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