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

By Edward H. Kerns, Li Di, Edward Kerns

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.

• Format: Hardcover
• Language: English
• ISBN: 0123695201
• ISBN13: 9780123695208
• Release Date: February 2008
• Publisher: Academic Press
• Length: 552 Pages
• Weight: 5.95 lbs.
• Dimensions: 10.2" x 1.4" x 7.3"

Customer Reviews

Impressive text.

This is quite simply a very impressive text and was great from the first to the last page. The introductory chapters adequately acquaint(or re-acquaint) the reader with concepts of drug-likeness and barriers to a successful drug. Topics covered in the intro chapters are then explained in great detail in individual chapters making the text very easy to follow and extremely informative. The later portion of the book describes methods used to assay and/or solve particular ADME/Tox issues and isn't necessarily useful to the non-practitioner but is definitely a go-to source if one needs this information. Also noteworthy are the problems at the end of each chapter that do a fairly good job of summarizing and applying the key topics learned in the chapter and answers are included in the appendix for reference. Overall this is a great book and would be especially useful for organic/medicinal chemistry doctoral/post-doctoral students.

Very, very helpful

This book contains a wealth of information concerning a number of topics of special interest to medicinal chemists in the pharmaceutical or animal science business. On many occasions I have sought and found useful information in this book - it serves as a very good primary source for basic information related to many aspects of preclinical drug discovery. This book fills a great void and should find its way onto the desk of any medicinal chemist who wants to learn more about understanding and manipulating the pharmaceutical properties of their compounds. Highly recommended!!

The medicinal chemistry book you were looking for.

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.

good for this neophyte

I needed to know what makes a good orally active drug. This book gave me most of the answers I needed in a very short amount of time. It's well written, well organized, and not too dense with jargon. There's a lot of overlap between chapters, which is good for quick reference but would probably bore a more informed reader.

A very impressive book!

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.