prodrug design

Prodrug Design
Author: Vivekkumar K Redasani
Publisher: Academic Press
Release Date: 2015-07-07
Pages: 84
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

Prodrug Design: Perspectives, Approaches and Applications in Medicinal Chemistry provides a focused overview of this critical area of drug discovery, as that continuous process strives not only to discover new drug compounds but also to modify the existing ones. This valuable primer supports this mission of drug development and its goal of reducing undesired effects and improving therapeutic effectiveness of drug compounds. Providing a unique compilation of data, insightful case studies, and review of existing literature in the area, the book will promote innovation in medicinal and pharmaceutical chemistry research, exploring the limitations of existing drugs and their improvement. Prodrug Design reviews marketed compounds, the safety of promoieties, and a detailed classification of prodrugs organized by therapeutic area for easy reference. Offers unique, detailed overview of Prodrug research and literature Provides detailed chemical structures Includes Prodrug listing by therapeutic area

Prodrugs Design
Author: Rafik Karaman
Publisher: Nova Science Pub Incorporated
Release Date: 2014-07-01
Pages: 277
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

The prodrug approach is a promising and well established strategy for the development of new entities that possess superior efficacy, selectivity and reduced toxicity. Hence an optimized therapeutic outcome can be accomplished using this approach. Prodrug design is becoming more elaborate in the development of efficient and selective drug delivery systems. The targeted prodrug approach, in combination with gene delivery and controlled expression of enzymes and carrier proteins, is a promising strategy for precise and efficient drug delivery and enhancement of the therapeutic effect. This book describes in details all prodrug approaches and examples of prodrugs that succeeded to enter the market. There are two major prodrug design approaches that are considered as widely used among all other approaches: the targeted drug design approach by which prodrugs can be designed to target specific enzymes or carriers by considering enzyme-substrate specificity or carrier-substrate specificity in order to overcome various undesirable drug properties. Examples for such approach is the antibody-directed enzyme prodrug therapy (ADEPT), gene-directed enzyme prodrug therapy (GDEPT), virus-directed enzyme prodrug therapy (VDEPT) and GDEPT. In addition, this book describes in details a novel prodrug chemical approach which is based on intramolecular reactions that were utilized to understand how enzymes exert their high catalysis. The information gained from the experimental and theoretical calculations on these enzyme models was used to design efficient chemical moieties to be utilized as prodrug linkers with the potential to release the corresponding parent drugs in a slow or fast release manner. Several prodrugs for commonly used drugs suffer from low bioavailability or/and bitter sensation were designed using quantum mechanics methods (DFT and ab initio) and recently a large number among these prodrugs were synthesized. Examples of such prodrugs are presented in the different chapters of the book.

Hydrolysis In Drug And Prodrug Metabolism
Author: Bernard Testa
Publisher: John Wiley & Sons
Release Date: 2003-08
Pages: 780
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

Many drugs and other xenobiotics (e.g., preservatives, insecticides, and plastifiers) contain hydrolyzable moieties such as ester or amide groups. In biological media, such foreign compounds are, therefore, important substrates for hydrolytic reactions catalyzed by hydrolases or proceeding non-enzymatically. Despite their significance, until now, no book has been dedicated to hydrolysis and hydrolases in the metabolism of drugs and other xenobiotics. This work fills a gap in the literature and reviews metabolic reactions of hydrolysis and hydarion from the point of views of enzymes, substrates, and reactions.

Design Of Prodrugs
Author: Hans Bundgaard
Publisher: Elsevier Publishing Company
Release Date: 1985
Pages: 360
ISBN:
Available Language: English, Spanish, And French
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Prodrugs
Author: Valentino Stella
Publisher: Springer Science & Business Media
Release Date: 2007-03-12
Pages: 1464
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

These volumes represent a comprehensive guide to prodrugs. They guide the reader through the current status of the prodrug concept and its many applications and highlight its many successes in overcoming formulation and delivery of problematic drugs. Replete with examples of approved and marketed prodrugs, these volumes introduce the topic to the novice as well as professional in the design of prodrugs.

Prodrugs And Targeted Delivery
Author: Jarkko Rautio
Publisher: John Wiley & Sons
Release Date: 2011-01-11
Pages: 520
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

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.

