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Criteria for Selection of New Analogs of Antitumor Antibiotics

  • A. Goldin
Part of the Recent Results in Cancer Research / Fortschritte der Krebsforschung / Progrès dans les recherches sur le cancer book series (RECENTCANCER, volume 63)

Abstract

A highly difficult area in the application of preclinical methodology involves the selection and development of new analogs of known antitumor agents for clinical trial. There are a considerable number of analogs of alkylating agents, purine and pyrimidine antagonists, folic acid antagonists, dimethane sulfonates, benzimidazols, antibiotics of a number of subcategories, and other classes of drugs which have demonstrable activity in antitumor test models but which have remained “dormant” with respect to development, pending any experimental observations that would provide a basis for further interest. The problems involved in the selection of new analogs of antitumor antibiotics are not dissimilar from those involved in the selection of new analogs in general. It is important to examine the preclinical criteria that may be employed in an attempt to identify analogs of antitumor antibiotics that are worthy of further development for the clinic. In general, standard preclinical testing methodologies may be employed to provide data as a guide for selection. Overall, if a new analog of a known antitumor antibiotic is to justify interest, the analog must be demonstrated to possess either quantitative or qualitative superiority over the parent compound in pharmacologic, toxicologic, immunologic, tumor cytotoxic, or other biologic properties that are therapeutically favourable. In such a determination, it is important to focus specific attention on the characteristics that are limiting for the parent antitumor antibiotic in clinical use. Various preclinical criteria for selection of new antitumor antibiotics for clinical use will be discussed below.

Keywords

Lewis Lung Carcinoma Cytosine Arabinoside Antitumor Antibiotic Anthracycline Derivative Arabinosyl Cytosine 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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© Springer-Verlag Berlin · Heidelberg 1978

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  • A. Goldin

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