Current Prodrug Design for Drug Discovery

Author(s): Pei-Wen Hsieh, Chi-Feng Hung, Jia-You Fang

Journal Name: Current Pharmaceutical Design

Volume 15 , Issue 19 , 2009

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Prodrugs are inactive compounds which are metabolized either chemically or enzymatically in a controlled or predictable manner to the parent active drug inside the body. Prodrugs can enhance the therapeutic efficacy and/or reduce adverse effects via different mechanisms, including increased solubility, improved permeability and bioavailability, prolonged half-life, and tissue-targeted delivery. Besides the prodrug itself, optimization of vehicles and other enhancement techniques is important as well. Strategies to improve the oral bioavailability and achieve tumor-specific targeting have been the most important developments in prodrug design during the last 5 years. This review describes recent developments in orally administered and tumor-targeted prodrugs. Pharmacokinetic and pharmacodynamic evaluations of these prodrugs are systematically introduced in this review.

Keywords: Prodrug, oral administration, anticancer drug, pharmacokinetics, pharmacodynamics

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Article Details

Year: 2009
Page: [2236 - 2250]
Pages: 15
DOI: 10.2174/138161209788682523
Price: $65

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