Table 1.
Pharmacokinetic parameter estimates for imatinib and N-desmethyl-imatinib (CGP74588) after oral administration of imatinib alone and with co-administration of a PPI (omeprazole) (n= 12)
| AUC(0,∞) | Cmax | tmax | t1/2 | V/F | CL/F | ||
|---|---|---|---|---|---|---|---|
| Analyte | Arm | (µg ml−1 h) | (µg ml−1) | (h) | (h) | (l) | (l h−1) |
| Imatinib | Alone | 34.1 (11.1) | 2.04 (0.56) | 3.0 (0.9) | 13.4 (1.5) | 244 (130) | 14.1 (9.5) |
| + PPI | 33.1 (9.3) | 2.02 (0.65) | 3.1 (1.2) | 14.1 (1.9) | 273 (168) | 15.2 (12.6) | |
| P value | 0.64 | 0.97 | 0.78 | 0.13 | 0.14 | 0.64 | |
| CGP74588 | Alone | 6.95 (2.46) | 0.27 (0.06) | 2.6 (1.2) | 31.6 (10.3) | 2494 (839) | 62.8 (17.3) |
| + PPI | 6.77 (1.81) | 0.28 (0.07) | 3.7 (0.9) | 32.1 (12.6) | 2545 (801) | 63.2 (17.7) | |
| P value | 0.79 | 0.91 | 0.82 | 0.97 | 0.87 | 0.78 |
The data are expressed as mean (SD). The percentage of the AUC(0,∞) extrapolated beyond Clast was < 6% for imatinib and < 45% for CGP74588. P values were obtained after log-transformation of the parameters by use of the non-parametrically two-tailed exact Wilcoxon signed rank test (paired data).