Tissue pharmacokinetic parameters of drug radioequivalents in female and male rats following oral administration of [14C]CP-544439 at a dose of 275 mg/kg
AUC(0-tlast) values (μg eq · h/g) were calculated using linear trapezoidal approximation. t1/2 (h) was calculated as 0.693/Kel. Cmax and Tmax values were reported as μg eq/g and h, respectively.
Female Rat | Male Rat | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| AUC0-tlast | Cmax | Tmax | t1/2 | AUC0-tlast | Cmax | Tmax | t1/2 | |||||||
| Adipose: Brown | 204 | 20 | 6 | —a | 221 | 18 | 18 | — | ||||||
| Adrenal Gland | 257 | 24 | 6 | — | 329 | 26 | 18 | — | ||||||
| Blood: Arterial | 89 | 25 | 6 | — | 94 | 20 | 6 | — | ||||||
| Blood: Hepatic | 65 | 15 | 1 | — | 339 | 22 | 18 | — | ||||||
| Blood: Myocardial | 436 | 22 | 6 | 11 | 579 | 22 | 18 | — | ||||||
| Blood: Venous | 256 | 19 | 6 | — | 328 | 23 | 18 | — | ||||||
| Bone Marrow: Femur | 198 | 18 | 6 | — | 240 | 17 | 18 | — | ||||||
| Bone Marrow: Vertebra | 156 | 12 | 6 | — | 160 | 11 | 3 | — | ||||||
| Buccal Gland | — | 15 | 6 | — | 155 | 14 | 18 | — | ||||||
| Cerebellum | 87 | 6 | 6 | — | 119 | 12 | 18 | — | ||||||
| Cerebrum | 95 | 7 | 6 | — | 117 | 10 | 18 | — | ||||||
| Clitoridean/Preputial Gland | 196 | 17 | 6 | — | 275 | 31 | 18 | — | ||||||
| Gastric Mucosa | 270 | 22 | 6 | — | 270 | 25 | 1 | — | ||||||
| Harderian Gland | — | 21 | 6 | — | 625 | 43 | 18 | — | ||||||
| Kidney | 601 | 46 | 6 | 8 | 505 | 35 | 18 | — | ||||||
| Lacrimal Gland: Exorbital | 77 | 7 | 1 | 22 | 1828 | 81 | 18 | — | ||||||
| Lacrimal Gland: Intraorbital | 206 | 19 | 6 | — | 325 | 26 | 18 | — | ||||||
| Liver | 680 | 47 | 6 | 9 | 1218 | 46 | 18 | — | ||||||
| Lung | 242 | 19 | 6 | — | 520 | 21 | 18 | — | ||||||
| Muscle | 39 | 10 | 6 | — | 112 | 9 | 18 | — | ||||||
| Myocardium | 207 | 19 | 6 | — | 267 | 18 | 18 | — | ||||||
| Ovary | 165 | 8 | 1 | — | N.P.b | |||||||||
| Pancreas | 216 | 22 | 6 | — | 245 | 18 | 18 | — | ||||||
| Parotid Gland | 51 | 19 | 6 | — | 228 | 19 | 18 | — | ||||||
| Periodontal Ligament | 8765 | 80 | 168 | — | 9921 | 99 | 168 | — | ||||||
| Renal Cortex | 114 | 35 | 6 | — | 396 | 28 | 18 | — | ||||||
| Renal Medulla | 185 | 53 | 6 | — | 579 | 41 | 18 | — | ||||||
| Salivary Gland: Sublingual | 44 | 11 | 1 | — | 252 | 20 | 18 | — | ||||||
| Salivary Gland: Submaxillary | 201 | 19 | 6 | — | 250 | 20 | 18 | — | ||||||
| Seminal Vesicle | N.P. | 420 | 42 | 18 | — | |||||||||
| Skin | 90 | 5 | 6 | — | 92 | 7 | 18 | — | ||||||
| Spleen | 171 | 15 | 6 | — | 182 | 13 | 18 | — | ||||||
| Thymus | 34 | 8 | 6 | — | 22 | 5 | 6 | — | ||||||
| Uvea | 34 | 12 | 6 | — | 147 | 13 | 18 | — | ||||||
| Whole-Body | 1220 | 104 | 6 | 6 | 2416 | 145 | 6 | 6 | ||||||