Table 3: Main pharmacokinetic parameters of BCR/ABL inhibitors.
(1): Cmax once a day 66.8 ng/ml, twice a day 37.6 ng/ml. Cmin: 2.69 vs 5.3 ng/ml.
(2): 400 mg twice a day + 35% compared with once a day.
(3): Alpha glycoprotein.
(4): The increase in bioavailability requires twice daily administration without food 2 hours before and 1 hour following administration.
(5): Administration with food is recommended to improve tolerability.
F: bioavailabiity; Tmax: maximum plasma concentration time; Cmax: maximum concentration in plasma; AUC: area under the curve of plasma concentrations over time; F. prot.: percentage of protein fixation; V: distribution volume; Cl: clearance; Ae: percentage of active drug eliminated in urine; t1/2: mean elimination half-life; Food: influence of food on absorbtion.
| Bosutinib | Dasatinib | Imatinib | Nilotinib | Ponatinib |
| F (%) | 33.8 | 14-34 | 98 | 30-50 | - |
| Tmax (h) | 3-6 | 0.5-3 | 1.5-6 | 3 | 4.6 |
| Dose (mg) | 500 | 100 | 400 | 400 | 45 |
| Cmax (ng/ml) | 112±29 | 29 | 1600 | 508 (2) | 77 |
| AUC (ng x h/ml) | 2740±790 | (1) | 24.8 mg h/l | 145656 | 1296 |
| F. prot. (%) | 96 | 9 | 6 95 (3) | 98 (3) | 99 |
| V (l) | 9560 | 2505 | - | 579 | 1101 |
| Cl (l/h) | 197 | - | - | 29.1 | 3535 |
| Ae (%) | 1 | 0.1 | 5 | <1 | <1 |
| t1/2 (h) | 32-41 | 5.6 | 18 | 17 | 22 |
| Food | + AUC x 1.5 (5) | - | - | + AUC 112% (4) | - |