Absolute bioavailability of imatinib (Glivec®) orally versus intravenous infusion

The purpose of this study was to investigate the absolute bioavailability of a single oral dose of imatinib (Glivec(R)), 400 mg (capsules vs. oral solution), compared with imatinib, 100 mg (intravenous [i.v] infusion), in healthy subjects. Twelve subjects received a single treatment in each treatment period: a 400-mg oral dose of imatinib in capsule form or as a solution or a 100-mg i.v. infusion of imatinib. Plasma imatinib concentrations were measured following each treatment; pharmacokinetic parameters and absolute bioavailability were determined. Absolute bioavailability values (compared with i.v infusion) for the imatinib capsule and oral solution were 98.3% and 97.2%, respectively. Both the rate and extent of imatinib absorption, as measured by C-max, partial AUC, and total AUC, were similar for the oral solution and the imatinib capsule intended for the market. The 400-mg oral dose of imatinib, as a capsule or a solution, was completely absorbed and was; almost completely bioavailable (>97%).