PMID: 3770056Aug 1, 1986Paper

Marked inter-patient variation in adriamycin biotransformation to 7-deoxyaglycones: evidence from metabolites identified in serum

European Journal of Cancer & Clinical Oncology
J CummingsS B Kaye

Abstract

Several factors are known to modulate the clinical pharmacokinetics of adriamycin (ADR). Biotransformation has not been studied in this context because of problems identifying serum metabolites. We have studied patterns of ADR biotransformation in 25 patients with normal liver and kidney function and in most cases receiving ADR for the first time. Three major serum metabolites were identified by HPLC, TLC and mass spectrometry and their pharmacokinetics were followed over a 24-hr period. The relative amount of each metabolite present in a patient was quantitated by calculating its AUC. Adriamycinol was the major metabolite detected in the majority of patients. Adriamycin 7-deoxyaglycone was detected in the serum of 15 patients where it accounted for a small percentage of the total ADR concentration (1-5%). Its apparent half-life was normally less than 30 min. Adriamycinol 7-deoxyaglycone was detected in the serum of only 13 patients where it accounted for a greater percentage of the total ADR concentration (10-20%). Its pharmacokinetics exhibited marked inter-patient variations, with apparent half-lives ranging from 0.1 to 24 hr. There was a correlation between the AUC of ADR and the relative amount of metabolites present in ea...Continue Reading

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Citations

Jan 1, 1987·Cancer Chemotherapy and Pharmacology·J CummingsS B Kaye
Jan 1, 1993·Cancer Chemotherapy and Pharmacology·K MrossD K Hossfeld
Feb 24, 2005·Cancer Chemotherapy and Pharmacology·M JoergerJ H Beijnen
Dec 1, 1994·The International Journal of Biochemistry·P M Sokolove
Jan 1, 1987·Pharmacology & Therapeutics·G Powis
Oct 4, 2002·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·David L ChinBranimir I Sikic
May 1, 1995·Postgraduate Medical Journal·L Samuel
Jan 1, 1990·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·K MrossD Hossfeld
May 1, 1995·Postgraduate Medical Journal·D C O'SullivanM R Heal
May 1, 1995·Postgraduate Medical Journal·C VidalA Gonzalez-Quintela
Mar 1, 1988·Biochemical Pharmacology·P M Sokolove, R G Shinaberry
Feb 1, 1991·Archives of Biochemistry and Biophysics·P M Sokolove

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