Prior to clinical trials, new drug molecules are examined and tested using in silico and in vitro approaches to weed out the ones with unwanted characteristics, such as low efficacy, toxicity or problematic pharmacokinetics. Despite the fact that the development of these approaches has progressed enormously in the last few years, they are still not advanced enough to replace in vivo animal studies.

This e-book explains the rationale of performing in vivo pharmacokinetic studies and describes common experimental set-ups supporting drug development. The aim of these studies is usually to evaluate whether the drug candidate can be absorbed via oral administration (bioavailability) or to determine other pharmacokinetic parameters, such as, clearance, half-life, volume of distribution, etc. These parameters can be used, e.g. for comparison of compounds for selecting a lead candidate, or for predicting safe starting dose in clinical trials. Not even perfectly planned and performed in vivo study is of any use if you can’t analyse your samples reliably. Therefore, a large part of this book is dedicated for the analytical aspects of biosamples, mainly from LC/MS perspective.