Pharmacokinetics of 4′-epi-doxorubicin in man

H. Weenen, J. Lankelma, P. G M Penders, J. G. McVie, W. W. Ten Bokkel Huinink, M. M. de Planque, H. M. Pinedo

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Abstract

The pharmacokinetics of 4′-epi-doxorubicin (4′-epi-adriamycin, 4′-epi-DX) in man can be described by a three-compartment model with a rapid distribution phase and a very long elimination phase. Urine excretion amounts to a total of about 11% of the administered dose during 48 h after drug administration, and less than 1% during the following 48 h. In plasma 4′-epi-doxorubicin is rapidly converted to five metabolites (4′-epi-doxorubicinol, aglycones and glucuronides), the concentration of the aglycones sometimes exceeding that of 4′-epi-DX. In urine only three metabolites were found in addition to the parent drug; they were identified as 4′-epi-doxorubicinol (EOH), 4′-epi-doxorubicin-glucuronide (E-Glu) and 4′-epi-doxorubicinol-glucuronide (EOH-Glu). Comparison of the pharmacokinetics and metabolic profiles of 4′-epi-DX and doxorubicin (DX) in man revealed that 4′-epi-DX eliminates faster than DX.

Original languageEnglish (US)
Pages (from-to)59-64
Number of pages6
JournalInvestigational New Drugs
Volume1
Issue number1
DOIs
StatePublished - Mar 1983
Externally publishedYes

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Keywords

  • 4′-epi-doxorubicin
  • anthracyclines
  • metabolism in man
  • pharmacokinetics in man

ASJC Scopus subject areas

  • Pharmacology
  • Molecular Medicine

Cite this

Weenen, H., Lankelma, J., Penders, P. G. M., McVie, J. G., Ten Bokkel Huinink, W. W., de Planque, M. M., & Pinedo, H. M. (1983). Pharmacokinetics of 4′-epi-doxorubicin in man. Investigational New Drugs, 1(1), 59-64. https://doi.org/10.1007/BF00180192