Concentrations of 10074-G5 in plasma and tissues after administration of 20 mg/kg 10074-G5 intravenously to C.B-17 SCID female mice bearing Daudi xenografts
| Time | Plasma | Tumor | Liver | Kidney | Lung | Spleen | Heart | Brain | Skeletal Muscles | Red Blood Cells | Fat |
|---|---|---|---|---|---|---|---|---|---|---|---|
| min | nmol/ml | nmol/g | nmol/g | nmol/g | nmol/g | nmol/g | nmol/g | nmol/g | nmol/g | nmol/mlg | nmol/g |
| 5 | 58.46 ± 2.73 | 5.61 ± 1.23 | 40.81 ± 8.71 | 29.26 ± 7.74 | 44.29 ± 8.18 | 7.95 ± 0.60 | 22.00 ± 3.48 | 16.76 ± 3.33 | 8.25 ± 0.83 | 13.64 ± 3.77 | 10.87 ± 1.52 |
| 10 | 20.98 ± 6.54 | 5.16 ± 1.18 | 22.92 ± 18.86 | 17.67 ± 6.31 | 40.37 ± 5.43 | 6.49 ± 1.97 | 11.44 ± 1.86 | 6.83 ± 2.40 | 5.39 ± 2.07 | 3.14 ± 2.07 | 10.09 ± 1.48 |
| 15 | 15.11 ± 3.37 | 5.12 ± 1.11 | 10.36 ± 4.18 | 5.28 ± 0.15 | 26.34 ± 0.10 | 2.88 ± 0.32 | 8.34 ± 2.25 | 3.30 ± 0.35 | 4.73 ± 1.11 | 2.68 ± 0.39 | 18.38 ± 5.01 |
| 30 | 6.66 ± 2.94 | 1.44 ± 0.76 | 6.71 ± 0.12 | 1.77 ± 0.15 | 12.36 ± 0.97 | 1.20 ± 0.12 | 2.53 ± 0.20 | 1.06 ± 0.21 | 2.75 ± 0.81 | 0.48 ± 0.17 | 19.30 ± 7.05 |
| 60 | 1.85 ± 0.37 | 1.47 ± 0.78 | 5.74 ± 0.68 | 1.04 ± 0.27 | 3.59 ± 1.57 | 0.89 ± 0.42 | 0.92 ± 0.22 | 0.52 ± 0.02 | 1.02 ± 0.45 | 0.19 ± 0.11 | 6.83 ± 4.03 |
| 120 | 1.05 ± 0.11 | 0.29 ± 0.03 | 3.33 ± 2.63 | 0.24 ± 0.04 | 3.08 ± 1.11 | ND | 0.52 ± 0.14 | 0.31 ± 0.02 | 0.68 ± 0.27 | 0.06 ± 0.00 | 4.59 ± 0.29 |
| 240 | 0.39 ± 0.19 | ND | 1.25 ± 0.32 | 0.21 ± 0.03 | 0.67 ± 0.12 | ND | ND | 0.04 ± 0.00 | ND | ND | 0.91 ± 0.46 |
| 360 | ND | ND | 0.65 ± 0.03 | ND | ND | ND | ND | ND | ND | ND | ND |
| 1020 | ND | ND | 0.42 ± 0.07 | ND | ND | ND | ND | ND | ND | ND | ND |
| 1440 | ND | ND | 0.49 ± 0.08 | ND | ND | ND | ND | ND | ND | ND | ND |
| t1/2 | 37 | 29 | — | — | — | — | — | — | — | — | — |
| AUC0→∞a | 864 (899) | 223 (212) | 1819 (1864) | 621 (681) | 1063 (1232) | 147 (141) | 349 (380) | 216 (228) | 255 (244) | 131 (132) | 1541 (1584) |
ND, not determined.
↵a AUCs were calculated noncompartmentally using both the Lagrange function and the Trapezoidal method (in parentheses). AUC units are nanomoles per milliliter per minute for plasma and nanomoles per gram per minute for tissues.