Positron emission tomography microdosing: a new concept with application in tracer and early clinical drug development
European Journal of Clinical Pharmacology September 1, 2003 Mats Bergstr�m, A. Grahn�n, B. L�ngstr�m 312 citations
Because three out of four drug candidates fail in clinical trials, and because costs and pressure to reduce animal experiments are rising, there is a need for better early human screening. Positron emission tomography (PET) allows non-invasive measurement of drug distribution and concentration in the human body when the drug is labeled with a positron-emitting radionuclide without altering its biochemical properties. Recent advances in rapid synthesis of labeled compounds enable many new drug candidates to be used as PET probes. The authors propose that early PET-microdosing studies, using very low drug doses, can help select or reject compounds based on human in vivo performance.