Bioavailability of Azacitidine Subcutaneous Versus Intravenous in Patients With the Myelodysplastic Syndromes.

Autor: Marcucci, Guido, Silverman, Lewis, Eller, Mark, Lintz, Linda, Beach, C. L.
Zdroj: Journal of Clinical Pharmacology; May2005, Vol. 45 Issue 5, p597-602, 6p
Abstrakt: The primary objectives of this study were to characterize the absolute bioavailability of azacitidine after subcutaneous (SC) administration and to compare the single-dose pharmacokinetics of azacitidine following SC and intravenous (IV) administration. Six patients with myelodysplastic syndromes were randomly assigned according to a crossover design to treatment A, consisting of azacitidine administered as a single 75-mg/m2SC dose, or treatment B, consisting of azacitidine administered as a single 75-mg/m2IV infusion dose over 10 minutes. A minimum of 7 days and a maximum of 28 days were permitted between treatments. The study demonstrated good bioavailability of a SC azacitidine dose compared to an IV infusion treatment. The exposure profiles following SC drug administration illustrate measurable azacitidine levels with bioavailability (AUC) values within 89% of those measured following IV administration (range, 70%-112%). The median IV half-life was 0.36±0.02 hours compared to 0.69±0.14 hours for SC administration. Regardless of the route of administration, a single dose of azacitidine, 75 mg/m2, was generally well tolerated. [ABSTRACT FROM PUBLISHER]
Databáze: Complementary Index