Table 2.
Summary of PK parameters for radioactivity, entrectinib and M5 after single dose [14C]entrectinib in healthy volunteers
| Analyte | N | Tmax (h) | Cmax (μM) | AUC0–24 (μM•h) | AUCinf (μM•h) | t1/2 (h) |
|---|---|---|---|---|---|---|
| Blood radioactivity | 6 | 4.0 (2.5, 5.0) | 5.38 (27) | 90.3 (31) | 180 (40) | 22.5 (15) |
| Plasma radioactivity | 6 | 3.0 (3.0, 8.0) | 2.99 (37) | 47.3 (46) | 104 (54) | 24.3 (16) |
| Entrectinib | 6 | 3.0 (3.0, 4.0) | 1.81 (38) | 22.6 (42) | 36.6 (47) | 18.5 (17) |
| M5 | 6 | 4.0 (3.0, 6.0) | 0.379 (67) | 4.83 (67) | 13.5 (61) | 43.9 (16) |
Values are mean (CV%) except for Tmax which is median (min, max)
Dosing was conducted under fasted conditions