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Abstract
Active drug efflux transporters of the ATP binding cassette (ABC)-containing family
of proteins have a major impact on the pharmacological behavior of most of the drugs
in use today. Pharmacological properties affected by ABC transporters include the
oral bioavailability, hepatobiliary, direct intestinal, and urinary excretion of drugs
and drug-metabolites and -conjugates. Moreover, the penetration of drugs into a range
of important pharmacological sanctuaries, such as brain, testis, and fetus, and the
penetration into specific cell- and tissue compartments can be extensively limited
by ABC transporters. These interactions with ABC transporters determine to a large
extent the clinical usefulness, side effects and toxicity risks of drugs. Many other
xenotoxins, (pre-)carcinogens and endogenous compounds are also influenced by the
ABC transporters, with corresponding consequences for the well-being of the individual.
We aim to provide an overview of properties of the mammalian ABC transporters known
to mediate significant transport of clinically relevant drugs.