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Oral Bioavailability Assessment. Basics and Strategies for Drug Discovery and Development. Wiley Series on Pharmaceutical Science and Biotechnology: Practices, Applications and Methods

  • ID: 3630927
  • Book
  • August 2017
  • 448 Pages
  • John Wiley and Sons Ltd
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Poor oral bioavailability is one of the leading causes of compound attrition and failure in preclinical and clinical development. In pharmacokinetics, oral bioavailability describes the fraction of an administered dose of a drug that reaches the systemic circulation following oral dosing. It is one of the essential parameters, as bioavailability must be considered when calculating oral doses needed to increase probability of testing the biological mechanism in humans. Since drug developability has become an important criterion to measure the success of scientists working in drug companies, understanding and testing a drug candidate′s oral bioavailability is a critical step in the development process.

Specifically geared to personnel in the pharmaceutical and biotechnology industries, Oral Bioavailability Assessment: Basics and Strategies for Drug Discovery and Development describes the basics and challenges of oral bioavailability one of the most significant hurdles in drug discovery and development. The book emphasizes the impact of drug transporters on drug absorption and practices for addressing bioavailability problems. The author includes tutorials for applying these strategies to medicinal chemistry for hit selection, lead optimization, and development candidate selection.

Writing from extensive experience in drug discovery and development, giving short courses on the topic, the author presents the material in an accessible and practical manner that:

  • Helps readers reduce the failure rate of drug candidates when transitioning from the bench to the clinic during development
  • Explains how preclinical animal models used in preclinical testing and in vitro tools translate to humans, which is underappreciated and complicated area of drug development
  • Includes chapters about pharmacokinetic modelling, the Biopharmaceutics Drug Disposition Classification System (BDDCS), and the Extended Clearance Classification System (ECCS)
  • Has tutorials for applying strategies to medicinal chemistry practices of drug discovery/development
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1 Drug Pharmacokinetics and Toxicokinetics 1

2 GIT Anatomy and Physiology and Drug Oral Bioavailability: Impact of Species Differences 35

3 Drug Routes of Excretion 77

4 Physicochemical and Biopharmaceutical Properties that Affect Drug Absorption of Compounds Absorbed by Passive Diffusion 139

5 Physicochemical and Biopharmaceutical Factors Affecting Hepatic/Intestinal First–Pass Effect 173

6 Impact of Intestinal Efflux Transporters on Oral Absorption 203

7 Impact of Influx Transporters on Drug Absorption 269

8 Extended Clearance Classification System (ECCS) and its Utility in Predicting Clearance Rate–Determining Step in Drug Discovery 309

9 In Vitro and In Situ Approaches to Measure Intestinal Permeability and Efflux Transporters 331

10 In Silico Approaches to Predict Intestinal Permeability 347

11 In Vivo Preclinical Approaches to Deconvolute The Contribution of First–Pass Effect from Oral Absorption 357

12 In Vitro Approaches to Assess Hepatic Metabolism and First–Pass Effect 377

13 The Utility of ECCS as a Roadmap to Improve Oral Bioavailability of New Molecular Entities: Industrial Perspective 387


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Ayman F. El–Kattan
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