Table 3.
Glasdegib plasma pharmacokinetics
| Parameter a (unit) |
Glasdegib 100 mg s.d. + Rifampin 600 mg q.d. (Test)
(N = 12) |
Glasdegib 100 mg s.d.
(Reference) (N = 12) |
Mean Ratio b (90% CI) |
|---|---|---|---|
| AUC inf (ng × h ml −1 ) | 2416 (25) | 8145 (23) | 29.66 (26.17–33.62) |
| AUC last (ng × h ml −1 ) | 2385 (26) | 8051 (23) | 29.62 (26.17–33.54) |
| C max (ng ml −1 ) | 455.0 (26) | 703.2 (19) | 64.71 (57.21–73.19) |
| T max (h) | 1.25 (1.00–2.07) | 1.50 (1.00–4.05) | – |
| CL/F (l/h) | 41.38 (25) | 12.27 (23) | – |
| Vz/F (l) | 299.3 (23) | 232.7 (18) | – |
| t 1/2 (h) | 5.11 ± 1.06 | 13.39 ± 2.76 | – |
Geometric mean (geometric %CV) for all except median (range) for T max and arithmetic mean (±standard deviation) for t 1/2.
Adjusted geometric mean ratio for glasdegib in the presence vs. absence of rifampin and confidence interval expressed as percentages.
AUC inf, area under the plasma concentration–time curve from time zero extrapolated to infinity time; AUC last, area under the plasma–concentration curve from time zero to the time of the last quantifiable concentration; CI, confidence interval; C max, maximum observed concentration; CL/F, apparent oral clearance; %CV, percent coefficient of variation; q.d., once daily; s.d., single dose; T max, time to maximum observed concentration; t 1/2, terminal half‐life; Vz/F, apparent volume of distribution