Summary
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.
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Weenen, H., Lankelma, J., Penders, P.G.M. et al. Pharmacokinetics of 4′-epi-doxorubicin in man. Invest New Drugs 1, 59–64 (1983). https://doi.org/10.1007/BF00180192
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DOI: https://doi.org/10.1007/BF00180192