Textbook Of Drug Design And Discovery  Third Edition
Author: Tommy Liljefors
Publisher: CRC Press
Release Date: 2002-07-25
Pages: 592
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

Building on the success of the previous editions, Textbook of Drug Design and Discovery has been thoroughly revised and updated to provide a complete source of information on all facets of drug design and discovery for students of chemistry, pharmacy, pharmacology, biochemistry, and medicine. The book follows drug design from the initial lead identification through optimization and structure-activity relationship with reference to the final processes of clinical evaluation and registration. Chapters investigate the design of enzyme inhibitors and drugs for particular cellular targets such as ion channels and receptors, and also explore specific classes of drug such as peptidomimetics, antivirals and anticancer agents. The use of gene technology in pharmaceutical research, computer modeling techniques, and combinatorial approaches are also included.

Gibaldi S Drug Delivery Systems In Pharmaceutical Care
Author: Mary Lee
Publisher: ASHP
Release Date: 2007
Pages: 525
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

It is important to make therapeutics a critical component of teaching about dosage forms and to make dosage forms and drug delivery systems an integral part of therapeutics. This book will be the first to focus on the therapeutic impact of drug dosage forms.Tying together concepts of traditional pharmaceutics with therapeutics, Drug Delivery Systemsin Pharmaceutical Care demonstrates how the modern clinical pharmacist can integrate knowledge in pharmaceutical sciences and therapeutics with appreciation of patient needs and nuances to advise on preferable and optimal product choices.Each chapter represents a collaboration of a clinical pharmacist practitioner and a pharmaceutical scientist. This unique perspective takes the science of dosage form design and helps translate the theory into the pragmatic.Special Features: Case studies and problems to help students get a better understanding of concepts Well-organized chapters with outlines and objectives Summary tables and helpful figures, along with reasonable compilations of original references Final sections with 'Learning Points' that reinforce essential material. Foreword by William J. Jusko, PhD, Professor and Chair, University of Buffalo, Department of Pharmaceutical Sciences

Drug Absorption Evaluation  Prodrug Design And Intestinal Transporter Expression By Genechip Analysis
Author: Duxin Sun
Publisher:
Release Date: 2002
Pages:
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

Enzyme Prodrug Strategies For Cancer Therapy
Author: Roger G. Melton
Publisher: Springer Science & Business Media
Release Date: 2012-12-06
Pages: 257
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

Antibody-directed enzyme prodrug therapy (ADEPT) directly addresses the major problem in cancer chemotherapy-its lack of selectivity. Antibody delivery combined with the amplification provided by the enzymatic activation of prodrugs enables selection to be made between tumour and normal tissue. ADEPT offers a novel field of opportunities in the therapy of systemic cancer and may be a major advance for the treatment of solid tumours. This book is the first to describe ADEPT in detail. Each chapter reviews an aspect of the immunology, enzymology, biochemistry, chemistry, and cancer chemotherapy which have been integrated into the ADEPT concept. An additional chapter describes the related approach of gene-directed enzyme prodrug therapy (GDEPT). This latter approach is still in its infancy but ADEPT has entered the clinic. The initial clinical studies with ADEPT are included and discussed in detail.

Application Of Peptide Based Prodrug Chemistry In Drug Development
Author: Arnab De
Publisher: Springer Science & Business Media
Release Date: 2012-08-18
Pages: 89
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

Macromolecular (specifically peptide-based) drugs could potentially be highly effective medicines. However they have a relatively short duration of action and variable therapeutic index. An example of such a peptide is Glucagon-like Peptide I which could potentially be used as a revolutionary drug for diabetes. This is because it stimulates insulin only when the blood glucose level is high thereby reducing the risk of hypoglycemia (a significant disadvantage of using insulin is that an insulin overdose is the single most potent cause of life-threatening hypoglycemia). However it’s short duration of action (half-life of 2 minutes in plasma) precludes its therapeutic use. In this volume, the use of novel therapeutics like GLP1 as an alternative to tradition insulin-based drugs in diabetes is described. Application of Peptide-Based Prodrug Chemistry in Drug Development elucidates the traditional concept of prodrugs as “specialized non-toxic protective groups used in a transient manner to alter or to eliminate certain limiting properties in the parent small molecule” (IUPAC definition). It goes on to provide insight into how prodrugs of peptides (with GLP1 as an example) could be appropriately used to extend the biological half life, broaden the therapeutic index of macromolecules and improve the pharmacodynamics of such drugs. Author explains the logic behind designing peptide prodrugs, synthetic procedures and bioassays to examine the conversion of the prodrug to the drug under therapeutic conditions. The prodrugs described slowly convert to the parent drug at physiological conditions of 37C and pH 7.2 driven by their inherent chemical instability without the need of any enzymatic cleavage. The diketopiperazine and diketomorpholine (DKP and DMP) strategies for prodrug conversion are demonstrated in detail with special emphasis on the chemical flexibility that it offers to develop prodrugs with variable time actions. This book will be of useful to chemists, biochemists, medicinal chemists, biologists and people in the medical profession (doctors). It may be used in undergraduate classes but will certainly help post-graduate students and advanced professionals. The author is grateful to Prof. Richard DiMarchi (Standiford H. Cox Professor of Chemistry and the Linda & Jack Gill Chair in Biomolecular Sciences at Indiana University) for valuable suggestions. The foreword for the book has been written by Prof. Jean Martinez, (Legion d'Honneur awarded by the French Republic; Professor of Chemistry and Medicinal Chemistry of the University of Montpellier, France; and Chairman of European Peptide Society, 2002-2010).

