Prodrugs and Targeted Delivery

Preface
 
PART ONE: Prodrug Design and Intellectual Property
 
PRODRUG STRATEGIES IN DRUG DESIGN
Prodrug Concept
Basics of Prodrug Design
Rationale for Prodrug Design
History of Prodrug Design
Recently Marketed Prodrugs
Concluding Remarks
 
THE MOLECULAR DESIGN OF PRODRUGS BY FUNCTIONAL GROUP
Introduction
The Prodrug Concept and Basics of Design
Common Functional Group Approaches in Prodrug Design
Conclusions
 
INTELLECTUAL PROPERTY PRIMER ON PHRAMACEUTICAL PATENTS WITH A SPECIAL EMPHASIS ON PRODRUGS AND METABOLITES
Introduction
Patents and FDA Approval Process
Obtaining a Patent
Conclusion
 
PART TWO: Prodrugs Addressing ADMET Issues
 
INCREADING LIPOPHILICITY FOR ORAL DRUG DELIVERY
Introduction
pKa, Degree of Ionization, Partition Coefficient, and Distribution Coefficient
Prodrug Strategies to Enhance Lipid Solubility
Prodrug Examples for Antibiotics
Antiviral Related Prodrugs
Cardiovascular Related Prodrugs
Lipophilic Prodrugs of Benzamidine Drugs
Miscellaneous Examples
Summary and Conclusion
 
MODULATING SOLUBILITY THROUGH PRODRUGS FOR ORAL AND IV DRUG DELIVERY
Introduction
Basics of Solubility and Oral/IV Drug Delivery
Prodrug Applications for Enhanced Aqueous Solubility
Challenges with Solubilizing Prodrugs of Insoluble Drugs
Additional Applications of Prodrugs for Modulating Solubility
Parallel Exploration of Analogues and Prodrugs in Drug Discovery (Commentary)
Conclusions
 
PRODRUGS DESIGNED TO TARGET TRANSPORTERS FOR ORAL DRUG DELIVERY
Introduction
Serendipity: An Actively Transported Prodrug
Requirements for Actively Transported Prodrugs
Peptide Transporters: PEPT1 and PEPT2
Monocarboxylate Transporters
Bile Acid Transporters
Conclusions
 
TOPICAL AND TRANSDERMAL DELIVERY USING PRODRUGS: MECHANISM OF ENHANCEMENT
Introduction
Arrangement of Water in the Stratum Corneum
A New Model for Diffusion Through the Stratum Corneum: The Biphasic Solubility

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.

"The book captures all the important aspects of prodrugs. It is well organized in that each chapter presents a specific topic with very little duplication of contents between chapters ... Given the fact that prodrugs are now increasingly integrated into early drug discovery, this type of book would be a valuable addition to the library of any drug discovery institution." (Journal of Medicinal Chemistry, 8 August 2011) "Every company employing medicinal chemists will be interested in this practice-oriented overview of a key strategy in modern drug discovery and development." (Pharmiweb, 16 February 2011)

"The book captures all the important aspects of prodrugs. It is well organized in that each chapter presents a specific topic with very little duplication of contents between chapters . . . Given the fact that prodrugs are now increasingly integrated into early drug discovery, this type of book would be a valuable addition to the library of any drug discovery institution." (Journal of Medicinal Chemistry, 8 August 2011)
"Every company employing medicinal chemists will be interested in this practice-oriented overview of a key strategy in modern drug discovery and development." (Pharmiweb, 16 February 2011)