Biological Dispersion and the Design of Site-Specific Protein Therapeutic Systems

  • E. Tomlinson
Part of the NATO ASI Series book series (NSSA, volume 199)


A drug acts when it reaches its pharmacological site of action. However, ideal clinical effectiveness relies additionally on the right amount of drug reaching its site(s) of action at the right rate and frequency, on (often) a drug-free interval (at the receptor site), and on not critically interacting with non-target sites. Few drugs in use today attain such ideality. As more attention is paid to drug/receptor interactions, (often through the use of molecular modelling procedures and/or the use of cloned endogenous proteins which can act as templates for the designed fit of agonist or antagonist drugs), increased effort is being focussed on controlling the biological dispersion of drugs. This activity, which was once reserved almost exclusively for cytotoxic drugs, is an increasingly important aspect of the discovery and drug development process, particularly in the design of therapeutic proteins. Approaches to site-specific delivery include simple low molecular weight prodrugs activated at sites of disease, suicide enzyme substrate inhibitors; polymeric soluble and particulate macromolecular carriers; and unique site-specific therapeutic proteins.


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Copyright information

© Plenum Press, New York 1990

Authors and Affiliations

  • E. Tomlinson
    • 1
  1. 1.Advanced Drug Delivery ResearchCiba-Geigy PharmaceuticalsHorsham, West SussexUK

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