Table 3.
Predicted tissue exposure in humans given a single 100 μCi IV dose of [14C] VNP40101M.
| Organ system | Organ/Tissue |
Cmax (μCi/g) |
Tmax (h) |
r2 | # of pts for t1/2 |
t1/2 (h) |
AUCinf (obs) (μCi-h/g) |
D Rat (rem) |
D Human (rem) |
D Human (mrem) |
|---|---|---|---|---|---|---|---|---|---|---|
| Adipose | Adipose (brown) | 0.0360 | 1.00 | 0.99 | 4 | 147 | 2.032 | 0.213 | 0.00389 | 3.8882 |
| Adipose (white) | 0.0086 | 0.50 | 0.96 | 3 | 262 | 0.688 | 0.072 | 0.00132 | 1.3159 | |
| Alimentary Canal | Cecum | 0.0320 | 1.00 | 0.99 | 5 | 76 | 1.132 | 0.119 | 0.00217 | 2.1661 |
| Large intestine | 0.0263 | 0.50 | 0.88 | 3 | 170 | 1.242 | 0.130 | 0.00238 | 2.3765 | |
| Small intestine | 0.1327 | 3.00 | 0.86 | 4 | 62 | 1.234 | 0.130 | 0.00236 | 2.3617 | |
| Stomach | 0.0381 | 1.00 | 0.95 | 4 | 79 | 0.978 | 0.103 | 0.00187 | 1.8705 | |
| Central Nervous System | Brain (cerebellum) | 0.0165 | 0.50 | 0.89 | 4 | 114 | 0.731 | 0.077 | 0.00140 | 1.3989 |
| Brain (cerebrum) | 0.0155 | 0.50 | 0.98 | 3 | 125 | 0.592 | 0.062 | 0.00113 | 1.1335 | |
| Brain (medulla) | 0.0141 | 0.50 | 0.93 | 4 | 114 | 0.544 | 0.057 | 0.00104 | 1.0409 | |
| Spinal cord | 0.0118 | 0.50 | 0.99 | 4 | 97 | 0.465 | 0.049 | 0.00089 | 0.8892 | |
| Dermal | Skin | 0.0296 | 0.50 | 0.88 | 5 | 66 | 1.294 | 0.136 | 0.00248 | 2.4766 |
| Endocrine | Adrenal gland | 0.0374 | 0.50 | 0.88 | 5 | 152 | 2.440 | 0.256 | 0.00467 | 4.6680 |
| Pituitary gland | 0.0439 | 3.00 | 0.88 | 4 | 104 | 1.167 | 0.123 | 0.00223 | 2.2329 | |
| Thyroid | 0.0464 | 1.00 | 1.00 | 3 | 87 | 1.143 | 0.120 | 0.00219 | 2.1859 | |
| Excretory/Metabolic | Liver | 0.0924 | 1.00 | 0.95 | 3 | 119 | 2.542 | 0.267 | 0.00486 | 4.8643 |
| Renal cortex | 0.2238 | 1.00 | 0.97 | 6 | 82 | 2.597 | 0.273 | 0.00497 | 4.9679 | |
| Renal medulla | 0.0826 | 0.50 | 0.92 | 6 | 79 | 2.086 | 0.219 | 0.00399 | 3.9916 | |
| Urinary bladder | 0.0363 | 24.00 | 0.89 | 4 | 81 | 2.374 | 0.249 | 0.00454 | 4.5425 | |
| Ocular | Eye Lens | 0.0034 | 8.00 | 1.00 | 2 | ND | 0.267 | 0.028 | 0.00051 | 0.5115 |
| Eye Uveal tract | 0.0261 | 0.50 | 0.89 | 5 | 61 | 0.493 | 0.052 | 0.00094 | 0.9434 | |
| Reproductive | Epididymis | 0.0279 | 3.00 | 0.87 | 6 | 96 | 0.768 | 0.081 | 0.00147 | 1.4688 |
| Prostate gland | 0.0184 | 0.50 | 0.96 | 5 | 65 | 0.724 | 0.076 | 0.00139 | 1.3851 | |
| Seminal vesicles | 0.0180 | 0.50 | 0.89 | 6 | 107 | 0.895 | 0.094 | 0.00171 | 1.7129 | |
| Testis | 0.0233 | 3.00 | 0.87 | 5 | 100 | 0.623 | 0.065 | 0.00119 | 1.1920 | |
| Respiratory | Lung | 0.0560 | 1.00 | 0.86 | 5 | 136 | 4.591 | 0.482 | 0.00878 | 8.7836 |
| Secretory | Harderian gland | 0.0966 | 3.00 | 0.99 | 6 | 51 | 1.481 | 0.156 | 0.00283 | 2.8342 |
| Pancreas | 0.0989 | 3.00 | 0.94 | 5 | 80 | 1.882 | 0.198 | 0.00360 | 3.6002 | |
| Salivary gland | 0.0347 | 0.50 | 0.96 | 5 | 84 | 1.142 | 0.120 | 0.00219 | 2.1851 | |
| Skeletal/Muscular | Bone | 0.0032 | 0.50 | 1.00 | 2 | ND | 0.141 | 0.015 | 0.00027 | 0.2695 |
| Heart | 0.0381 | 0.50 | 0.96 | 6 | 90 | 1.717 | 0.180 | 0.00328 | 3.2844 | |
| Skeletal muscle | 0.0275 | 0.50 | 0.93 | 6 | 135 | 1.544 | 0.162 | 0.00295 | 2.9543 | |
| Vascular/Lymphatic | Blood | 0.0468 | 3.00 | 0.92 | 4 | 138 | 6.836 | 0.718 | 0.01308 | 13.0793 |
| Bone marrow | 0.0359 | 1.00 | 1.00 | 3 | 57 | 1.157 | 0.122 | 0.00221 | 2.2141 | |
| Lymph node | 0.0399 | 0.50 | 0.97 | 4 | 66 | 1.192 | 0.125 | 0.00228 | 2.2808 | |
| Spleen | 0.0407 | 1.00 | 0.89 | 6 | 108 | 1.930 | 0.203 | 0.00369 | 3.6933 | |
| Thymus | 0.0536 | 3.00 | 0.92 | 5 | 65 | 1.575 | 0.165 | 0.00301 | 3.0140 |
ND, Not determined; unable to determine this value from the data.