Table 2.

PK parameters of taselisib (GDC-0032)

Single doseSteady state
Cohort (dose)NCmax (μmol/L)Tmax (hr)AUC0–24hr (μmol/L•hr)AUCinf (μmol/L•hr)CL/F (mL/hr)t1/2 (hr)Vz/F (L)NCmax (μmol/L)Tmax (hr)Cmin (μmol/L)AUC0–24hr (μmol/L•hr)CLss/F (mL/hr)
Cohort 1 (3 mg)60.0256 (37%)4 (3–8)0.441 (32%)1.48 (33%)4770 (29%)43.8 (26%)301 (45%)60.111 (65%)3 (2–4)0.046 (48%)1.79 (55%)4320 (37%)
Cohort 2 (5 mg)30.0304 (40%)8 (3–8)0.547 (43%)1.64 (54%)9170 (77%)40 (48%)433 (39%)30.091 (53%)3 (2–4)0.042 (55%)1.49 (49%)9150 (64%)
Cohort 3 (8 mg)40.0764 (43%)4 (2–4)1.342 (34%)3.47 (15%)5070 (13%)38.2 (32%)277 (38%)30.188 (63%)3 (2–4)0.098 (55%)3.21 (50%)6310 (44%)
Cohort 5 (12 mg)100.127 (42%)3 (1–8)1.8 (35%)4.00 (30.5%)4750 (77%)36.7 (20%)267 (81%)100.302 (31%)4 (2–24)0.128 (36%)5.1 (40%)4810 (61%)
Cohort 4 (16 mg)110.134 (39%)4 (2–24)2.26 (37%)6.36 (48%)6640 (45%)39.7 (20%)372 (45%)90.441 (52%)4 (2–8)0.241 (76%)8.1 (57%)5440 (61%)
  • NOTE: PK parameters were reported as cohort mean (%CV), except for Tmax, which was reported as cohort median (range).

  • Abbreviations: AUC0–24 hr, area under the plasma concentration–time curve from 0 to 24 hours after dose; AUCinf, area under the plasma concentration−time curve from time 0 to infinity; CL/F, apparent clearance; Cmax, highest observed plasma concentration; Cmin, minimum concentration during the dosing interval; t1/2, terminal half-life; Tmax, time of maximum observed concentration; Vz/F, apparent terminal phase distribution volume.