Table 2.
Plasma PK parameters for brigatinib
| Parameter a |
Normal
Hepatic Function (n=9) |
Mild
(Child-Pugh A) Hepatic Impairment (n=6) |
Moderate
(Child-Pugh B) Hepatic Impairment (n=6) |
Severe
(Child-Pugh C) Hepatic Impairment (n=6) |
|---|---|---|---|---|
| Tmax (h) | 2.00 (1.00‒6.00) | 1.75 (1.00‒3.00) | 2.00 (0.50‒3.00) | 0.50 (0.50‒3.00) |
| Cmax,u (ng/mL) | 30.3 (27.2) | 28.7 (9.5) | 27.8 (24.8) | 50.0 (34.5) |
| AUC0−last,u (h·ng/mL) | 581 (25.0) | 522 (24.6) | 578 (38.3) | 781 (20.7) |
| AUC0−∞,u (h·ng/mL) | 603 (25.0) | 539 (24.9) | 601 (39.8) | 829 (20.0) |
| CL/Fu (L/h) | 149 (25.0) | 167 (24.9) | 150 (39.8) | 109 (20.0) |
| Vz/Fu (L) | 10,200 (31.0) | 11,300 (45.8) | 10,500 (29.5) | 7,990 (33.2) |
| t1/2 (h) | 47.6 (29.1) | 47.0 (30.9) | 48.7 (22.0) | 51.0 (26.1) |
AUC0−∞,u unbound area under the plasma concentration-time curve from time 0 to infinity, AUC0−last,u unbound area under the plasma concentration-time curve from time 0 to the time of the last measurable concentration, CL/Fu unbound apparent oral clearance, Cmax,u unbound maximum observed plasma concentration, PK pharmacokinetic, t1/2 terminal elimination half-life, Tmax time to first maximum observed plasma concentration, Vz / Fu unbound apparent volume of distribution during the terminal disposition phase
aData are presented as geometric mean (geometric % coefficient of variation) with the exception of Tmax, which is presented as the median (range)