【摘 要】
：
One of the most critical drug evaluation systems is a pre-clinical evaluation for absorption, distribution, metabolism and elimination and toxicity (ADMET), which has been demonstrated to cause approx
【机 构】
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President & CEO, Shanghai Medicilon Inc.China
【出 处】
：
2005 WHTS3rd Annual Congress of International Drug Discovery
论文部分内容阅读
One of the most critical drug evaluation systems is a pre-clinical evaluation for absorption, distribution, metabolism and elimination and toxicity (ADMET), which has been demonstrated to cause approximately over 40% new drug development failure.Pharmacokinetic criteria have to be considered as a clinical strategy to increase the accuracy when making decisions for go/no go.The ability to be administered by the oral route is a highly desirable property for new drugs because it is the safest, most convenient and economic method.Appropriate oral bioavailability is good as long as plasma drug levels can be reached the therapeutic concentrations.This characteristic is indeed a demand in drugs destined for the long-term treatment.Chemical structural criteria for selecting NCE (i.e Lipinski rule of 5) has been proposed and has been applied in drug development, however pharmacokinetic criteria has not been defined.There are several methods for predicting DMPK profiles including OraSpotterTM99, IDEA and GastroPlus.Application of GastroPlus in simulating GI absorption and pharmacokinetics for orally dosed drugs will be discussed.
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