Predicting oral absorption and bioavailability.

Publisher Summary The prediction of oral absorption and bioavailability is an important tool, both in the early phases of drug discovery to select the most promising leads for further optimization and in the later stages to select candidates for clinical development. Progress in predicting oral absorption is based on a much better understanding of the transport processes across membranes. The identification of the key physico-chemical properties, and in addition, the identification of the key transporter proteins and metabolizing enzymes in the gut wall, has led to the development of in vitro and in vivo screens that allow reasonably accurate estimates of oral absorption in man to be made. Predicting bioavailability is more challenging. However, in recent years, very promising progress has been made using a combination of several in vitro measures, as well as the development of in silico tools.