Effect of grapefruit juice on the pharmacokinetics of nilotinib in healthy participants.

Journal of Clinical Pharmacology
Ophelia Q P YinHorst Schran

Abstract

Nilotinib (Tasigna; Novartis Pharmaceuticals) is a second-generation BCR-ABL tyrosine kinase inhibitor newly approved for the treatment of imatinib-resistant or imatinib-intolerant Philadelphia chromosome positive (Ph+) chronic myeloid leukemia in chronic phase or accelerated phase. This study evaluated the effect of grapefruit juice on the pharmacokinetics of nilotinib in 21 healthy male participants. All participants underwent 2 study periods during which they received a single oral dose of 400 mg nilotinib with 240 mL double-strength grapefruit juice or 240 mL water in a crossover fashion. Serial blood samples were collected for the determination of serum nilotinib concentrations by a validated liquid chromatography/tandem mass spectrometry assay. Concurrent intake of grapefruit juice increased the nilotinib peak concentration (C(max)) by 60% and the area under the serum concentration-time curve (AUC(0-infinity)) by 29% but did not affect the time to reach C(max) or the elimination half-life of nilotinib. The most common adverse events were headache and vomiting, which were mild or moderate in severity, and their frequency appeared to be similar between 2 treatments. Based on the currently available information about nilotin...Continue Reading

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Citations

Oct 17, 2012·Cancer Chemotherapy and Pharmacology·Ophelia Q P YinSteven Novick
Nov 20, 2012·Journal of Nutrition in Gerontology and Geriatrics·Roschelle Heuberger
Sep 3, 2009·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·George D DemetriPeter Reichardt
Nov 28, 2012·CMAJ : Canadian Medical Association Journal = Journal De L'Association Medicale Canadienne·David G BaileyJ Malcolm O Arnold
Dec 15, 2010·Drugs·Kay SedenDavid Back
Feb 25, 2011·Future Oncology·Paula Garland, Jane Apperley
May 11, 2011·Medicinski pregled·Zoran Z BojanićVladmila V Bojanić
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Oct 14, 2014·Journal of Pharmaceutical Sciences·Jie ShaoGuohua An
Apr 1, 2011·Seminars in Oncology·Jonathan Trent, Mathieu Molimard
Aug 13, 2010·Journal of Clinical Pharmacology·Chiaki TanakaHorst Schran
May 1, 2013·Drug Metabolism and Pharmacokinetics·Min-Jung KimJae-Gook Shin
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Jun 30, 2011·Journal of Clinical Pharmacology·Ophelia Q P YinHorst Schran
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Dec 19, 2018·International Journal of Molecular Sciences·Jeong-Hyeon KoKwang Seok Ahn

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