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Receptor imaging of human diseases using radiolabeled peptides.

The peptide somatostatin and its analog octreotide play an important role in neoplasia where their actions have been shown to be mediated by specific somatostatin receptors located in the tumor tissue. The identification of a high density of SS receptors in vitro in different types of human tumors has provided completely new and attractive possibilities for their diagnostic localization in vivo. This can be achieved by intravenous injection of 123I-[Tyr3]-octreotide or 111In-DTPA-D-Phe1-octreotide in patients suspected of having SS receptor-positive tumors and by subsequent localization of the tumors with gamma camera scintigraphy techniques. Hot spots representing radioligand binding on SS receptor-positive tumors are visualized with this method. This new SS receptor imaging method may help the clinicians for the localization of the primary tumor and its metastases, for the staging of certain tumors, to predict a successful SS therapy, and as a prognostic or differential diagnostic marker. It may also be of use in non-tumoral pathologies, to localize selected inflammatory processes and to monitor anti-inflammatory therapy. Somatostatin receptor imaging represents the first example of the clinical use of a small peptide as an efficient in vivo diagnostic tool and may be considered as a paradigm for further research on the role and the potential diagnostic use of other peptide receptors in pathological states.