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Chemical Compound Review

Idarubicinol     (9R)-7-[(2S,4S,5S,6S)-4- amino-5-hydroxy-6...

Synonyms: SureCN1649690, KST-1A8934, LS-93995, AR-1A4477, AC1L32W8, ...
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Disease relevance of NSC 256439


High impact information on NSC 256439


Biological context of NSC 256439


Anatomical context of NSC 256439


Associations of NSC 256439 with other chemical compounds


Gene context of NSC 256439

  • IDA is converted in the liver into idarubicinol (2HIDA) and, in this form, seems to exert its antitumoral activity in vivo [21].
  • A specific, sensitive, and reliable high-performance liquid chromatographic (HPLC) method for the determination of idarubicin (IDA) and its known fluorescent metabolites idarubicinol (IDAol) and 4-demethoxy-daunomycinone (AG1) in biological fluids (human plasma and urine) was developed and tested [22].

Analytical, diagnostic and therapeutic context of NSC 256439


  1. Pharmacokinetics of oral idarubicin in breast cancer patients with reference to antitumor activity and side effects. Elbaek, K., Ebbehøj, E., Jakobsen, A., Juul, P., Rasmussen, S.N., Bastholt, L., Dalmark, M., Steiness, E. Clin. Pharmacol. Ther. (1989) [Pubmed]
  2. Toxicity of idarubicin and doxorubicin towards normal and leukemic human bone marrow progenitors in relation to their proliferative state. Minderman, H., Linssen, P., van der Lely, N., Wessels, J., Boezeman, J., de Witte, T., Haanen, C. Leukemia (1994) [Pubmed]
  3. Bioavailability and pharmacology of oral idarubicin. Stewart, D.J., Grewaal, D., Green, R.M., Verma, S., Maroun, J.A., Redmond, D., Robillard, L., Gupta, S. Cancer Chemother. Pharmacol. (1991) [Pubmed]
  4. Anthracyclines and their C-13 alcohol metabolites: growth inhibition and DNA damage following incubation with human tumor cells in culture. Kuffel, M.J., Reid, J.M., Ames, M.M. Cancer Chemother. Pharmacol. (1992) [Pubmed]
  5. In vitro effect of multidrug resistance modifiers on idarubicinol efflux in blasts of acute myeloid leukemia. Schröder, J.K., Kasimir-Bauer, S., Seeber, S., Scheulen, M.E. J. Cancer Res. Clin. Oncol. (2000) [Pubmed]
  6. Dose-finding and pharmacologic study of chronic oral idarubicin therapy in metastatic breast cancer patients. Toffoli, G., Sorio, R., Aita, P., Crivellari, D., Corona, G., Bearz, A., Robieux, I., Colussi, A.M., Stocco, F., Boiocchi, M. Clin. Cancer Res. (2000) [Pubmed]
  7. Oral idarubicin pharmacokinetics--correlation of trough level with idarubicin area under curve. Schleyer, E., Kühn, S., Rührs, H., Unterhalt, M., Kaufmann, C.C., Kern, W., Braess, J., Sträubel, G., Hiddemann, W. Leukemia (1997) [Pubmed]
  8. Cellular pharmacology of idarubicinol in multidrug-resistant LoVo cell lines. Toffoli, G., Corona, G., Simone, F., Gigante, M., De Angeli, S., Boiocchi, M. Int. J. Cancer (1996) [Pubmed]
  9. Formation and longevity of idarubicin-induced DNA topoisomerase II cleavable complexes in K562 human leukaemia cells. Willmore, E., Errington, F., Tilby, M.J., Austin, C.A. Biochem. Pharmacol. (2002) [Pubmed]
  10. Phase I trial of 4-demethoxydaunorubicin (idarubicin) with single oral doses. Kaplan, S., Sessa, C., Willems, Y., Pacciarini, M.A., Tamassia, V., Cavalli, F. Investigational new drugs. (1984) [Pubmed]
  11. Pharmacokinetics and tissue distribution of idarubicin-loaded solid lipid nanoparticles after duodenal administration to rats. Zara, G.P., Bargoni, A., Cavalli, R., Fundarò, A., Vighetto, D., Gasco, M.R. Journal of pharmaceutical sciences. (2002) [Pubmed]
