Table 3.
Extensive PK Study Tissue PK and Partition Coefficients
| Tissue | Cmax (ng/mL) | Tmax (min) | AUC0-t (μg/mL•min) | AUC0-∞ (μg/mL•min)b | Partition Coefficient |
|---|---|---|---|---|---|
|
| |||||
| Plasma | 649 (266) | 15 | 30.7 (4.7) | 32.3 (4.7) | |
| RBC | 209 (84) | 15 | 9.7 (2.52) | 10.0 (2.52) | 0.311 (0.075) |
| Liver | 6,272 (3,194) | 15 | 310 (41) | 329 (41) | 10.2 (2.0) |
| Kidneys | 996 (387) | 15 | 56.3 (6.6) | 65.5 (6.6) | 2.03 (0.36) |
| Spleen | 519 (83) | 15 | 29.7 (8.7) | 31.2 (8.7) | 0.966 (0.305) |
| Lungs | 1,200 (64) | 15 | 49.2 (6.2) | 51.5 (6.2) | 1.60 (0.30) |
| Heart | 1,077 (825) | 15 | 37.3 (8.7) | 39.1 (8.7) | 1.21 (0.32) |
| Fat | 314 (170) | 15 | 24.3 (2.9) | 27.1 (2.9) | 0.841 (0.152) |
| Muscle | 274 (119) | 15 | 14.7 (2.8) | 15.3 (2.8) | 0.473 (0.111) |
| Brain | 204 (79) | 15 | 8.97 (1.45) | 9.8 (1.45) | 0.303 (0.063) |
| Tumor | 356 (88) | 15 | 20.2 (2.3) | 22.1 (2.3) | 0.685 (0.122) |
| Small Intestine | 9,933 (9,932) | 5 | 434 (75) | 453 (75) | 14.0 (3.1) |
| Draining Lymph Node | 945 (493) | 15 | 43.2 (7.0) | 47.1 (7.0) | 1.46 (0.31) |
| Non-draining Lymph Node | 946 (339) | 15 | 39.0 (4.5) | 42.1 (4.5) | 1.31 (0.24) |
| Esophagus | 17,812 (2,058) | 15 | 430.7 (103) | 436 (103) | 13.5 (3.8) |
| Spinal Cord | 179 (35) | 15 | 145 (22) | 9.83 (22) | 0.305 (0.064) |
| Thymus | 999 (336) | 15 | 32.6 (7.1) | 35.5 (7.1) | 1.10 (0.27) |
| Bone Marrowa | 2,341 (937) | 15 | 63.6 (10.0) | 85.4 (10.0) | 2.65 (0.50) |
Error is presented as SD for Cmax and SEM for AUC.
a.
Bone marrow fellow below LLQ after 120 min, and reported AUC is from 0-120 min. The partition coefficients with a plasma AUC from the same time
b.
All infinity extrapolated AUC portions are <1%, except for bone marrow which is 25.6%