9); 3 | 661 (62.3); 2 | 50.6 (18.0); 2 |
| 90 | 1058 (84.4); 3 | 671 (162); 3 | 1813 (91.0); 2 | 3370 (135); 2 |
| 120 | 1291 (79.0); 5 | 3907 (209); 5 | 1515 (66.0); 5 | 8744 (203); 5 |
| 150 | 2145 (49.1); 6 | 688 (82.9); 6 | 3033 (48.1); 4 | 7553 (9.62); 4 |
| Total Ab | ||||
| 15 | 205 (78.8); 4 | 610 (195); 4 | 1251 (138); 2 | 1012 (129); 2 |
| 30 | 317 (61.1); 7 | 408 (153); 7 | 366 (68.5); 4 | 1140 (184); 4 |
| 60 | 717 (59.8); 2 | 59.9 (72.6); 2 | 689 (55.4); 2 | 40.2 (0.0608); 2 |
| 90 | 1049 (85.1); 3 | 558 (161); 3 | 1845 (90.8); 2 | 3671 (138); 2 |
| 120 | 1722 (45.6); 4 | 5718 (169); 4 | 2125 (44.4); 4 | 13 519 (169); 4 |
| 150 | 2761 (62.2); 6 | 1091 (61.6); 6 | 4338 (56.7); 4 | 10 493 (19.3); 4 |
| SG3199 | ||||
| 15 | — | — | — | — |
| 30 | 0.0428 (0.165); 2 | 0.00355 (41.5); 2 | 0.0459 (—); 1 | 0.00522 (—); 1 |
| 60 | — | — | 0.0697 (—); 1 | 0.0129 (—); 1 |
| 90 | 0.0617 (38.7); 2 | 0.00930 (72.6); 2 | 0.0551 (—); 1 | 0.00830 (—); 1 |
| 120 | 0.0810 (35.6); 3 | 0.0194 (119); 3 | 0.108 (22.1); 3 | 0.0433 (73.0); 3 |
| 150 | 0.0907 (55.2); 6 | 0.0338 (44.2); 6 | 0.0550 (50.4); 2 | 0.00927 (95.1); 2 |
| Cohort, µg/kg . | Arithmetic mean (CV%); n . | |||
|---|---|---|---|---|
| Cycle 1 . | Cycle 2 . | |||
| Cmax, µg/L* . | AUClast, d × µg/L . | Cmax, µg/L* . | AUClast, d × µg/L . | |
| Conjugated Ab | ||||
| 15 | 178 (72.0); 4 | 337 (193); 4 | 2150 (-); 1 | 1596 (—); 1 |
| 30 | 258 (62.9); 7 | 127 (180); 7 | 339 (81.5); 4 | 735 (190); 4 |
| 60 | 449 (62.7); 3 | 43.0 (86.9); 3 | 661 (62.3); 2 | 50.6 (18.0); 2 |
| 90 | 1058 (84.4); 3 | 671 (162); 3 | 1813 (91.0); 2 | 3370 (135); 2 |
| 120 | 1291 (79.0); 5 | 3907 (209); 5 | 1515 (66.0); 5 | 8744 (203); 5 |
| 150 | 2145 (49.1); 6 | 688 (82.9); 6 | 3033 (48.1); 4 | 7553 (9.62); 4 |
| Total Ab | ||||
| 15 | 205 (78.8); 4 | 610 (195); 4 | 1251 (138); 2 | 1012 (129); 2 |
| 30 | 317 (61.1); 7 | 408 (153); 7 | 366 (68.5); 4 | 1140 (184); 4 |
| 60 | 717 (59.8); 2 | 59.9 (72.6); 2 | 689 (55.4); 2 | 40.2 (0.0608); 2 |
| 90 | 1049 (85.1); 3 | 558 (161); 3 | 1845 (90.8); 2 | 3671 (138); 2 |
| 120 | 1722 (45.6); 4 | 5718 (169); 4 | 2125 (44.4); 4 | 13 519 (169); 4 |
| 150 | 2761 (62.2); 6 | 1091 (61.6); 6 | 4338 (56.7); 4 | 10 493 (19.3); 4 |
| SG3199 | ||||
| 15 | — | — | — | — |
| 30 | 0.0428 (0.165); 2 | 0.00355 (41.5); 2 | 0.0459 (—); 1 | 0.00522 (—); 1 |
| 60 | — | — | 0.0697 (—); 1 | 0.0129 (—); 1 |
| 90 | 0.0617 (38.7); 2 | 0.00930 (72.6); 2 | 0.0551 (—); 1 | 0.00830 (—); 1 |
| 120 | 0.0810 (35.6); 3 | 0.0194 (119); 3 | 0.108 (22.1); 3 | 0.0433 (73.0); 3 |
| 150 | 0.0907 (55.2); 6 | 0.0338 (44.2); 6 | 0.0550 (50.4); 2 | 0.00927 (95.1); 2 |
—, not available; Ab, antibody; AUClast, AUC from time 0 to last measurable time point in respective cycle; CV, coefficient of variation.
Approximates the concentration at the end of infusion for conjugated and total Ab (0.480-4.56 hours) and after the end of infusion for SG3199 (0.960-47.5 hours).