Analogue based Drug Discovery III 1st Edition by Janos Fischer, Robin Ganellin, David Rotella ISBN 978-3527330737 3527330737

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Product details: 

ISBN 10:  3527330737

ISBN 13: 978-3527330737

Author:  Janos Fischer, C. Robin Ganellin, David P. Rotella 

Most drugs are analogue drugs. There are no general rules how a new drug can be discovered, nevertheless, there are some observations which help to find a new drug, and also an individual story of a drug discovery can initiate and help new discoveries. Volume III is a continuation of the successful book series with new examples of established and recently introduced drugs.
The major part of the book is written by key inventors either as a case study or a study of an analogue class. With its wide range across a variety of therapeutic fields and chemical classes, this is of interest to virtually every researcher in drug discovery and pharmaceutical chemistry, and — together with the previous volumes — constitutes the first systematic approach to drug analogue development.

Table of contents: 

PART I – General Aspects
Pioneer and Analogue Drugs

Monotarget, Dual‑Acting, Multitarget Drugs – Summary

Competition in the Pharmaceutical Drug Development

Are analogue-based drugs “just copies”?

Insights from GPCR patent space

Metabolic Stability and Analogue‑Based Drug Discovery

Metabolism-guided design, fluorine substitution

Clearance, half-life, enzyme liabilities, mutagenicity, electrophilic/reactive metabolites (RMs)

Case studies in RM elimination

Use of Macrocycles in Drug Design (case study: ulimorelin)

From high-throughput screening to preclinical, clinical evaluation

PART II – Drug Classes
Anticancer Drugs Targeting Epigenetic Enzymes

DNMT and HDAC inhibitors (e.g., azacitidine, vorinostat)

Thienopyridyl & Direct‑Acting P2Y₁₂ Receptor Antagonists (antiplatelet drugs)

Selective Estrogen Receptor Modulators

Covers tamoxifen, raloxifene

Non‑peptide Vasopressin V₂ Receptor Antagonists

Cysteinyl-Leukotriene Receptor Antagonists

Includes zafirlukast, montelukast, pranlukast

PART III – Case Studies
Discovery of Dabigatran Etexilate (oral anticoagulant)

Discovery of Citalopram & Refinement to Escitalopram (SSRIs)

Tapentadol: From Morphine & Tramadol to a New Analgesic

Novel Taxanes: Cabazitaxel Case Study

Discovery of Boceprevir & Narlaprevir (HCV protease inhibitors; structure-based design)

Febuxostat: A New‑Generation Uric Acid Production Inhibitor (anti-gout agent)

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Tags: Janos Fischer, Robin Ganellin, David Rotella, Drug Discovery III