Nonclinical applications of quantitative whole-body autoradiography, and imaging mass spectrometry in drug discovery and development

Regulatory agencies require that drug developers characterize the absorption, pharmacokinetics, distribution, metabolism, and elimination (ADME) characteristics of new small and large molecule therapeutic entities. Quantitative whole-body autoradiography (QWBA) has become the definitive tool used for the determining tissue distribution patterns and is specifically requested by the FDA for IND submissions. However, the use of imaging mass spectrometry (IMS) to examine tissue distribution of xenobiotics has quickly gained the attention of pharmaceutical researchers because it does not require the use of radiolabeled test compounds and it can specifically identify the test article and their known metabolites with high imaging resolution. This talk will describe the state-of-the-art of both techniques and present examples of their applications in drug discovery and development.