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Metabolism of Cancer Chemotherapeutic Agents via Pathways Utilized by Xenobiotics

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Antineoplastic and Immunosuppressive Agents Part I

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Abstract

The main factors which affect the duration and intensity of drug action are absorption, distribution, excretion, and metabolism; in this chapter attention will be focused on one important factor, the metabolism of antineoplastic agents. The metabolism of a drug can lead to an increase, a decrease, or no change in the pharmacologic or toxicologic activity of that drug. The catabolic reactions which are usually directed toward enhancing the elimination of a drug are emphasized in this and the preceding chapter. The anabolic processes by which conversion of drugs to more complex forms, and, in some cases, incorporation into body constituents occurs, have been discussed (Johns, Chapt. 14, this volume). In the latter case assimilation can occur only when the enzymes involved in intermediary anabolism cannot distinguish the antineoplastic compound from endogenous substrates because of a close resemblance in structural and/or physicochemical properties. Such a substitution of a drug for a natural metabolite is defined by the term “parametabolite” where substitution in a morphological, as well as a functional sense can occur. When the drug substitutes for the natural metabolite only in a morphological sense, with a resultant blockage in the normal biochemical process, the drug is called an antimetabolite.

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Authors
  1. A. M. Guarino
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  2. C. L. Litterst
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Editors and Affiliations

  1. Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut, 06510, USA

    Alan C. Sartorelli (Professor) (Professor)

  2. Laboratory of Chemical Pharmacology, National Cancer Institute, National Istitutes of Health, Bethesda, Maryland, 20014, USA

    David G. Johns M. D.

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Guarino, A.M., Litterst, C.L. (1974). Metabolism of Cancer Chemotherapeutic Agents via Pathways Utilized by Xenobiotics. In: Sartorelli, A.C., Johns, D.G. (eds) Antineoplastic and Immunosuppressive Agents Part I. Handbuch der experimentellen Pharmakologie / Handbook of Experimental Pharmacology, vol 38 / 1. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-65678-1_15

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