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

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

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: ferro_flores@yahoo.com.mx.
  • 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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