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

Poor oral bioavailability is one of the leading causes of compound failure in preclinical and clinical development. In pharmacology, bioavailability describes the fraction of an administered dose of a drug that actually reaches the systemic circulation and it is one of the essential tools in pharmacokinetics, as bioavailability must be considered when calculating dosages for non–intravenous routes of administration. 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 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 relate to humans, which is an underappreciate but complicated area of drug development

          Includes chapters about pharmacokinetic (PBPK) modeling and the Biopharmaceutics Drug Disposition Classification System (BDDCS)

          Has tutorials for applying strategies to medicinal chemistry practices of drug discovery / development

Ayman F. El–Kattan, B. Pharm, PhD, is Associate Research Fellow in Pfizer s Pharmacokinetics, Dynamics, and Metabolism Department. He is also an Adjunct Professor at the College of Pharmacy University of Rhode Island and serves on the executive committee of the physical pharmacy and biopharmaceutics and Northeastern Regional Discussion Group (NERDG) sections of the American Association of Pharmaceutical Scientists (AAPS). Dr. El–Kattan has been invited speaker over 30 times at national and international conferences and meetings and has published over 90 papers in peer–reviewed journals, book chapters, and proceedings.