PMID: 8605275Jan 1, 1996Paper

Reversal effect of itraconazole on adriamycin and etoposide resistance in human leukemia cells

Annals of Hematology
M KurosawaM Asaka

Abstract

Itraconazole is a triazole antifungal agent that inhibits cell membrane serol biosynthesis. Currently, itraconazole is a potent candidate for in vivo use to revert multidrug resistance in acute leukemias, with the added benefit of its antifungal effect. As previously reported, itraconazole, as well as verapamil, reversed adriamycin-resistant K562 cells (K562/ADR) and HL60 cells (HL60/ADR) in dosages compatible to the plasma levels achieved by the therapeutic dosages used for the treatment of fungal infections. By RT-PCR analysis of mdr1, mdr3, and mrp mRNA, these adriamycin-resistant cells showed a higher expression of the transcript of these genes than those of the parent cells. By FACS analysis, both the adriamycin-resistant cells showed a higher expression of P-glycoprotein on their cell surfaces. These results suggested the involvement of itraconazole in the mdr gene and/or mrp gene product-associated resistance. Furthermore, itraconazole partially reversed etoposide resistance in both the K562 and K562/ADR cells. The present study suggests that itraconazole may reverse multidrug resistance, at least in part, via a classical MDR-associated mechanism.

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Citations

Apr 27, 2000·Leukemia Research·T FunatoT Sasaki
Dec 26, 2001·Antimicrobial Agents and Chemotherapy·Er-jia WangWilliam W Johnson
Jul 11, 2001·Pharmacotherapy·C J MathenyG M Pollack
Mar 10, 2000·Clinical Pharmacokinetics·K VenkatakrishnanD J Greenblatt
Aug 3, 2004·Journal of Clinical Pharmacology·Chetan S KaryekarThomas C Dowling
Apr 12, 2003·Pharmacotherapy·Chetan S KaryekarThomas C Dowling
Mar 3, 1998·Blood Reviews·D S Richardson, S A Johnson
Sep 21, 2017·Oncology Letters·Rachel PoundsSean Kehoe
Jan 8, 1998·Therapeutic Drug Monitoring·K M JalavaP J Neuvonen
Aug 10, 2017·Oncology Letters·Hiroshi TsubamotoTakashi Sonoda
Jul 14, 1998·Antimicrobial Agents and Chemotherapy·T MiyamaY Sawada
Jul 3, 2020·Drug Resistance Updates : Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy·Jelena DinićIvanka Tsakovska
Aug 17, 1999·Biochemical and Biophysical Research Communications·A G Abulrob, M Gumbleton
Jun 28, 2013·Journal of Chemical Information and Modeling·Ricardo J FerreiraDaniel J V A dos Santos

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