Stereoselectivity of iododoxorubicin reduction in various animal species and humans

M. Strolin Benedetti, D. Fraier, E. Pianezzola, M. G. Castelli, P. Dostert, L. Gianni

Research output: Contribution to journalArticlepeer-review

Abstract

1. The excretion of iododoxorubicin in urine as the 13-dihydro derivative, iododoxo-rubicinol, is much greater in man than in rat, dog, rabbit and monkey. Iododoxorubicinol epimers in urine from man and the animal species after i.v. administration of iododoxorubicin, were quantified by h.p.l.c. 2. (13R)-Iododoxorubicinol was not detectable in rat, dog and human urine and accounted for no more than 0.15% dose in urine of 1/3 rabbits and 3/3 monkeys. (13S)-Iododoxorubicinol in human urine amounted to 5.6% dose, whereas in rat only 0.01% dose and in monkey only 0.91% dose was found. 3. As for idarubicin, the in vivo reduction of iododoxorubicin is highly stereoselective, giving the (13S)-epimer almost exclusively. Erythrocyte ketone reductases may account for the higher formation of (13S)-iododoxorubicinol in man.

Original languageEnglish
Pages (from-to)115-121
Number of pages7
JournalXenobiotica
Volume23
Issue number2
DOIs
Publication statusPublished - 1993

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology
  • Biochemistry
  • Health, Toxicology and Mutagenesis
  • Biochemistry, Genetics and Molecular Biology(all)

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