Regulated Bioanalysis—Historical Aspects and Key Concepts Related to Its Use

The history and key concepts of bioanalysis are discussed. Historically, the scientific need driving the development of bioanalytical methodology was the evolution of the science of pharmacology as well as the field of pharmacokinetics. Similarly, the ability to actually perform bioanalysis was linked to the development of analytical methodology/instrumentation. Each of these historical aspects of bioanalysis is discussed in this chapter. Key attributes of molecules quantitated in bioanalytical procedures for small molecules and protein therapeutics are described. Topics discussed in this regard include plasma protein binding, free drug versus total drug measurements, prodrugs versus active moieties, metabolites, minimum required dilution, and parallelism. In addition, important considerations with respect to different types of study samples are described. These factors include the influence of dosing vehicle and collection methodology. Matrices discussed include whole blood, urine, cerebral spinal fluid, tissues, and dried blood spots.