Synthesis and evaluation of Lys¹(α,γ-Folate)Lys³(¹⁷⁷Lu-DOTA)-Bombesin(1-14) as a potential theranostic radiopharmaceutical for breast cancer

  • Appl Radiat Isot. 2016 Jan:107:214-219. doi: 10.1016/j.apradiso.2015.10.030.
Liliana Aranda-Lara  1 ,  Guillermina Ferro-Flores  2 ,  Erika Azorín-Vega  3 ,  Flor de María Ramírez  3 ,  Nallely Jiménez-Mancilla  4 ,  Blanca Ocampo-García  3 ,  Clara Santos-Cuevas  3 ,  Keila Isaac-Olivé  5
Affiliations
  • 1. 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.
  • 2. Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico. Electronic address: [email protected].
  • 3. Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico.
  • 4. Catedrática CONACyT, Instituto Nacional de Investigaciones Nucleares, Ocoyoacac 52750, Estado de México, Mexico.
  • 5. Facultad de Medicina, Universidad Autónoma del Estado de México, Toluca 50180, Mexico.
PMID: 26545016 DOI: 10.1016/j.apradiso.2015.10.030
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.

Keywords
Breast cancer; Lutetium-177; Theranostic radiopharmaceuticals; Theterobivalent molecules.
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