Mean (±S.D.) percentage of [14C]GDC-0973 bound in mouse, rat, dog, cynomolgus monkey, human plasma, human AAG, and HSA
| Matrix/Species | Total GDC-0973 Concentrationa | Percentage Unbound [14C]GDC-0973 |
|---|---|---|
| μM | ||
| Mouse | 1 | 4.1 ± 0.8 |
| 5 | 3.4 ± 0.1 | |
| 10 | 3.3 ± 0.2 | |
| Rat | 1 | 2.8 ± 0.4 |
| 5 | 3.5 ± 0.4 | |
| 10 | 3.7 ± 0.3 | |
| Dog | 1 | 0.7 ± 0.0 |
| 5 | 1.2 ± 0.2 | |
| 10 | 1.4 ± 0.2 | |
| Cynomolgus monkey | 1 | 4.5 ± 1.1 |
| 5 | 4.4 ± 0.3 | |
| 10 | 4.8 ± 0.3 | |
| Human | 1 | 5.2 ± 0.4 |
| 5 | 6.5 ± 0.4 | |
| 10 | 5.8 ± 0.2 | |
| AAG, 1 mg/ml | 1 | 4.4 ± 0.6 |
| 5 | 4.2 ± 0.2 | |
| 10 | 5.3 ± 0.1 | |
| HSA, 40 mg/ml | 1 | 46.9 ± 14.9 |
| 5 | 40.8 ± 0.2 | |
| 10 | 40.8 ± 1.2 |
↵a Unlabeled + [14C]-labeled GDC-0973 (free-base equivalents).