Table 2. AUC and clearance of 111In-labeled ALN-modified proteins in mice after intravenous injection of 1 mg protein/kg.
Compound | AUC(h•% of dose/ml) | CLtotal (ml/h) | CLbone (ml/h) | CLliver (ml/h) | CLkidney (ml/h) | CLlung (ml/h) | CLurine (ml/h) |
---|---|---|---|---|---|---|---|
GR | 545 | 0.18 | 0.04 | 0.02 | 0.01 | 0.002 | 0.003 |
GR-ALN(4) | 130 | 0.77 | 0.37 | 0.22 | 0.04 | 0.006 | 0.02 |
GR-ALN(17) | 1.91 | 52.4 | 1.37 | 35.8 | 1.87 | 1.37 | 0.38 |
BSA | 259 | 0.39 | 0.02 | 0.03 | 0.01 | 0.003 | 0.004 |
BSA-ALN (3) | 265 | 0.38 | 0.12 | 0.03 | 0.02 | 0.002 | 0.03 |
BSA-ALN (28) | 1.86 | 53.8 | 2.21 | 32.6 | 2.17 | 3.19 | 0.41 |
BSA-ALN (40) | 0.81 | 124 | 6.73 | 62.8 | 2.62 | 18 | 2.14 |
SOD | 9.64 | 10.4 | 0.1 | 0.02 | 8.43 | 0.02 | 3.28 |
SOD-ALN(3) | 6.49 | 15.4 | 1.51 | 0.45 | 11.8 | 0.02 | 0.75 |
SOD-ALN(32) | 2.32 | 43.1 | 6.26 | 14.7 | 7.65 | 0.36 | 6.85 |
PEG(10)-SOD | 207 | 0.48 | 0.12 | 0.03 | 0.02 | 0.002 | 0.002 |
PEG(10)-SOD-ALN(4) | 30.8 | 3.25 | 0.94 | 0.11 | 0.38 | 0.01 | 0.06 |
LZM | 4.18 | 24 | 1.39 | 0.65 | 9.5 | 0.38 | 2.99 |
LZM-ALN(5) | 3.48 | 28.7 | 2.55 | 3.06 | 12.1 | 0.59 | 2.43 |
LZM-ALN(9) | 3.5 | 28.6 | 2.35 | 1.76 | 13.1 | 0.35 | 2.54 |