Table 3 Tumour uptake, blood levels and tumour-to-blood ratios for 131I- and 111In-CHX-A″ DTPA-labelled hu3S193 antibody variants in A431 tumour-bearing mice
Antibody | Time (hours) | Tumour (%ID/g) | Blood (%ID/g) | T/B | Tumour (%ID/g) | Blood (%ID/g) | T/B |
|---|---|---|---|---|---|---|---|
131I | 111In | ||||||
Wild type | 4 | 9.02 ± 0.73a | 39.37 ± 3.33 | 1:4 | 13.17 ± 2.40 | 35.56 ± 5.48 | 1:3 |
24 | 17.37 ± 1.25 | 22.17 ± 1.81 | 1:1 | 33.42 ± 7.75 | 21.83 ± 3.32 | 2:1 | |
48 | 17.58 ± 2.60 | 15.09 ± 1.70 | 1:1 | 39.01 ± 3.92 | 14.50 ± 1.11 | 3:1 | |
72 | 17.76 ± 1.72 | 13.18 ± 1.91 | 1:1 | 39.27 ± 4.33 | 9.97 ± 1.85 | 4:1 | |
120 | 15.10 ± 3.89 | 7.13 ± 1.46 | 2:1 | 37.26 ± 8.67 | 5.78 ± 2.12 | 6:1 | |
168 | 11.40 ± 4.56 | 4.44 ± 1.56 | 2:1 | 24.24 ± 2.57 | 1.06 ± 0.32 | 9:1 | |
I253A | 4 | 10.01 ± 3.25 | 29.95 ± 3.59 | 1:3 | 9.64 ± 0.74 | 38.74 ± 3.57 | 1:4 |
24 | 9.95 ± 2.26 | 6.94 ± 1.34 | 1:1 | 27.17 ± 2.00 | 17.99 ± 1.57 | 2:1 | |
48 | 5.07 ± 2.10 | 1.09 ± 0.32 | 5:1 | 31.75 ± 3.98 | 10.19 ± 1.04 | 3:1 | |
72 | 2.03 ± 0.81 | 0.04 ± 0.08 | 48:1 | 33.11 ± 4.05 | 7.64 ± 1.32 | 4:1 | |
120 | 0.78 ± 0.79 | 0.00 ± 0.00 | >500:1 | 23.68 ± 6.52 | 2.99 ± 0.73 | 8:1 | |
168 | 0.10 ± 0.14 | 0.00 ± 0.00 | >500:1 | 14.66 ± 4.80 | 1.14 ± 0.63 | 13:1 | |
H435A | 4 | 8.79 ± 0.45 | 32.46 ± 2.63 | 1:4 | 10.25 ± 1.30 | 37.97 ± 2.68 | 1:4 |
24 | 11.52 ± 1.38 | 8.46 ± 1.89 | 1:1 | 33.69 ± 3.77 | 17.09 ± 1.59 | 2:1 | |
48 | 5.53 ± 1.18 | 2.27 ± 1.21 | 2:1 | 31.10 ± 4.76 | 7.65 ± 1.60 | 4:1 | |
72 | 3.18 ± 0.22 | 0.69 ± 0.17 | 5:1 | 28.48 ± 4.00 | 5.18 ± 1.40 | 6:1 | |
120 | 1.64 ± 1.09 | 0.00 ± 0.00 | >500:1 | 25.60 ± 4.16 | 3.19 ± 0.62 | 8:1 | |
168 | 0.54 ± 0.58 | 0.00 ± 0.00 | >500:1 | 15.34 ± 4.65 | 1.16 ± 0.62 | 13:1 | |
H310A | 4 | 9.80 ± 1.83 | 32.56 ± 3.00 | 1:3 | 10.79 ± 2.87 | 30.52 ± 5.06 | 1:3 |
24 | 9.58 ± 1.73 | 3.85 ± 0.35 | 3:1 | 22.85 ± 2.93 | 11.05 ± 1.62 | 2:1 | |
48 | 5.10 ± 1.87 | 0.01 ± 0.02 | >500:1 | 25.10 ± 2.91 | 5.61 ± 2.01 | 5:1 | |
72 | 2.43 ± 1.10 | 0.00 ± 0.00 | >500:1 | 22.12 ± 2.55 | 2.56 ± 0.60 | 9:1 | |
120 | 1.81 ± 0.71 | 0.00 ± 0.00 | >500:1 | 12.89 ± 1.33 | 0.54 ± 0.16 | 24:1 | |
168 | 1.45 ± 0.99 | 0.00 ± 0.00 | >500:1 | 8.64 ± 0.96 | 0.17 ± 0.06 | 51:1 | |
I253A/H310A | 4 | 9.90 ± 2.42 | 30.20 ± 3.97 | 1:3 | 8.92 ± 2.00 | 28.84 ± 6.05 | 1:3 |
24 | 8.04 ± 1.82 | 3.88 ± 1.32 | 2:1 | 23.72 ± 0.85 | 5.28 ± 0.81 | 5:1 | |
48 | 5.10 ± 0.76 | 0.06 ± 0.09 | 80:1 | 14.84 ± 1.43 | 0.46 ± 0.07 | 32:1 | |
72 | 3.04 ± 1.58 | 0.00 ± 0.00 | >500:1 | 11.92 ± 2.46 | 0.08 ± 0.03 | 154:1 | |
120 | 1.92 ± 0.53 | 0.00 ± 0.00 | >500:1 | 5.85 ± 1.31 | 0.00 ± 0.00 | >500:1 | |
168 | 1.43 ± 0.27 | 0.00 ± 0.00 | >500:1 | 3.52 ± 1.00 | 0.00 ± 0.00 | >500:1 | |