TABLE 1

Steady-state GDC-0853 (fenebrutinib) pharmacokinetic parameters (geometric mean, CV%) for BID fenebrutinib administered alone on day 20, and in combination with a single dose of 7.5 mg of methotrexate (MTX) on day 21

PK Parameter200-mg Fenebrutinib
Day 20, Fasting (n = 13)a+ 7.5 mg MTX Day 21, Fasting (n = 13)b
tmax,ss (h)c1.00 (0.50–2.00)0.50 (0.50–2.00)
Cmax,ss (ng/ml)659 (54.1)673 (51.4)
AUC0–12,ss (ng·h/ml)3270 (45.2)3360 (39.2)
t1/2,ss (h)4.63 (16.0)6.87 (28.5)
Geometric mean ratio of AUC0–12,ss (90% CI)NA1.03 (0.95–1.11)
Geometric mean ratio of Cmax,ss (90% CI %)NA1.02 (0.90–1.15)
  • AUC, area under the plasma concentration–time curve; BID, twice daily; CI, confidence interval; NA, not applicable; PK, pharmacokinetic.

  • a Single dose of 200 mg of fenebrutinib BID on days 15–20 under fasting conditions (an overnight fast for the morning dose and a 2-hour fast for the evening dose).

  • b Single dose of 200 mg of fenebrutinib (along with 7.5 mg of MTX) on day 21 under fasting conditions.

  • c Median (range).