Abstract
A large number of applications for fibroblast activation protein inhibitors (FAPI)-based PET agents have been evaluated in conditions ranging from cancer to non-malignant diseases such as myocardial infarction. In particular, 68Ga-FAPI-46 was reported to have a high specificity and affinity for FAP-expressing cells, a fast and high accumulation in tumor lesions/injuries together with a fast body clearance when investigated in vivo. Due to the increasing interest in the use of the agent both preclinically and clinically, we developed an automated synthesis for the production of 68Ga-FAPI-46 on a Trasis AiO platform. The new synthetic procedure, which included the processing of the generator eluate using a strong cation exchange resin and a final purification step through an HLB followed by a QMA cartridge, yielded 68Ga-FAPI-46 with high radiochemical purity (>98%) and apparent molar activity (271.1 ± 105.6 MBq/nmol). Additionally, the in vitro and in vivo properties of the product were assessed on glioblastoma cells and mouse model. Although developed for the preparation of 68Ga-FAPI-46 for preclinical use, our method can be adapted for clinical production as a reliable alternative to the manual (i.e., cold kit) or modular systems preparations already described in the literature.
Highlights
The membrane-associated protease fibroblast activation protein (FAP) is upregulated in the stroma of a large variety of cancers [1,2] and in inflammatory conditions such as liver cirrhosis and both cardiovascular and rheumatoid diseases [3,4]
Our study provides a detailed fully automated procedure for the production of 68GaFAPI-46 on the extensively used commercial cassette-based synthesis platform Trasis AllinOne (AiO)
fibroblast activation protein inhibitors (FAPI)-46 was added to the 68Ga solution (350–900 MBq, ca. 1 M HCl (1 mL))
Summary
The membrane-associated protease fibroblast activation protein (FAP) is upregulated in the stroma of a large variety of cancers [1,2] and in inflammatory conditions such as liver cirrhosis and both cardiovascular and rheumatoid diseases [3,4]. FAP overexpression is associated with high tumor stage/grade, lymph node invasion, recurrence and reduced patient survival [5]. Amongst the molecules developed to inhibit FAP for therapeutic purposes, a group of quinoline-based compounds showed great potential [7]. Due to 68Ga-FAPI-46 s high lesion uptake, rapid body clearance and low accumulation in normal tissues, this agent has been investigated in a large number of patients with different tumor entities and non-malignant diseases [9]
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