Eribulin mesylate pharmacokinetics in patients with solid tumors receiving repeated oral ketoconazole.

Investigational New Drugs
L A DevrieseJ H M Schellens

Abstract

Purpose To study the influence of repeated oral administration of ketoconazole, a potent CYP3A4 inhibitor, on the plasma pharmacokinetics of eribulin mesylate administered by single-dose intravenous infusion. Eribulin mesylate is a non-taxane microtubule dynamics inhibitor that is currently under development in phase I-III trials for the treatment of solid tumors. Experimental design A randomized, open-label, two treatments, two sequences, crossover phase I study was performed in patients with advanced solid tumors. Treatments were given on day 1 and day 15 and consisted of 1.4 mg/m(2) eribulin mesylate alone or 0.7 mg/m(2) eribulin mesylate plus 200 mg ketoconazole on the day of eribulin mesylate administration and the following day. Pharmacokinetic sampling for determination of eribulin plasma concentration was performed up to 144 h following administration of eribulin mesylate. Also safety and anti-tumor activity were determined. Results Pharmacokinetic sampling and analysis was completed in ten patients. Statistical analysis of dose-normalized log-transformed AUC0-∞ and Cmax indicated that single-dose exposure of eribulin was not statistically different when co-administered with ketoconazole (ratio of geometric least square...Continue Reading

References

Jan 1, 1976·Nephron·D W Cockcroft, M H Gault
Dec 1, 1982·American Journal of Clinical Oncology·M M OkenP P Carbone
Dec 26, 2001·Antimicrobial Agents and Chemotherapy·Er-jia WangWilliam W Johnson
Jul 16, 2002·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Diederik F S KehrerAlex Sparreboom
Apr 30, 2004·Clinical Pharmacology and Therapeutics·Frederike K EngelsAlex Sparreboom
May 3, 2008·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Sanjay GoelSridhar Mani
Jul 23, 2008·Molecular Cancer Therapeutics·Tatiana OkounevaMary Ann Jordan
Mar 10, 2009·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Karl Broich, UNKNOWN Committee for Medicinal Products for Human Use
Apr 8, 2009·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Linda T VahdatJoanne L Blum
Jun 11, 2009·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Antoinette R TanLee S Rosen
Jun 11, 2009·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Sanjay GoelChris H Takimoto
Apr 20, 2010·Expert Opinion on Drug Metabolism & Toxicology·Caroline A LeeDennis A Smith
Aug 4, 2010·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Javier CortesMary Ann Allison
Dec 18, 2010·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Jan-Shiang TaurY Nancy Wong
Mar 8, 2011·Lancet·Javier CortesUNKNOWN EMBRACE (Eisai Metastatic Breast Cancer Study Assessing Physician's Choice Versus E7389) investigators
Apr 5, 2011·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·A C DubbelmanJ H Beijnen
Oct 28, 2011·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·Zahra HanaiziFrancesco Pignatti
Nov 2, 2011·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Anne-Charlotte DubbelmanJos H Beijnen

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Citations

Sep 27, 2012·Cancer Chemotherapy and Pharmacology·L A DevrieseJ H M Schellens
Oct 29, 2013·Women's Health·Helena VerdaguerAnder Urruticoechea
Sep 22, 2015·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Pedro MartinsAlexandra R Fernandes
Aug 12, 2015·Marine Drugs·Umang SwamiSanjay Goel
Apr 23, 2013·British Journal of Clinical Pharmacology·J G Coen van HasseltAlwin D R Huitema
Feb 7, 2017·Expert Opinion on Investigational Drugs·Umang SwamiSanjay Goel
Jun 18, 2017·Expert Review of Anticancer Therapy·Elisabetta SetolaRobin L Jones
Sep 2, 2017·Breast Cancer : the Journal of the Japanese Breast Cancer Society·Masaya HattoriHiroji Iwata
Feb 8, 2018·Future Oncology·Mahesh SeetharamSant P Chawla
Jul 19, 2012·British Journal of Clinical Pharmacology·Lot A DevrieseJan H M Schellens
Mar 20, 2021·Breast Cancer Research : BCR·Iain R MacphersonCarlo Palmieri

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