  12. Only association of low concentrations of idarubicin plus idarubicinol induced apoptosis on leukaemic cells. Musso, M., Porretto, F., Crescimanno, A., Bondi, F., Polizzi, V., Scalone, R., Tolomeo, M., Mariani, G. Leuk. Res. (1998) [Pubmed]
  13. A phase I study of idarubicin hydrochloride in patients with acute leukemia. The Idarubicin Study Group of Japan. Tamura, K. Semin. Hematol. (1996) [Pubmed]
  14. Idarubicin-related side effects in recipients of T-cell-depleted allogeneic bone marrow transplants are schedule dependent. Muus, P., Donnelly, P., Schattenberg, A., Linssen, P., Minderman, H., Dompeling, E., de Witte, T. Semin. Oncol. (1993) [Pubmed]
  15. Idarubicinol myelotoxicity: a comparison of in vitro data with clinical outcome in patients treated with high-dose idarubicin. Corsini, C., Ghielmini, M., Mancuso, P., Tealdo, F., Paolucci, M., Zucchetti, M., Ferrucci, P.F., Cocorocchio, E., Mezzetti, M., Mori, A., Riggi, M., D'Incalci, M., Martinelli, G. Br. J. Cancer (2000) [Pubmed]
  16. Comparison of idarubicin and daunorubicin and their main metabolites regarding intracellular uptake and effect on sensitive and multidrug-resistant HL60 cells. Tidefelt, U., Prenkert, M., Paul, C. Cancer Chemother. Pharmacol. (1996) [Pubmed]
  17. An efficient method for culturing human breast carcinoma to evaluate antiblastic drug activity in vitro: experience on 136 primary cancers and on 116 recurrences. Zoli, W., Volpi, A., Bonaguri, C., Riccobon, A., Savini, S., Brizio, R., Saragoni, A., Medri, L., Marra, G.A., Amadori, D. Breast Cancer Res. Treat. (1991) [Pubmed]
  18. Cytotoxicity of anthracyclines: correlation with cellular uptake, intracellular distribution and DNA binding. Gieseler, F., Biersack, H., Brieden, T., Manderscheid, J., Nüssler, V. Ann. Hematol. (1994) [Pubmed]
  19. Effects of idarubicin and idarubicinol on rat coronary resistance and vasoconstrictor responsiveness of isolated aorta and mesentery. Weiss, M., Giessler, C., Kang, W. Anticancer Drugs (2006) [Pubmed]
  20. Idarubicin overcomes P-glycoprotein-related multidrug resistance: comparison with doxorubicin and daunorubicin in human multiple myeloma cell lines. Roovers, D.J., van Vliet, M., Bloem, A.C., Lokhorst, H.M. Leuk. Res. (1999) [Pubmed]
  21. Comparative activity of idarubicin and idarubicinol in combination with cyclosporin A in multidrug-resistant leukemia cells. Tolomeo, M., Gancitano, R.A., Musso, M., Porretto, F., Perricone, R., Abbadessa, V., Cajozzo, A. Cancer Chemother. Pharmacol. (1996) [Pubmed]
  22. High-performance liquid chromatographic analysis of idarubicin and fluorescent metabolites in biological fluids. Camaggi, C.M., Carisi, P., Strocchi, E., Pannuti, F. Cancer Chemother. Pharmacol. (1992) [Pubmed]
  23. Idarubicin (4-demethoxydaunorubicin). A preliminary overview of preclinical and clinical studies. Ganzina, F., Pacciarini, M.A., Di Pietro, N. Investigational new drugs. (1986) [Pubmed]
  24. Hepatobiliary metabolism and urinary excretion of 4-demethoxydaunorubicin as compared to daunorubicin in rats. Catapano, C.V., Guaitani, A., Broggini, M., Corada, M., Bartosek, I., Italia, C., Donelli, M.G. Anticancer Res. (1988) [Pubmed]
  25. Determination of idarubicin and idarubicinol in plasma by capillary electrophoresis. Hempel, G., Haberland, S., Schulze-Westhoff, P., Möhling, N., Blaschke, G., Boos, J. J. Chromatogr. B Biomed. Sci. Appl. (1997) [Pubmed]
  26. Comparison of the interaction of doxorubicin, daunorubicin, idarubicin and idarubicinol with large unilamellar vesicles. Circular dichroism study. Gallois, L., Fiallo, M., Garnier-Suillerot, A. Biochim. Biophys. Acta (1998) [Pubmed]
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