Theoretical Predictions of Drug Absorption in Drug Discovery and Development
作者:
Patric Stenberg,
Christel A.S. Bergström,
Kristina Luthman,
Per Artursson,
期刊:
Clinical Pharmacokinetics
(ADIS Available online 2002)
卷期:
Volume 41,
issue 11
页码: 877-899
ISSN:0312-5963
年代: 2002
出版商: ADIS
关键词: Clinical pharmacokinetics;Research and development
数据来源: ADIS
摘要:
The clinical development of new drugs is often terminated because of unfavourable pharmacokinetic properties such as poor intestinal absorption after oral administration. Intestinal permeability and solubility are two of the most important factors that determine the absorption properties of a compound. Efficient and reliable computational models that predict these properties as early as possible in drug discovery and development are therefore desirable.In this review, we first discuss the implementation of predictive models of intestinal drug permeability and solubility in drug discovery and development. Secondly, we discuss the mechanisms of intestinal drug permeability and computational methods that can be used to predict it. We then discuss factors influencing drug solubility and models for predicting it. We finally speculate that once these and other predictive computational models are implemented in drug discovery and development, these processes will become much more effective. Further, an increased fraction of drug candidates that are less likely to fail during clinical development will be selected.
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