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Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System
Published on: December 11, 2016
Prodrugs: design and clinical applications
Jarkko Rautio1, Hanna Kumpulainen, Tycho Heimbach
1Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, FI-70211 Kuopio, Finland. jarkko.rautio@uku.fi
Nature Reviews. Drug Discovery
|January 26, 2008
Summary
Prodrugs are modified drug molecules that become active after the body transforms them. This strategy enhances drug properties and is increasingly used in drug discovery and development.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Drug Discovery
Background:
- Prodrugs are bioreversible drug derivatives.
- They transform in vivo to release active parent drugs.
- Prodrugs improve drug physicochemical, biopharmaceutical, and pharmacokinetic properties.
Purpose of the Study:
- To highlight the utility of the prodrug strategy in drug discovery and development.
- To describe common functional groups used in prodrug design.
- To showcase examples of prodrugs in clinical use or trials.
Main Methods:
- Review of prodrugs and their design principles.
- Identification of common functional groups amenable to prodrug modification.
- Compilation of examples of approved or investigational prodrugs.
Main Results:
- Prodrugs are established tools in drug discovery and development.
- Approximately 5-7% of approved drugs are prodrugs.
- A growing trend shows increased implementation of prodrugs early in drug discovery.
Conclusions:
- The prodrug approach is a valuable strategy for optimizing drug properties.
- Various functional groups can be modified to create effective prodrugs.
- Numerous prodrugs are successfully utilized in medicine or are in development.
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