Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization PDF

Rating: (7 reviews) Author: Edward Kerns ISBN : 9780123695208 New from $45.84 Format: PDF

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Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process.

The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties.

* Serves as an essential working handbook aimed at scientists and students in medicinal chemistry
* Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies
* Discusses improvements in pharmacokinetics from a practical chemist's standpoint

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• Product Details
• Table of Contents
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• Hardcover: 552 pages
• Publisher: Academic Press; 1 edition (February 19, 2008)
• Language: English
• ISBN-10: 0123695201
• ISBN-13: 978-0123695208
• Product Dimensions: 1.4 x 7.5 x 10.2 inches
• Shipping Weight: 3 pounds (View shipping rates and policies)

Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization PDF

I have spent some of the last two days reading this book and I am very impressed with it. It is destined to become an authoritative text on the whole topic area of drug-like molecules and ADME screening. The chapters are well written and include sufficient detail and references so that the reader can make use of the information effectively. The book could be used in a graduate-level course for medicinal chemists or DMPK scientists.
The book would also be very helpful for scientists working in one area of DMPK who wish to become DMPK project managers and need to increase their understanding of other areas of DMPK that are outside of their own specific expetise function. The chapter on pharmacokinetics was well written and provides a very good overview of the topic. Overall, I can state that this book is well worth the purchase price.

By Walter Korfmacher

It is very nice overview of the practical topics for the practicing medicinal chemist.
For the just arrived synthetic chemist, it represents a way of looking not so puzzled in project meetings when interacting with experienced collegues.
For senior drug-hunters, it is a guide to check for clear understanding of drug properties in the selection and optimization of new leads. Emphasis is placed on the methods for measuring properties using high throughput, diagnostic and in-depth methods.
In a nutshell, a very useful learning material for scientists engaged in drug discovery and a reference for regular use.

By Carlos Mateos Gutierrez