Peptide-based radiopharmaceuticals and cytotoxic conjugates: potential tools against cancer.

A hope for the diagnosis and treatment of cancer is the development of new tumor-specific peptide-based radiopharmaceuticals. The overexpression of many peptide receptors on human tumors makes such receptors an attractive potential target for diagnostic imaging and radiotherapy with specifically designed radiolabeled peptides. The use of solid-phase peptide synthesis, and the availability of a wide range of bifunctional chelating agents for the convenient radiolabeling of bioactive peptides with different radionuclides have produced a wide variety of medicinally useful peptide radiopharmaceuticals. A few of these peptides, such as somatostatin, bombesin, cholecystokinin/gastrin, neurotensin and vasoactive intestinal peptide are currently under investigation for their possible clinical applications in nuclear oncology. This article presents the recent development in radiolabeled small peptides, with major emphasis on somatostatin and bombesin analogs.