Table 4.
hu3F8-IgG1 | hu3F8-IgG1n | hu3F8-IgG1-DEL | hu3F8-IgG1n-DEL | |
---|---|---|---|---|
KD (CD16A-158F)* | 1 | 4 | 16 | 37 |
KD (CD16A-158V)* | 3 | 11 | 25 | 63 |
KD (CD32A-131R)** | 1.0 | 0.5 | 1.4 | 0.3 |
KD (CD32A-131H)** | 1.3 | 0.6 | 1.3 | 0.3 |
A:I FcR ratioˆ | 9 | 35 | 18 | 165 |
ADCC(CD16A-158V) | 1 | 26 | 35 | 84 |
ADCC(CD32A-131H) | 1.0 | 0.1 | 0.9 | 0.1 |
CMC | 1.0 | 0.6 | 0.4 | ≤0.05 |
t1/2 | 17 | 22 | 31 | 2 |
Cmax | 55 | 69 | 84 | 103 |
AUC | 1171 | 902 | 2029 | 293 |
In vivo antitumor effect | + | +++ | + | + |
Normalized to KD of hu3F8-IgG1 on CD16A-158F.
Normalized to KD of hu3F8-IgG1 on CD32A-131R.
A:I = Activating: inhibitory = (relative KA on CD16-158V)/(relative KA on CD32B).