Journal
EXPERT OPINION ON DRUG DISCOVERY
Volume 2, Issue 1, Pages 51-64Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1517/17460441.2.1.51
Keywords
alpha(1)-acid glycoprotein; albumin; brain:plasma ratio; equilibrium dialysis; Free Drug Principle; free fraction; microdialysis; plasma protein binding; shift assay; unbound fraction
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Plasma protein binding of drugs is a well-recognised phenomena, but it is only recently that the implications for drug action in vivo have been fully appreciated. Plasma proteins, by virtue of their high concentration, control the free drug concentration in plasma and in compartments in equilibrium with plasma, thereby, effectively attenuating drug potency in vivo. The historical background and thermodynamic basis for the 'Free Drug Principle' is presented, along with special considerations for intracellular targets, deep compartments and alpha(1)-acid glycoprotein binding. Real and apparent exceptions to the principle are discussed along with a survey of citations from the recent medicinal chemistry literature.
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