TABLE 3.
Tissue pharmacokinetic parameters following a single oral dose of 90 mg/kg 14C-omadacycline in LEH ratsa
| Tissue | Tmax (h) | Cmax (ng · eq/g) | AUClast (ng · eq · h/g) | AUC0–∞ (ng · eq · h/g) | t1/2 (h) | t/b |
|
|---|---|---|---|---|---|---|---|
| Cmax | AUClast | ||||||
| Blood | 3 | 125 | 2,210 | 3,030 | 13 | 1.0 | 1.0 |
| Adrenal cortex | 1 | 1,760 | 4,470 | 5,920 | 2.9 | 14.1 | 2.02 |
| Adrenal medulla | NA | NA | NA | NA | NA | NA | NA |
| Bile | NA | NA | NA | NA | NA | NA | NA |
| Bone marrow | 7 | 492 | 9,630 | NA | NA | 3.94 | 4.36 |
| Bone mineral | 3 | 1,460 | 28,100 | NA | NA | 11.7 | 12.7 |
| Brain | 7 | 67.3 | 364 | NA | NA | 0.53 | 0.16 |
| Brown fat | NA | NA | NA | NA | NA | NA | NA |
| Colon wall | 7 | 3,060 | 11,500 | NA | NA | 24.5 | 5.20 |
| Epididymis | NA | NA | NA | NA | NA | NA | NA |
| Esophagus | 3 | 19,400 | 84,800 | 109,000 | 3.5 | 155 | 38.4 |
| Eye | 3 | 74.1 | 173 | NA | NA | 0.59 | 0.078 |
| Harderian gland | 7 | 1,070 | 17,100 | NA | NA | 8.56 | 7.74 |
| Heart | 0.5 | 349 | 5,030 | 7,320 | 15 | 2.79 | 2.28 |
| Kidney cortex | 1 | 721 | 9,240 | 11,000 | 9.3 | 5.77 | 4.18 |
| Kidney medulla | 1 | 722 | 8,450 | 10,900 | 11 | 5.78 | 3.82 |
| Kidney pelvis | 0.5 | 1,580 | 9,360 | 10,500 | 7.9 | 12.6 | 4.24 |
| Liver | 0.5 | 1,510 | 16,400 | 21,300 | 12 | 12.1 | 7.42 |
| Lung | 3 | 328 | 4,240 | 6,900 | 16 | 2.62 | 1.92 |
| Lymph node | NA | NA | NA | NA | NA | NA | NA |
| Muscle | 3 | 267 | 1,330 | NA | NA | 2.14 | 0.60 |
| Pancreas | 7 | 608 | 3,200 | NA | NA | 4.86 | 1.45 |
| Pituitary gland | 1 | 346 | 1,400 | 2,590 | 5.4 | 2.77 | 0.63 |
| Salivary gland | 7 | 974 | 15,000 | NA | NA | 7.79 | 6.79 |
| Seminal vesicle(s) | NA | NA | NA | NA | NA | NA | NA |
| Skin | 7 | 395 | 1,860 | NA | NA | 3.16 | 0.84 |
| Small intestine wall | 3 | 7,030 | 27,100 | NA | NA | 56.2 | 12.3 |
| Spinal cord | 7 | 77.3 | 409 | NA | NA | 0.62 | 0.19 |
| Spleen | 1 | 1,680 | 13,800 | 16,300 | 9 | 13.4 | 6.24 |
| Stomach, glandular | 1 | 5,940 | 28,800 | 32,300 | 6.9 | 47.5 | 13.0 |
| Testis | 3 | 171 | 822 | NA | NA | 1.37 | 0.37 |
| Thymus | 3 | 322 | 5,960 | NA | NA | 2.58 | 2.70 |
| Thyroid gland | 7 | 729 | 3,790 | NA | NA | 5.83 | 1.71 |
| Uveal tract | NA | NA | NA | NA | NA | NA | NA |
| White fat | NA | NA | NA | NA | NA | NA | NA |
a
Tissue-to-blood concentration ratios (t/b) were calculated using either AUClast or Cmax. NA: not applicable.