There is an increasing realization of the role of non-invasive monitoring o
f drug pharmacology. In this review, we discuss the role of positron emissi
on tomography in such monitoring of tumour and normal tissue drug pharmacok
inetics as well as assessment of tumour response, drug-receptor interaction
s and mechanisms of drug action and resistance. These studies represent a m
ultidisciplinary research effort involving radiochemists, imaging scientist
s, clinicians, pharmacologists and mathematical modellers. This review eval
uates achievements in the field from assessment of commonly used therapeuti
c agents such as 5-fluorouracil to target specific molecules such as marker
s for gene expression. It is envisaged that application of this technology
will facilitate rational drug design and rapid translation of new ideas to
the bedside. (C) 2000 Elsevier Science B.V. All rights reserved.