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Screening for human ADME/Tox drug properties in drug discovery

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DRUG DISCOVERY TODAY
卷 6, 期 7, 页码 357-366

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ELSEVIER SCI LTD
DOI: 10.1016/S1359-6446(01)01712-3

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There is no doubt that ADME/Tox drug properties, absorption, distribution, metabolism, elimination and toxicity, are properties crucial to the final clinical success of a drug candidate. It has been estimated that nearly 50% of drugs fail because of unacceptable efficacy, which includes poor bioavailability as a result of ineffective intestinal absorption and undesirable metabolic stability(1). It has also been estimated that up to 40% of drug candidates have failed in the past because of safety issues(2). In this review, the methodologies that are available for use in drug development as in vitro human-based screens for ADME/Tox drug properties are discussed.

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