Preparation and quality control of 225Ac-PSMA-617 with potential to treat prostate cancer

Rezazadeh-Sefideh, Fatemeh; Shirvani, Simindokht; Hosseini, Seyed Abolfazl; Zolghadri, Samaneh; Yousefnia, Hassan; Bahramisamani, Ali

doi:10.24200/nst.2025.1707.2065

Preparation and quality control of 225Ac-PSMA-617 with potential to treat prostate cancer

Articles in Press

Document Type : Research Paper

Authors

Fatemeh Rezazadeh-Sefideh ¹

simindokht shirvani ²

Seyed Abolfazl Hosseini ³

Samaneh Zolghadri ⁴

Hassan Yousefnia ⁴

ali bahramisamani ⁴

¹ 1. Radiation Medicine Department, Faculty of Energy, Sharif University of Technology, P.O.Box: 1458889694, Tehran-Iran

² دکتر

³ دانشگاه صنعتی شریف

⁴ Nuclear Science and Technology Research Institute, AEOI, P.O.Box: 14395-836, Tehran – Iran

https://doi.org/10.24200/nst.2025.1707.2065

Abstract

Prostate-Specific Membrane Antigen (PSMA) is a membrane-bound glycoprotein that is overexpressed in prostate cancer. PSMA has been recognized as a promising target in the diagnosis and treatment of prostate cancer. Alpha particle-emitting radionuclides have shown promising results as radiotherapeutic agents for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Actinium-225 (225Ac), with T½ = 9.9 d, has been one of the most commonly used options for clinical applications. 225Ac emits five alpha particles with energy ranges from 5.8 to 8.4 MeV during its decay chain. The decay cascade also includes beta particle emissions ranging from 0.6 to 2 MeV and gamma emissions from Francium-221 (221Fr) and Bismuth-213 (213Bi). Considering the favorable properties of this radionuclide for targeted alpha therapy of prostate cancer, this study initially determined the radionuclide purity of 225Ac using gamma spectrometry equipped with a high-resolution high-purity germanium detector and a liquid scintillation detector. Then, PSMA-617 labeling was performed with 225Ac at 95°C for 30 minutes. The radiochemical purity of the resulting compound was determined to be over %96 using thin-layer chromatography. This study demonstrated the successful labeling of PSMA-617 with 225Ac under optimal conditions and high radiochemical purity for clinical applications.

Keywords

Prostate cancer

225Ac

PSMA-617

HPGe detector

Main Subjects