Based on the hypothesis that the selectivity of the antitumor action of a drug is dependent on a multiplicity of systemic and target cell factors, the role of pharmacokinetics and biotransformation in determining drug bioavailability and the target cell determinants of the action of arabinosylcytosine and of methotrexate are briefly discussed. The modulation of the action of an antimetabolite by a modification of the bioavailability of certain metabolites is mentioned as an approach towards the development of more selective chemotherapy.
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