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- Title
Preparation and preclinical evaluation of <sup>68</sup>Ga-iPSMA-BN as a potential heterodimeric radiotracer for PET-imaging of prostate cancer.
- Authors
Mendoza-Figueroa, Mónica Janet; Escudero-Castellanos, Alondra; Ramirez-Nava, Gerardo Julián; Ocampo-García, Blanca Elí; Santos-Cuevas, Clara Leticia; Ferro-Flores, Guillermina; Pedraza-Lopez, Martha; Avila-Rodriguez, Miguel Angel
- Abstract
In this research, we report the labeling and preclinical evaluation of the heterodimer 68Ga-iPSMA-BN ligand regarding its ability to target the prostate-specific membrane antigen (PSMA) and the gastrin-releasing peptide receptor (GRPr) in prostate cancer tumors. A heterodimer conjugate of iPSMA (PSMA inhibitor) (Nal-Lys-CO-Glu-OH) and Lys3-Bombesin (BN) with DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) as chelator was synthesized, labeled with 68Ga and the in vitro PSMA/GRPr affinity assessed. Using pulmonary micrometastasis LNCaP (PSMA+) and PC3 (GRPr+) models, the influence of the ligand heterobivalency and affinity on the tumor uptake was analyzed quantitatively from the micro-PET imaging data, obtaining promising results.
- Subjects
HETERODIMERS; RADIOACTIVE tracers; POSITRON emission tomography; CANCER diagnosis; PROSTATE cancer
- Publication
Journal of Radioanalytical & Nuclear Chemistry, 2018, Vol 318, Issue 3, p2097
- ISSN
0236-5731
- Publication type
Article
- DOI
10.1007/s10967-018-6285-3