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1.4 Concluding Remarks

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Transporter‐mediated drug uptake and efflux are clear determinants of intracellular concentrations of drugs and metabolites which are substrates of the transporters. Individual variations in the expression of drug metabolism enzymes and transporters due to genetic polymorphism, exposure to drugs, foods and food supplements, and various diseases have been well‐established. A thorough understanding of the role of drug metabolism and transport in the disposition of a potentially toxic drug will aid the assessment of its toxic potential and the identification of the critical determinants of events leading to the formation and accumulation of the toxic moiety. Routine evaluation of the toxicological consequence of drug metabolism and transport may therefore aid the development of drugs with lower potential of causing idiosyncratic toxicity and may eventually lead to the identification of at‐risk populations.

Transporters and Drug-Metabolizing Enzymes in Drug Toxicity

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