Polypharmacology in Drug Discovery

Polypharmacology in Drug Discovery

by Jens-Uwe Peters
     
 

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Polypharmacology can be the two-faced Janus in drug discovery and pharmacology: an adverse, off-target safety risk in some cases or a necessity for effectively treating complex diseases like psychosis and cancer. This book overviews these facets of polypharmacology to help drug discovery researchers both address adverse polypharmacology and approach the

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Overview

Polypharmacology can be the two-faced Janus in drug discovery and pharmacology: an adverse, off-target safety risk in some cases or a necessity for effectively treating complex diseases like psychosis and cancer. This book overviews these facets of polypharmacology to help drug discovery researchers both address adverse polypharmacology and approach the discovery of polypharmacological drugs, with a third section of the book uses selected case studies to illustrate drug discovery opportunities. This resource fosters interdisciplinary drug discovery research by guiding researchers in neighboring areas to polypharmacology.

Editorial Reviews

From the Publisher
“The book is well presented and the price is reasonable for anyone (drug designers, medicinal chemists, biochemists, biologists, clinicians and toxicologists) interested in any of the many facets that come together to make polypharmacology.”  (British Toxicology Society, 1 July 2013)

“However, anyone interested in the complex issues relating to drug promiscuity should find this very timely and topical book to be a reliable and stimulating reference that they will revisit many times.”  (ChemMedChem, 2012)

Doody's Review Service
Reviewer: Rachel R Chennault, PhD (American College of Clinical Pharmacy)
Description: This book examines the emerging polypharmacological philosophy in drug discovery research (a single compound with multiple targets), challenging the current "one-drug-one-target" approach to drug discovery. It reviews the necessary considerations during safety profiling to assess the delicate balance between promiscuous drugs' therapeutic efficacies (benefits) and adverse drug reactions, or ADRs (risks).
Purpose: Historically, researchers have sought to develop highly selective drugs in an effort to minimize ADRs due to unintended off-target effects. However, this book educates readers about the unique advantages that polypharmacological therapies have over single-target compounds, particularly in treating complex disease states, where either multiple factors contribute to pathogenicity or drug resistance arises.
Audience: This book is intended to guide drug development researchers in academic and industry sectors alike through the inherent challenges of the polypharmacological approach, with in-depth discussion of the benefits and dangers of promiscuous ligands and targets. Additionally, as the chapters of this book are authored by highly qualified experts in the pharmaceutical sciences, pharmacology students will benefit from the discussion of the fundamental concepts of polypharmacology.
Features: Organized into four distinct sections, the book begins with a discussion of the safety concerns due to off-target activities, as well as rationale for considering these activities early in the drug discovery process. The next section describes the advantages of a polypharmacological approach to drug development over a single-target philosophy by targeting networks of disease-related pathways, citing therapies for psychiatric diseases, cancer, bacterial infections, and epilepsy. The third section reviews state-of-the-art interdisciplinary approaches to promiscuous drug development that combine computational modeling with in vitro and in vivo screening assays. Finally, the last section contains various case studies with real examples of currently marketed multitargeted compounds that modulate diverse networks in the treatment of complex, polygenic diseases.
Assessment: To date, the discussion surrounding polypharmacology has been limited to a small number of journal articles and a single chapter in Drug Repositioning: Bringing New Life to Shelved Assets and Existing Drugs, Barratt and Frail Wiley-Blackwell, 2012). This book is a unique and comprehensive resource for navigating the field of promiscuous drug development and research.

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Product Details

ISBN-13:
9780470590904
Publisher:
Wiley
Publication date:
03/06/2012
Pages:
544
Product dimensions:
6.20(w) x 9.20(h) x 1.60(d)

What People are saying about this

From the Publisher
“Only recently, the characterization of promiscuous ligands turned from ‘dirty drugs’ into ‘agents being rich in pharmacology.’ … Polypharmacology in Drug Discovery covers all aspects, the good, the bad and the ugly. On the one hand, a lack of specificity (the ‘bad’) causes more or less serious side effects; inhibition of certain antitargets (the ‘ugly’), e.g. the hERG channel, results in a termination of a development project, in the past even the withdrawal of already marketed drugs; on the other hand, a desired promiscuity (the ‘good’) may be beneficial, e.g. in the case of certain CNS drugs and of anti-tumor kinase inhibitors. In Peters‘ book, all these topics are discussed in great detail by internationally leading authors. Therefore, Polypharmacology in Drug Discovery is of utmost importance for all drug designers, medicinal chemists as well as biochemists and biologists. The price of the book is in excellent relationship to its 500 pages and the overall quality, in content and presentation.”—Prof. Dr. Hugo Kubinyi

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