Biologically targeted radiotherapy in clinical practice requires a mol
ecule which has a relative specificity for tumour tissue-the missile-c
oupled to a radionuclide with appropriate physical characteristics-the
warhead. When administered to a patient this combination should resul
t in selective irradiation of the target tumour cells with relative sp
aring of normal tissues. Simple ions and small molecules which follow
physiological pathways as either the natural substrates or analogues f
orm the best examples of biological targeting. Clinically valuable res
ults are seen with, for instance, iodine uptake by normal and malignan
t thyroid cells, incorporation of the calci-mimetic element strontium
in areas of increased bone metabolism and accumulation of the catechol
amine analogue meta-iodobenzylguanidine in neuroblastoma. The use of m
onoclonal antibodies as targeting vehicles has not proved to be a pana
cea, yet some patients with lymphoma, hepatoma and ovarian carcinoma h
ave obtained benefit. Current clinical studies in targeted radiotherap
y focus on the integration of radionuclide treatment with conventional
treatments, and the optimization of such combined approaches. The dev
elopment of modifications to offset the limitations inherent in the us
e of crude antibodies also offers an opportunity for improved clinical
outcomes.