Advanced search×

Effects of nilotinib on single-dose warfarin pharmacokinetics and pharmacodynamics: a randomized, single-blind, two-period crossover study in healthy subjects.

Ophelia Q P Yin, Neil Gallagher, Deirdre Fischer, Lily Zhao, Wei Zhou, Elisabeth Leroy, Georg Golor, and Horst Schran

Clin Drug Investig 31(3):169-79 (2011) PMID 21184622

Nilotinib (Tasigna®), a highly selective and potent BCR-ABL tyrosine kinase inhibitor, is approved for the treatment of chronic myeloid leukaemia in the chronic phase (CML-CP) and the accelerated phase (CML-AP) in patients resistant or intolerant to prior therapy, including imatinib. Nilotinib has shown competitive inhibition of cytochrome P450 enzyme (CYP) 2C9 in vitro, but its effect on CYP2C9 activity in humans is unknown. This study evaluated the effects of nilotinib on the pharmacokinetics and pharmacodynamics of warfarin, a sensitive CYP2C9 substrate, in healthy subjects.

DOI: 10.2165/11538700-000000000-00000
Version: za2963e q8za8 q8zba q8zce q8zd1 q8zef q8zf7 q8zg6
Buy PDF

Similar articles you may find interesting…

  1. The prokinetic cinitapride has no clinically relevant pharmacokinetic interaction and effect on QT during coadministration with ketoconazole...
    Marta M Robert, Miquel M Salvà, ... Georg G Golor

    Drug Metab Dispos 35(7):1149-56 (2007) PMID 17437965

    The present clinical trial was designed to evaluate the possible pharmacokinetic and electrocardiographic interactions of the gastroenteric prokinetic drug cinitapride with ketoconazole. The safety and tolerability of the study treatments were also evaluated. After a placebo-controlled, double-blind...
    Buy PDF
  2. Histone H2A deubiquitinase activity of the Polycomb repressive complex PR-DUB.
    Johanna C JC Scheuermann, Andrés Gaytán AG de Ayala Alonso, ... Jürg J Müller

    Nature 465(7295):243-7 (2010) PMID 20436459 PMCID PMC3182123

    We show that the uncharacterized Drosophila PcG gene calypso encodes the ubiquitin carboxy-terminal hydrolase BAP1. Biochemically purified Calypso exists in a complex with the PcG protein ASX, and this complex, named Polycomb repressive deubiquitinase (PR-DUB), is bound at PcG target genes in Drosop...
    View PDF
  3. Safety of hydroxocobalamin in healthy volunteers in a randomized, placebo-controlled study.
    Wolfgang W Uhl, Arno A Nolting, ... Andreas A Kovar

    Clin Toxicol (Phila) (2006) PMID 16990190

    This randomized, double-blind, placebo-controlled, ascending-dose study was conducted in healthy volunteers to evaluate the safety of the investigational cyanide antidote hydroxocobalamin. Four ascending dosing groups received intravenous doses of 2.5, 5, 7.5 or 10 g...
    Buy PDF