Bioavailability of azacitidine subcutaneous versus intravenous in patients with the myelodysplastic syndromes

Guido Marcucci, Lewis Silverman, Mark Eller, Linda Lintz, C. L. Beach

Research output: Contribution to journalArticlepeer-review

126 Scopus citations

Abstract

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/m2 SC dose, or treatment B, consisting of azacitidine administered as a single 75-mg/m 2 IV 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.

Original languageEnglish
Pages (from-to)597-602
Number of pages6
JournalJournal of Clinical Pharmacology
Volume45
Issue number5
DOIs
StatePublished - May 2005
Externally publishedYes

Keywords

  • Azacitidine
  • Bioavailability
  • Epigenetics
  • Myelodysplastic syndromes
  • Pharmacokinetics

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