title: A freeze-dried kit formulation for the preparation of Lys(27)(99mTc-EDDA/HYNIC)-Exendin(9-39)/99mTc-EDDA/HYNIC-Tyr3-Octreotide to detect benign and malignant insulinomas.
abstract: About 90% of insulinomas are benign and 5%-15% are malignant. Benign insulinomas express the glucagon-like peptide-1 receptor (GLP-1R) and low levels of somatostatin receptors (SSTR), while malignant insulinomas over-express SSTR or GLP-1R in low levels. A kit for the preparation of Lys(27)((99m)Tc-EDDA/HYNIC)-Exendin(9-39)/(99m)Tc-EDDA/HYNIC-Tyr(3)Octreotide was formulated to detect 100% of insulinomas. The formulation showed radiochemical purity of 97±1%, high stability in human serum, and GLP-1R and SSTR affinity. The biodistribution and imaging studies demonstrated properties suitable for its use as a target-specific agent for the simultaneous molecular imaging of GRP-1R- and/or SSTR-positive tumors.
authors.affiliation: Instituto Nacional de Investigaciones Nucleares, Estado de México, 52750, Mexico; Universidad Autónoma del Estado de México, Estado de México, 50180, Mexico.
authors.forename: Veronica
authors.initials: V
authors.lastname: Medina-García
authors.affiliation: Instituto Nacional de Investigaciones Nucleares, Estado de México, 52750, Mexico. Electronic address: ocampo_be@yahoo.com.mx.
authors.forename: Blanca E
authors.initials: BE
authors.lastname: Ocampo-García
authors.affiliation: Instituto Nacional de Investigaciones Nucleares, Estado de México, 52750, Mexico.
authors.forename: Guillermina
authors.initials: G
authors.lastname: Ferro-Flores
authors.affiliation: Instituto Nacional de Investigaciones Nucleares, Estado de México, 52750, Mexico.
authors.forename: Clara L
authors.initials: CL
authors.lastname: Santos-Cuevas
authors.affiliation: Instituto Nacional de Investigaciones Nucleares, Estado de México, 52750, Mexico; Universidad Autónoma del Estado de México, Estado de México, 50180, Mexico.
authors.forename: Liliana
authors.initials: L
authors.lastname: Aranda-Lara
authors.affiliation: Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán, México City, 14000, Mexico.
authors.forename: Rocio
authors.initials: R
authors.lastname: García-Becerra
authors.affiliation: Instituto Nacional de Ciencias Médicas y Nutrición Salvador Zubirán, México City, 14000, Mexico.
authors.forename: David
authors.initials: D
authors.lastname: Ordaz-Rosado
authors.affiliation: University of Padua, Padua, 35128, Italy.
authors.forename: Laura
authors.initials: L
authors.lastname: Melendez-Alafort
mesh_terms: D000818:Animals; D004492:Edetic Acid / Q000031:analogs & derivatives* / Q000737:chemistry; D005612:Freeze Drying; D006801:Humans; D007340:Insulinoma / Q000000981:diagnostic imaging* / Q000473:pathology; D008297:Male; D051379:Mice; D008819:Mice, Nude; D015609:Organotechnetium Compounds / Q000737:chemistry* / Q000493:pharmacokinetics*; D010190:Pancreatic Neoplasms / Q000000981:diagnostic imaging* / Q000473:pathology; D011854:Radiochemistry; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000493:pharmacokinetics*; D051381:Rats; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured
chemical_list: D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C026058:EDDA; D004492:Edetic Acid
keywords: Glucagon-like peptide 1 receptor; Insulinomas; Lys(27)((99m)Tc-EDDA/HYNIC)-Exendin(9-39); Somatostatin receptor