Prodrugs and Targeted Delivery : Towards Better ADME Properties.

Front Matter -- Prodrug Design and Intellectual Property. Prodrug Strategies in Drug Design / Jarkko Rautio -- The Molecular Design of Prodrugs by Functional Group / Victor R Guarino -- Intellectual Property Primer on Pharmaceutical Patents with a Special Emphasis on Prodrugs and Metabolites / Eyal H Barash -- Prodrugs Addressing ADMET Issues. Increasing Lipophilicity for Oral Drug Delivery / Majid Y Moridani -- Modulating Solubility Through Prodrugs for Oral and IV Drug Delivery / Victor R Guarino -- Prodrugs Designed to Target Transporters for Oral Drug Delivery / Mark S Warren, Jarkko Rautio -- Topical and Transdermal Delivery Using Prodrugs: Mechanism of Enhancement / Kenneth Sloan, Scott C Wasdo, Susruta Majumdar -- Ocular Delivery Using Prodrugs / Deep Kwatra, Ravi Vaishya, Ripal Gaudana, Jwala Jwala, Ashim K Mitra -- Reducing Presystemic Drug Metabolism / Majid Y Moridani -- Enzyme-Activated Prodrug Strategies for Site-Selective Drug Delivery / Krista Laine, Kristiina Huttunen -- Prodrug Approaches for Central Nervous System Delivery / Quentin R Smith, Paul R Lockman -- Directed Enzyme Prodrug Therapies / Dan Niculescu-Duvaz, Gabriel Negoita-Giras, Ion Niculescu-Duvaz, Douglas Hedley, Caroline J Springer -- Codrugs and Soft Drugs. Improving the Use of Drug Combinations Through the Codrug Approach / Peter A Crooks, Harpreet K Dhooper, Ujjwal Chakraborty -- Soft Drugs / Paul W Erhardt, Michael D Reese -- Preclinical and Clinical Consideration for Prodrugs. Pharmacokinetic and Biopharmaceutical Considerations in Prodrug Discovery and Development / John P O'Donnell -- The Impact of Pharmacogenetics on the Clinical Outcomes of Prodrugs / Jane P F Bai, Mike Pacanowski, Atiqur Rahman, Lawrence L Lesko -- Index.

Prodrugs and Targeted Delivery: Towards Better ADME Properties; Contents; List of Contributors; Preface; A Personal Foreword; Part One: Prodrug Design and Intellectual Property; 1 Prodrug Strategies in Drug Design; 2 The Molecular Design of Prodrugs by Functional Group; 3 Intellectual Property Primer on Pharmaceutical Patents with a Special Emphasis on Prodrugs and Metabolites; Part Two: Prodrugs Addressing ADMET Issues; 4 Increasing Lipophilicity for Oral Drug Delivery; 5 Modulating Solubility Through Prodrugs for Oral and IV Drug Delivery.

6 Prodrugs Designed to Target Transporters for Oral Drug Delivery7 Topical and Transdermal Delivery Using Prodrugs: Mechanism of Enhancement; 8 Ocular Delivery Using Prodrugs; 9 Reducing Presystemic Drug Metabolism; 10 Enzyme-Activated Prodrug Strategies for Site-Selective Drug Delivery; 11 Prodrug Approaches for Central Nervous System Delivery; 12 Directed Enzyme Prodrug Therapies; Part Three: Codrugs and Soft Drugs; 13 Improving the Use of Drug Combinations Through the Codrug Approach; 14 Soft Drugs; Part Four: Preclinical and Clinical Consideration for Prodrugs.

15 Pharmacokinetic and Biopharmaceutical Considerations in Prodrug Discovery and Development16 The Impact of Pharmacogenetics on the Clinical Outcomes of Prodrugs; Index.

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.

Print version record.

Includes bibliographical references (pages 473-481) and index.