Prodrugs and Targeted Delivery Towards Better ADME Properties

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Edition: 1st
Format: Hardcover
Pub. Date: 2011-01-31
Publisher(s): Wiley-VCH
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Summary

This topical reference and handbook addresses the chemistry, pharmacology, toxicology and the patentability of prodrugs, perfectly mirroring the integrated approach prevalent in today's drug design. It summarizes current experiences and strategies for the rational design of prodrugs, beginning at the early stages of the development process, as well as discussing organ- and site-selective prodrugs. Every company employing medicinal chemists will be interested in this practice-oriented overview of a key strategy in modern drug discovery and development.

Author Biography

Jarkko Rautio is professor of pharmaceutical chemistry and head of the multidisciplinary Pharmaceutical and Medicinal Chemistry (PMC) research group at the School of Pharmacy, University of Eastern Finland (formerly University of Kuopio), where he received his PhD in pharmaceutical chemistry in 2000. He subsequently carried out his postdoctoral studies at the University of Maryland, Baltimore, USA, and was a visiting scientist at GlaxoSmithKline, North Carolina, while also co-founding the American Association of Pharmaceutical Scientists (AAPS) Prodrug Focus Group in 2005. Professor Rautio's research focuses on chemistry-based methods, especially prodrugs, to overcome the liabilities of drugs.

Table of Contents

Prodrug Design and Intellectual Property
Prodrug strategies in drug design
The molecular design of prodrugs by functional group
Increasing lipophilicity for oral drug delivery
Prodrugs Addressing Admet Issues
Modulating solubility through prodrugs for oral and IV drug delivery
Topical and transdermal delivery using prodrugs: mechanism of enhancement
Ocular delivery using prodrugs
Prodrugs designed to target transporters for oral drug delivery
Enzyme-activated prodrug strategies for site-selective drug delivery
Reducing Pre-systemic Drug Metabolism
Codrugs and Soft Drugs
Prodrug approaches for central nervous system delivery
Soft drugs
Improving the use of drug combinations through the codrug approach
The impact of pharmacogenetics on the clinical outcomes of prodrugs
Preclinical and Clinical Consideration for Prodrugs
Intellectual Property Primer on Pharmaceutical Patents with a Special Emphasis on Prodrugs and Metabolites
Pharmacokinetic and biopharmaceutical considerations in prodrug discovery and development
Directed enzyme prodrug therapies
Table of Contents provided by Publisher. All Rights Reserved.

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