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Updated: Jun 21, 2026

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System
Published on: December 11, 2016
Current prodrug design for drug discovery
Pei-Wen Hsieh1, Chi-Feng Hung, Jia-You Fang
1Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan.
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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