Table 2.
Extensive Tissue Distribution Study PK and Partition Coefficients.
| Tissue | Cmaxa (μg/mL) | Tmax (min) | AUC0-tb (μg/mL•min) | AUC0-∞ (μg/mL•min) | Tissue Partition Coefficient |
|---|---|---|---|---|---|
|
| |||||
| Plasma | 13.3 (4.91) | 5 | 854 | 906 | 1 |
| Bone Marrow | 164 (153) | 60 | 63,581 | 66,660 | 74.5 |
| Kidney | 117 (25.4) | 5 | 49,230 | 52,367 | 57.7 |
| Liver | 79.8 (26.7) | 5 | 21,805 | 23,205 | 25.5 |
| Spleen | 39.0 (3.86) | 120 | 17,571 | 18,375 | 20.6 |
| Lung | 45.2 (11.8) | 5 | 11,889 | 12,959 | 13.9 |
| Small Intestine | 31.3 (5.80) | 15 | 10,845 | 12,510 | 12.7 |
| Tumor | 13.1 (1.39) | 60 | 7,413 | 8,378 | 8.68 |
| Non-Draining Lymph Node | 20.7 (8.26) | 30 | 6,650 | 6,945 | 7.79 |
| Thymus | 13.5 (5.31) | 30 | 5,070 | 5,572 | 5.94 |
| Draining Lymph Node | 12.9 (0.131) | 60 | 4,818 | 5,222 | 5.70 |
| Heart | 31.6 (6.27) | 5 | 4,869 | 5,189 | 5.64 |
| Esophagus | 12.1 (8.06) | 30 | 2,619 | 2,803 | 3.07 |
| Sk. Muscle | 9.95 (1.41) | 15 | 2,364 | 2,504 | 2.77 |
| Fat | 4.28 (2.55) | 5 | 1,358 | 1,511 | 1.59 |
| RBC | 1.69 (0.957) | 5 | 332 | 352 | 0.389 |
| Brain | 0.627 (0.079) | 15 | 254 | 271 | 0.297 |
| Spinal Cord | 0.307 (0.102) | 15 | 120 | 129 | 0.140 |
Error is presented as SD for Cmax
a.
Observed parameter
b.
AUC are from 0–1440 min with corresponding tissue partition coefficient
c.
All infinity extrapolated AUC portions are < 14%