Radiolabeled peptides in the diagnosis and therapy of oncological diseases.
There has been an exponential growth in the development of radiolabeled peptides for diagnostic and therapeutic applications in oncology. Peptides have fast clearance, rapid tissue penetration, low antigenicity and can be produced easily and inexpensively. However, peptides have problems with in vivo catabolism, unwanted physiological effects, and chelate attachment. The approved 111In-DTPA-OctreoScan, a somatostatin receptor binder, is well established for diagnosis of neuroendocrine tumors. NeoTect, an approved, 99mTc-labeled, somatostatin-receptor-binding analogue has good specificity for lung cancer detection. The receptors for Vasoactive Intestinal Peptide, Cholecystokinin-B/gastrin, Bombesin, Epidermal Growth Factor, and Alpha Melanocyte Stimulating Hormone and the Integrin, alpha(v)beta(3), are under active investigation as targets. Octreotide and its analogues labeled with 111In, 90Y, 64Cu or 177Lu are under study for the treatment of patients with promising results.
Weiner
Ronald E
RE
Department of Diagnostic Imaging and Therapeutics, University of Connecticut Health Center, Farmington 06030-2804, USA. weiner@adp.uchc.edu
Thakur
Mathew L
ML
D006801:Humans; D036341:Intercellular Signaling Peptides and Proteins; D009369:Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000532:radiotherapy*; D015282:Octreotide / Q000031:analogs & derivatives* / Q000627:therapeutic use; D004369:Pentetic Acid / Q000031:analogs & derivatives* / Q000627:therapeutic use; D010455:Peptides / Q000737:chemistry / Q000627:therapeutic use*; D010456:Peptides, Cyclic / Q000627:therapeutic use; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000627:therapeutic use*; D018000:Receptors, Peptide / Q000378:metabolism; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000627:therapeutic use
D036341:Intercellular Signaling Peptides and Proteins; C121869:NeoTect; D010455:Peptides; D010456:Peptides, Cyclic; D019275:Radiopharmaceuticals; D018000:Receptors, Peptide; C060347:lanreotide; C071632:SDZ 215-811; D013004:Somatostatin; D004369:Pentetic Acid; D015282:Octreotide