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Oral Bioavailability Assessment: Basics and Strategies for Drug Discovery and Development

Oral Bioavailability Assessment: Basics and Strategies for Drug Discovery and Development

Ayman F. El-Kattan, Mike S. Lee (Series Editor)

ISBN: 978-1-118-91692-6

May 2017

448 pages


Specifically geared to personnel in the pharmaceutical and biotechnology industries, this book describes the basics and challenges of oral bioavailability – one of the most significant hurdles in drug discovery and development.

•    Describes approaches to assess pharmacokinetics and how drug efflux and uptake transporters impact oral bioavailability
•    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 an 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