Table 1. Binding of TNF inhibitors to TNF at 25 °C.
| TNF inhibitor | ka (106 M−1 s−1)a,b | kd (10−4 s−1)a | Kd (pM)a,b | Kd (pM)b,c |
|---|---|---|---|---|
| adalimumab | 0.72 (0.02) | 1.3 (0.3) | 183 (40) | 244 (53) |
| certolizumab | 3.2 (0.5) | 1.5 (0.6) | 71 (35) | 9 (4) |
| golimumab | 1.9 (0.2) | 1.2 (0.3) | 59 (20) | 26 (6) |
| infliximab | 1.7 (0.2) | 2.4 (0.5) | 138 (30) | 123 (11) |
| etanercept | 11 (2) | 1.7 (0.7) | 16 (8) | 11 (3)d |
aMeasured using Biacore (n = 2–5).
bAssociation rates and dissociation constants are expressed relative to the molar concentrations of actual binding sites on TNF, which equals 3 for adalimumab, certolizumab, golimumab, and infliximab; for etanercept, 1:1 binding was assumed. To compare results to papers where molar trimeric TNF concentrations were used, multiply ka and divide Kd by a factor of three for the mAbs.
cMeasured in fluid phase by fluorescence-assisted HP-SEC (n = 3).
dDetermined in reverse experiment in which etanercept was titrated to TNF-488.