Membrane Transport of Antifolates as a Critical Determinant of Drug Cytotoxicity

  • I. David Goldman
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 84)


There are few areas in therapeutics in which membrane transport of pharmacologic agents has been subjected to as intense study as in the treatment of malignant diseases with cytotoxic agents. Unlike the antibacterial or antifungal agents, which may selectively inhibit biochemical processes unique to the bacterial or fungal organism, the agents which comprise the current armamentarium of the cancer chemotherapist produce toxic effects on both tumor and susceptible host tissues. The lack of understanding of the basic biochemical differences between normal and malignant cells require the utilization of subtle techniques, often empirical, to achieve “selective” effects of the agents in an attempt to minimize toxicity to susceptible host tissues while maximizing toxicity to the tumor. The better understood of these techniques usually exploit quantitative rather than qualitative differences in the tumor vs. host cell rates of (a) cellular proliferation, (b) drug activation or inactivation, (c) drug transport across the cell membrane, and (d) drug interaction with target sites within the cell.


Membrane Transport Free Drug Organic Phosphate Ehrlich Ascites Tumor Cell Intracellular Drug 
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Copyright information

© Plenum Press, New York 1977

Authors and Affiliations

  • I. David Goldman
    • 1
  1. 1.Department of MedicineMedical College of VirginiaRichmondUSA

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