Table 4.
|
AUC |
Beta half-life |
Clearance rate |
||
---|---|---|---|---|---|
h·µg/mL | % vs. trastuzumab | h | % vs. trastuzumab | mL/h/kg | |
Trastuzumab | 6964.9 | 100% | 115.7 | 100% | 0.37 |
T-N-F (T) | 6795.7 | 98% | 122.1 | 106% | 0.37 |
T-N-F (C) | 6813.2 | 98% | 118.3 | 102% | 0.38 |
T-C-F (T) | 5933.5 | 85% | 111.6 | 96% | 0.43 |
T-C-F (C) | 4315.4 | 62% | 84.6 | 73% | 0.60 |
T-K-F (T) | 4324.3 | 62% | 65.1 | 56% | 0.64 |
T-K-F (C) | 3718.7 | 54% | 53.2 | 46% | 0.69 |
ADCs: antibody–drug conjugates, AUC: area under the curve, T-N-F: trastuzumab-monomethyl auristatin F (MMAF) conjugate synthesized via NTERM conjugation, (T): total antibody concentration, (C): conjugate antibody concentration, T-C-F: trastuzumab-MMAF conjugate synthesized via thiol conjugation, T-K-F: trastuzumab-MMAF conjugate synthesized via lysine conjugation.