Abstract
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
Current Pharmaceutical Design
Title: Current Prodrug Design for Drug Discovery
Volume: 15 Issue: 19
Author(s): Pei-Wen Hsieh, Chi-Feng Hung and Jia-You Fang
Affiliation:
Keywords: Prodrug, oral administration, anticancer drug, pharmacokinetics, pharmacodynamics
Abstract: 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.
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Cite this article as:
Hsieh Pei-Wen, Hung Chi-Feng and Fang Jia-You, Current Prodrug Design for Drug Discovery, Current Pharmaceutical Design 2009; 15 (19) . https://dx.doi.org/10.2174/138161209788682523
DOI https://dx.doi.org/10.2174/138161209788682523 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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