Tissue-to-blood ratios of radioactivity in selected tissues after oral administration of [14C]-osimertinib (4 mg/kg) to male partially pigmented rats and male and female albino rats
Male Partially Pigmented Rats | Male Albino Rats | Female Albino Rats | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
0.5 h | 1 h | 6 h | 24 h | 2 days | 7 days | 21 days | 60 days | 1 h | 6 h | 24 h | 1 h | 6 h | 24 h | |
Bile ducts | 63.4 | 56.5 | 28.7 | 2.63 | 1.57 | 0.39 | NC | NC | 66.8 | 27.4 | 2.99 | 29.1 | 19.0 | 3.25 |
Blood | 1.00 | 1.00 | 1.00 | 1.00 | 1.00 | 1.00 | 1.00 | NC | 1.00 | 1.00 | 1.00 | 1.00 | 1.00 | 1.00 |
Brain | 1.06 | 2.17 | 1.85 | 0.37 | 0.19 | 0.22 | 0.23 | NC | 1.41 | 1.80 | 0.24 | 2.09 | 2.25 | 0.49 |
Liver | 32.6 | 24.5 | 13.3 | 3.23 | 2.18 | 1.01 | 0.41 | NC | 29.6 | 17.3 | 4.47 | 35.8 | 18.6 | 4.60 |
Lung | 14.0 | 21.3 | 20.4 | 3.11 | 1.24 | 0.85 | 0.81 | NC | 25.2 | 33.9 | 3.21 | 37.3 | 43.1 | 6.10 |
Muscle | 0.90 | 1.68 | 2.01 | 0.46 | 0.38 | 0.41 | 0.27 | NC | 1.95 | 2.33 | 0.41 | 2.51 | 2.15 | 0.55 |
Ovary | ND | ND | ND | ND | ND | ND | ND | ND | ND | ND | ND | 5.38 | 14.6 | 1.94 |
Pituitary | 11.6 | 10.5 | 23.8 | 5.35 | 2.31 | 1.22 | 1.05 | NC | 14.9 | 32.9 | 14.3 | 12.0 | 31.9 | 13.6 |
Renal cortex | 11.7 | 15.7 | 22.2 | 11.4 | 8.40 | 4.07 | 1.06 | NC | 18.5 | 26.4 | 13.9 | 18.3 | 15.2 | 4.69 |
Renal medulla | 3.82 | 9.30 | 11.5 | 2.89 | 1.89 | 1.12 | 0.60 | NC | 10.6 | 14.5 | 2.87 | 17.5 | 20.00 | 3.00 |
Skin (non-pigmented) | 0.640 | 1.40 | 2.18 | 0.578 | 0.310 | 0.199 | 0.147 | NC | ND | ND | ND | ND | ND | ND |
Skin (pigmented) | 1.01 | 2.10 | 2.87 | 3.15 | 2.02 | 5.34 | 0.170 | NC | ND | ND | ND | ND | ND | ND |
Skin | ND | ND | ND | ND | ND | ND | ND | ND | 1.30 | 2.22 | 0.49 | 0.77 | 1.82 | 1.18 |
Spleen | 11.1 | 19.4 | 22.7 | 5.38 | 3.09 | 2.77 | 3.40 | NC | 23.8 | 26.6 | 4.07 | 29.2 | 32.7 | 10.8 |
Testis | 0.44 | 0.77 | 2.47 | 1.08 | 0.77 | 0.76 | 0.68 | NC | 0.58 | 1.71 | 0.70 | — | — | — |
Thyroid | 13.9 | 12.1 | 10.8 | 2.63 | 1.71 | 1.84 | 1.27 | NC | 18.7 | 20.1 | 2.94 | 20.3 | 15.1 | 3.16 |
Uvea and RPE | 7.62 | 15.0 | 71.9 | 97.2 | 173 | 151 | 180 | NC | 3.34 | 3.72 | 1.06 | 2.94 | 1.39 | 0.79 |
NC, not calculable; ND, not done; RPE, retinal pigment epithelium; —, not applicable.