Oral Bioavailability Assessment
Basics and Strategies for Drug Discovery and Development
Wiley Series on Pharmaceutical Science
1. Edition August 2017
448 Pages, Hardcover
Wiley & Sons Ltd
Short Description
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. The author presents the material in an accessible and practical manner, helping readers reduce failure rate in drug development when moving a candidate drug from the bench to the clinic.
Further versions
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
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
INDEX 431
