The chemistry, radiochemistry, radiobiology, and radiopharmacology of
radiopharmaceuticals containing copper radionuclides are reviewed. Cop
per radionuclides offer application in positron emission tomography, t
argeted radiotherapy, and single photon imaging. The chemistry of copp
er is relatively simple and well-suited to radiopharmaceutical applica
tion. Current radiopharmaceuticals include biomolecules labelled via b
ifunctional chelators primarily based on cyclic polyaminocarboxylates
and polyamines, and pyruvaldehyde-bis(N-4-methylthiosemicarbazone) (PT
SM) and its analogues. The chemistry of copper, of which only a fracti
on has yet been exploited, is likely to be applied more fully in the f
uture. Copyright (C) 1996 Elsevier Science Inc.