Table 2.
KD and KD(FcγRIIIa)/KD(FcγRIIb) ratios of glycoengineered trastuzumab variants
| Trastuzumab variants | KD for FcγRIIb (mol/L) |
KD for FcγRIIIaF158 (mol/L) |
KD for FcγRIIIaV158 (mol/L) |
KD for FcγRIIaH131 (mol/L) |
KD for FcγRIIaR131 (mol/L) |
KD(FcγRIIIaF158)/KD(FcγRIIb) | KD(FcγRIIIaV158)/KD(FcγRIIb) |
|---|---|---|---|---|---|---|---|
| H268E/K326S/I332E (defucosylation) |
1.46E-06 | 2.62E-09 | 1.36E-09 | 6.69E-07 | 3.69E-07 | 0.0018 | 0.0009 |
| H268E/K326M/I332E (defucosylation) |
1.03E-06 | 3.55E-09 | 1.71E-09 | 1.04E-06 | 4.20E-07 | 0.0034 | 0.0017 |
| WT (defucosylation) | 1.78E-06 | 4.65E-08 | 1.23E-08 | 2.09E-06 | 1.46E-06 | 0.0261 | 0.0069 |
| WT (fucosylation) | 1.24E-06 | 1.74E-07 | 3.85E-08 | 1.00E-06 | 1.50E-06 | 0.1403 | 0.0310 |