Radiolabelled peptides are an emerging class of radiopharmaceuticals that s
hare chemical and biological properties. From the chemical point of view th
ey have a poly-amino acid structure varying from 3 to more that 200 amino a
cids, and they are labelled with different isotopes directly or by a linker
. Biologically, they bind to specific cell membrane receptors, thus providi
ng in vivo histopathological information for diagnostic put-poses, therapy
follow-up or targeted radiotherapy. This paper reviews most of the radiolab
elled peptides that have been tested in animals and humans in the fields of
oncology, neurology, cardiology, inflammation/infection, atherosclerosis a
nd thrombosis. A new classification is also proposed for peptides targeting
tumour cells based on the biological function of target receptors. These t
ailored radiopharmaceuticals are the basis of the new era of "molecular nuc
lear medicine".