title: Synthesis and evaluation of Lys¹(α,γ-Folate)Lys³(¹⁷⁷Lu-DOTA)-Bombesin(1-14) as a potential theranostic radiopharmaceutical for breast cancer.
abstract: The aim of this work was to synthesize Lys(1)(α,γ-Folate)-Lys(3)((177)Lu-DOTA)-Bombesin (1-14) ((177)Lu-Folate-BN), as well as to assess its potential for molecular imaging and targeted radiotherapy of breast tumors expressing folate receptors (FR) and gastrin-releasing peptide receptors (GRPR). Radiation absorbed doses of (177)Lu-Folate-BN (74 MBq, i.v.) estimated in athymic mice with T47D-induced breast tumors (positive to FR and GRPR), showed tumor doses of 23.9±2.1 Gy. T47D-tumors were clearly visible (Micro-SPECT/CT images). (177)Lu-Folate-BN demonstrated properties suitable as a theranostic radiopharmaceutical.
authors.affiliation: Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico; Facultad de Medicina, Universidad Autónoma del Estado de México, Toluca 50180, Mexico.
authors.forename: Liliana
authors.initials: L
authors.lastname: Aranda-Lara
authors.affiliation: Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico. Electronic address: ferro_flores@yahoo.com.mx.
authors.forename: Guillermina
authors.initials: G
authors.lastname: Ferro-Flores
authors.affiliation: Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico.
authors.forename: Erika
authors.initials: E
authors.lastname: Azorín-Vega
authors.affiliation: Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico.
authors.forename: Flor de María
authors.initials: FM
authors.lastname: Ramírez
authors.affiliation: Catedrática CONACyT, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico.
authors.forename: Nallely
authors.initials: N
authors.lastname: Jiménez-Mancilla
authors.affiliation: Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico.
authors.forename: Blanca
authors.initials: B
authors.lastname: Ocampo-García
authors.affiliation: Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico.
authors.forename: Clara
authors.initials: C
authors.lastname: Santos-Cuevas
authors.affiliation: Facultad de Medicina, Universidad Autónoma del Estado de México, Toluca 50180, Mexico.
authors.forename: Keila
authors.initials: K
authors.lastname: Isaac-Olivé
mesh_terms: D000818:Animals; D001839:Bombesin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000000981:diagnostic imaging / Q000532:radiotherapy*; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D005260:Female; D006801:Humans; D008187:Lutetium / Q000627:therapeutic use*; D051379:Mice; D008819:Mice, Nude; D064847:Multimodal Imaging; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D011868:Radioisotopes / Q000627:therapeutic use; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D011879:Radiotherapy Dosage; D000068936:Theranostic Nanomedicine / Q000379:methods; D015899:Tomography, Emission-Computed, Single-Photon; D014057:Tomography, X-Ray Computed; D023041:Xenograft Model Antitumor Assays
chemical_list: D056831:Coordination Complexes; D009842:Oligopeptides; D011868:Radioisotopes; D019275:Radiopharmaceuticals; C000611063:bombesin(1-14), lysyl(1)(alpha,gamma-folate)-lysyl(3)(177Lu-DOTA)-; D008187:Lutetium; D001839:Bombesin
keywords: Breast cancer; Lutetium-177; Theranostic radiopharmaceuticals; Theterobivalent molecules