177Lu-DOTA-HYNIC-Lys(Nal)-Urea-Glu: synthesis and assessment of the ability to target the prostate specific membrane antigen
- 101 Downloads
SPECT/CT images have proved the capability of 99mTc-EDDA/HYNIC-Lys(β-naphthylalanine)-NH-CO-NH-Glu to detect prostate cancer tumors in patients. Considering that theranostics combines the potential of therapeutic and diagnostic radionuclides in the same molecular probe, this research aimed to prepare 177Lu-DOTA-HYNIC-Lys(β-naphthylalanine)-NH-CO-NH-Glu (177Lu-iPSMA) and evaluate the in vitro and in vivo radiotracer ability to target the PSMA protein overexpressed in prostate cancer cells (LNCaP). 177Lu-iPSMA, obtained with radiochemical purities of 99%, showed specific in vitro and in vivo recognition for PSMA in prostate cancer cells and high LNCaP-tumor uptake (11 ± 2% ID/g at 24 h). The results obtained warrant further studies to evaluate the therapeutic efficacy of 177Lu-iPSMA.
KeywordsDOTA-HYNIC-PSMA inhibitor 177Lu-iPSMA Prostate cancer Theranostic pair
This research received financial support from the Mexican National Council of Science and Technology (CONACyT-Mexico, Grant 242443). This work was performed as part of the activities of the ‘‘Laboratorio Nacional de Investigación y Desarrollo de Radiofármacos, CONACyT’’.
Compliance with ethical standards
Conflict of interest
The authors declare no potential conflicts of interest with regard to the research, authorship, and/or publication of this article.
All applicable international, national, and/or institutional guidelines for the care and use of animals were followed. This research was approved by the CICUAL-ININ ethics committee (Internal committee of care and use of laboratory animals of the National Institute of Nuclear Research, Approval No. 01/02/2018).
- 2.Santoni M, Scarpelli M, Mazzucchelli R et al (2013) Targeting prostate-specific membrane antigen for personalized therapies in prostate cancer: morphologic and molecular backgrounds and future promises. J Biol Regul Homeost Agents 28:555–563Google Scholar
- 13.Ferro-Flores G, Ocampo-Garcia B, Santos-Cuevas C et al (2017) 99mTc-EDDA/HYNIC-iPSMA as a radiopharmaceutical for detecting the overexpression of prostate-specific membrane antigen. Patent Cooperation Treaty Application. Patent No. WO2017222362Google Scholar