GMP-Compliant Automated Radiolabeling and Quality Controls of [Ga]Ga-FAPI-46 for Fibroblast Activation Protein-Targeted PET Imaging in Clinical Settings.

In nuclear medicine, molecular imaging of the tumor microenvironment using radiopharmaceuticals (RPs) targeting cancer-associated fibroblasts is gaining significant interest. Among these RPs, [Ga]Ga-FAPI-46 for positron emission tomography (PET) imaging is frequently used in clinical research protocols. To ensure that the production of this RP complies with good manufacturing practices, process automation is widely adopted.

Towards Optimal Automated Ga-Radiolabeling Conditions of the DOTA-Bisphosphonate BPAMD Without Pre-Purification of the Generator Eluate.

DOTA-functionalized bisphosphonates can be useful tools for PET imaging of bone metastases when radiolabeled with Ga. Moreover, the versatility of DOTA allows the complexation of radiometals with therapeutic applications (e.g.

"One Method to Label Them All": A Single Fully Automated Protocol for GMP-Compliant Ga Radiolabeling of PSMA-11, Transposable to PSMA-I&T and PSMA-617.

Background: Prostate-specific membrane antigen (PSMA) is an ideal target for molecular imaging and targeted radionuclide therapy in prostate cancer. Consequently, various PSMA ligands were developed. Some of these molecules are functionalized with a chelator that can host radiometals, such as Ga for PET imaging.

[Ga]Ga-FAPI-46 synthesis on a GAIA® module system: Thorough study of the automated radiolabeling reaction conditions.

The influence of several parameters involved in the Ga radiolabeling of FAPI-46 was studied at the scale of the automated reaction. Among the buffers tested, HEPES 0.3 M pH 4 allowed both high radiochemical purity (RCP) and radiochemical yield (RCY), without prepurification of Ga but after final purification of [Ga]Ga-FAPI-46 on a C cartridge.

Bisphosphonates as Radiopharmaceuticals: Spotlight on the Development and Clinical Use of DOTAZOL in Diagnostics and Palliative Radionuclide Therapy.

Bisphosphonates are therapeutic agents that have been used for almost five decades in the treatment of various bone diseases, such as osteoporosis, Paget disease and prevention of osseous complications in cancer patients. In nuclear medicine, simple bisphosphonates such as Tc-radiolabelled oxidronate and medronate remain first-line bone scintigraphic imaging agents for both oncology and non-oncology indications. In line with the growing interest in theranostic molecules, bifunctional bisphosphonates bearing a chelating moiety capable of complexing a variety of radiometals were designed.

Ac-Labeled Somatostatin Analogs in the Management of Neuroendocrine Tumors: From Radiochemistry to Clinic.

The widespread use of peptide receptor radionuclide therapy (PRRT) represents a major therapeutic breakthrough in nuclear medicine, particularly since the introduction of Lu-radiolabeled somatostatin analogs. These radiopharmaceuticals have especially improved progression-free survival and quality of life in patients with inoperable metastatic gastroenteropancreatic neuroendocrine tumors expressing somatostatin receptors. In the case of aggressive or resistant disease, the use of somatostatin derivatives radiolabeled with an alpha-emitter could provide a promising alternative.

Development and Implementation of a Professional Practices Evaluation during Radiopharmaceuticals Administration.

Securing both the patient and radiopharmaceuticals (RPs) circuit is an essential concern in nuclear medicine (NM). These circuits converge at the RP administration phase, a key step in patient management in NM. In a continuous quality improvement approach, we developed and implemented an evaluation of professional practices (EPPs) methodology focused on RPs injection to identify and correct deviations from good practices.

Lu-Dotatate administration using an infusion pump or a peristaltic pump: comparison of two methods.

Objectives: Lu-oxodotreotide (Lutathera) is an intravenous peptide receptor radionuclide therapy to treat unresectable metastatic digestive neuroendocrine tumours. The recommended method for Lutathera administration is gravity infusion; however, other appropriate and safe techniques are possible. This work compares two infusion methods from a medico-economic, radiation protection, efficiency and practicality point of view.

AAZTA-Derived Chelators for the Design of Innovative Radiopharmaceuticals with Theranostic Applications.

With the development of Ga and Lu radiochemistry, theranostic approaches in modern nuclear medicine enabling patient-centered personalized medicine applications have been growing in the last decade. In conjunction with the search for new relevant molecular targets, the design of innovative chelating agents to easily form stable complexes with various radiometals for theranostic applications has gained evident momentum. Initially conceived for magnetic resonance imaging applications, the chelating agent AAZTA features a mesocyclic seven-membered diazepane ring, conferring some of the properties of both acyclic and macrocyclic chelating agents.

Tailored Media-Fill Test Protocols Inspired by Ga Kit-Based Radiopharmaceuticals.

Gallium-68 radiolabeling is an increasingly common activity in radiopharmacy. Single vial cold kits to radiolabel DOTATOC and PSMA-11 with Ga were developed, either for manual or automated preparation. Both approaches are very specific and require aseptic compounding skills, raising the need for dedicated training.