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Pharmacokinetics of Anthracyclines in Dogs: Evidence for Structure-Related Body Distribution and Reduction to Their Hydroxy Metabolites

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Abstract

The pharmacokinetic disposition of the anthracyclines, adriamycin (doxorubicin), daunorubicin, 4′-epi-adriamycin, carminomycin, and 4-demethoxy-daunorubicin, and the formation of their reduced C13 hydroxy metabolites were studied in dogs. The presence of a C14hydroxy group (adriamycin and 4′epi-adriamycin) drastically reduces the appearance of the C13 hydroxy metabolites in plasma. Substitution of the C4-H with C4-OH and C4-OCH3, in this rank order, decreases the area under the plasma concentration-time curves of the parent compounds and their C13 hydroxy metabolites.

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Oosterbaan, M.J.M., Dirks, R.J.M., Vree, T.B. et al. Pharmacokinetics of Anthracyclines in Dogs: Evidence for Structure-Related Body Distribution and Reduction to Their Hydroxy Metabolites. Pharm Res 1, 33–38 (1984). https://doi.org/10.1023/A:1016378609450

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