Pharmacokinetics and metabolism in early drug discovery.
The need for high-throughput approaches in absorption, distribution, metabolism and excretion studies is driven by the impact of high-speed chemistry and pharmacological screening. Perhaps an even greater impact is that these studies will, in the future, provide large data sets that can be used to predict biological events related to absorption, bioavailability and metabolism of drugs. Through linking of in silico and in vitro methods, considerable progress has recently been made towards this future perspective. Despite this progress, these approaches do not yet replace in vivo methods.
Smith
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Pfizer Central Research, Department of Drug Metabolism, Sandwich, Kent, CT13 9NJ, UK. dennis_a_smith@sandwich.pfizer.com
van de Waterbeemd
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D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D051544:Cytochrome P-450 CYP3A; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D015195:Drug Design; D006899:Mixed Function Oxygenases / Q000378:metabolism; D010599:Pharmacokinetics; D014018:Tissue Distribution; D014116:Toxicology
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D003577:Cytochrome P-450 Enzyme System; D006899:Mixed Function Oxygenases; C104464:CYP3A protein, human; D051544:Cytochrome P-450 CYP3A