Automated radiosynthesis of [⁶⁸Ga]Ga‐PSMA‐11 and [¹⁷⁷Lu]Lu‐PSMA‐617 on the iPHASE MultiSyn module for clinical applications

Abstract

Prostate‐specific membrane antigen (PSMA)‐targeted imaging and therapy of prostate cancer using theranostic pairs is rapidly changing clinical practice. To facilitate clinical trials, fully automated procedures for the radiosyntheses of [ 68 Ga]Ga‐PSMA‐11 and [ 177 Lu]Lu‐PSMA‐617 were developed from commercially available precursors using the cassette based iPHASE MultiSyn module. Formulated and sterile radiopharmaceuticals were obtained in 76 ± 3% ( n = 20) and 91 ± 4% ( n = 15) radiochemical yields after 17 and 20 min, respectively. Radiochemical purity was always >95% and molar activities exceeded 792 ± 100 and 88 ± 6 GBq/μmol, respectively. Quality control showed conformity with all relevant release criteria and radiopharmaceuticals were used in the clinic.

Automated radiolabeling and handling of 177Lu‐ and 225Ac‐PSMA‐617 using a robotic pipettor

“…To test the feasibility of automated radiolabeling and product formulation using OT-2, a well-established radiolabeling protocol for 177 Lu-PSMA-617 was exploited. 8 [ 177 Lu]LuCl3 (Isotopia Molecular Imaging Ltd), PSMA-617 (MedChemExpress LLC) precursor solution, sodium acetate buffer, and gentisic acid solution were each prepared in 1.5 mL microcentrifuge tubes and placed on a rack in OT-2 block 9. An automated protocol for the radiolabeling and QC sampling of 177 Lu-PSMA-617 was constructed using the online Opentrons Protocol Designer.…”

[177Lu]Lu-PSMA-617 (PluvictoTM): The First FDA-Approved Radiotherapeutical for Treatment of Prostate Cancer

“…The fully automated GMP compliant production of [ 177 Lu]Lu-PSMA-617 using n.c.a. 177 Lu was described by the group of Scott et al [ 27 ]. The labeling precursor (103 nmol) was reacted with n.c.a.…”

Synthesis of [68Ga]Ga-PSMA-11 using the iMiDEV™ microfluidic platform

“…4,5 A number of technics have been described for a GMP-compliant 68 Ga-labelling of PSMA-11 using the 68 Ge/ 68 Ga generator on conventional automated synthesis modules (Scintomics GRP, miniAiO, iPHASE MultiSyn, iQS® Ga-68 Fluidic Labeling Module). [6][7][8][9][10] Moreover, two ready to use kits are commercially available, the first is developed by Isotopia Molecular Imaging Ltd. (isoPROtrace-11; Petach Tikva, Israel) 11,12 and the second one is from Telix Pharmaceuticals (TLX591-CDx, Illumet™ or Illuccix®; Melbourne, Australia). 12 The broadening of the theranostic approach and personalized medicine, particularly [ 177 Lu]Lu-PSMA-617 (Pluvicto®) for prostate cancer treatment, 13,14 revealed an emerging need for onsite and on-demand production of PET probes.…”