Peptide Transport And Delivery Into The Central Nervous System
Author: Laszlo Prokai
Publisher: Springer Science & Business Media
Release Date: 2003
Pages: 245
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

Various peptides native to the brain and the spinal cord, as well as various synthetic peptides, peptide analogues and peptidomimetics could be useful in the treatment of diseases of the central nervous system. This book provides an overview of the role and neuropharmaceutical potential of these peptides, and discusses the state of the art and future trends in the use of peptide pharmacotherapy involving the brain.

Design Of Biopharmaceutical Properties Through Prodrugs And Analogs
Author: Edward B. Roche
Publisher: Amer Pharmacutical Assn
Release Date: 1977
Pages: 455
ISBN:
Available Language: English, Spanish, And French
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Chirality In Drug Design And Development
Author: Indra K. Reddy
Publisher: CRC Press
Release Date: 2004-03-15
Pages: 1200
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

Covering every essential element in the development of chiral products, this reference provides a solid overview of the formulation, biopharmaceutical characteristics, and regulatory issues impacting the production of these pharmaceuticals. It supports researchers as they evaluate the pharmacodynamic, pharmacokinetic, and toxicological characteristics of specific enantiomers and chiral drug compounds and addresses in one convenient reference all the major challenges pertaining to drug chirality that have been neglected in the literature. Chirality in Drug Design and Development collects the latest studies from an interdisciplinary team of experts on chiral drug design.

Design Of Enzymatically Reconvertible Prodrugs
Author: Pradip Kumar Banerjee
Publisher:
Release Date: 1979
Pages: 376
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

Designing Anticancer Prodrugs For Targeting Drug Transporters And Activating Enzymes
Author: Christopher P. Landowski
Publisher:
Release Date: 2005
Pages:
ISBN:
Available Language: English, Spanish, And French
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Frontiers In Drug Design And Discovery
Author: Atta-ur- Rahman
Publisher: Bentham Science Publishers
Release Date: 2009
Pages: 457
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

"Frontiers in Drug Design and Discovery" is an Ebook series devoted to publishing the latest and the most important advances in drug design and discovery. Eminent scientists write contributions on all areas of rational drug design and drug discovery inclu

Topical Drug Bioavailability  Bioequivalence  And Penetration
Author: Vinod P. Shah
Publisher: Springer Science & Business Media
Release Date: 1993-11-30
Pages: 453
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

This volume presents the state-of-the-art of measuring percutaneous penetration and determining biological relevance in dermal and transdermal drug delivery. Both in vivo and in vitro models and methods are discussed in detail to provide pharmaceutical drug developers with an invaluable guide and reference.

Medicinal Chemistry And Drug Discovery  Drug Discovery And Drug Development
Author: Alfred Burger
Publisher:
Release Date: 2003
Pages:
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

The Organic Chemistry Of Drug Design And Drug Action
Author: Richard B. Silverman
Publisher: Elsevier
Release Date: 2012-12-02
Pages: 617
ISBN:
Available Language: English, Spanish, And French
EBOOK SYNOPSIS:

Standard medicinal chemistry courses and texts are organized by classes of drugs with an emphasis on descriptions of their biological and pharmacological effects. This book represents a new approach based on physical organic chemical principles and reaction mechanisms that allow the reader to extrapolate to many related classes of drug molecules. The Second Edition reflects the significant changes in the drug industry over the past decade, and includes chapter problems and other elements that make the book more useful for course instruction. New edition includes new chapter problems and exercises to help students learn, plus extensive references and illustrations Clearly presents an organic chemist's perspective of how drugs are designed and function, incorporating the extensive changes in the drug industry over the past ten years Well-respected author has published over 200 articles, earned 21 patents, and invented a drug that is under consideration for commercialization