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

Edward Kerns (Author), Li Di (Author)
4.7 out of 5 stars  See all reviews (6 customer reviews)

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Book Description

February 19, 2008 0123695201 978-0123695208 1
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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Editorial Reviews

Review

JOURNAL OF MEDICINAL CHEMISTRY, OCTOBER 2008: "The authors do an excellent job of providing insight into the background of the many factors that influence drug-like properties...[This] easy-to-read text is...an excellent addition to the library of practicing medicinal chemists and of graduate students in the pharmaceutical sciences. It provides a wealth of information for a reasonable price."--Thomas E. Prisinzano, Dept. of Medicinal Chemistry, University of Kansas, KS, USA

DOODY'S, SEPTEMBER 2008: "This is a valuable reference for any scientist who works as part of a drug discovery team and especially those who are involved in ADME to toxicity optimization [.] The authors have done a nice job of presenting this information in a concise, readable format."--Thomas Pazdernik, University of Kansas Medical Center, KS, USA

"[Recently] I bought your excellent book, and I want to congratulate you and thank you for injecting life into the science of ADMET, lifting the subject to 'bestseller,' enjoyable reading material. It is the best book that I have come across that makes a great job of fostering collaborative interactions between ADMET and Medicinal Chemistry scientists in advancing strategies of drug discovery."--Dr. Collen Masimirembwa, Chief Scientific Officer, AiBST

"I am very impressed...[The book] 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 expertise function. The chapter on pharmacokinetics provides a very good overview of the topic. This book is well worth the purchase price." --Walter Korfmacher, NJ, USA

Product Details

  • Hardcover: 552 pages
  • Publisher: Academic Press; 1 edition (February 19, 2008)
  • Language: English
  • ISBN-10: 0123695201
  • ISBN-13: 978-0123695208
  • Product Dimensions: 10.3 x 7.6 x 1.4 inches
  • Shipping Weight: 3 pounds (View shipping rates and policies)
  • Average Customer Review: 4.7 out of 5 stars  See all reviews (6 customer reviews)
  • Amazon Best Sellers Rank: #157,222 in Books (See Top 100 in Books)

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6 of 7 people found the following review helpful:
5.0 out of 5 stars A very impressive book!, February 23, 2008
This review is from: Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization (Hardcover)
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.
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1 of 1 people found the following review helpful:
4.0 out of 5 stars The medicinal chemistry book you were looking for., March 28, 2009
This review is from: Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization (Hardcover)
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.
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5.0 out of 5 stars A very good service, September 19, 2011
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This review is from: Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization (Hardcover)
The book was really as new as they said , i couldn't believe , Hopefully they continue in their excellent services
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Inside This Book (learn more)
Key Phrases - Statistically Improbable Phrases (SIPs): (learn more)
solubility methods, permeability methods, pharmaceutical aspects, solution isotonic, transporter effects
Key Phrases - Capitalized Phrases (CAPs): (learn more)
Journal of Medicinal Chemistry, Drug Discovery Today, Journal of Pharmaceutical Sciences, Section References, Advanced Drug Delivery Reviews, Journal of Chromatography, Current Opinion, New York, Pharmaceutical Research, International Journal of Pharmaceutics, Structure Modification Strategies, Journal of Biomolecular Screening, Analytical Chemistry, Rapid Communications, Mutation Research, Chemical Biology, Section Problems, Drug Exposure, Inhibition Methods, Blood-Brain Barrier Methods, Effects of Properties, Company Web, Current Drug Metabolism, Consequences of Chirality, Current Topics
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