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![Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F68356.jpg&w=3840&q=50)
Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
Published on: April 25, 2025
A novel (68)Ga-labeled pteroic acid-based pet tracer for tumor imaging via the folate receptor
Berit Kühle1, Cristina Müller, Tobias L Ross
1Johannes Gutenberg-University, Mainz, Germany. kuehle@uni-mainz.de
Abstract:
The folate receptor (FR) is a very attractive target in oncological imaging as it is overexpressed by a variety of cancer types, whereas the expression in healthy tissue is very limited. The synthesis of regioisomeric pure folic acid derivatives normally requires a regioselective approach and does not allow the use of native folic acid (FA). As the pharmacophore of FA is assumed to be pteroic acid, its use without the glutamic acid moiety may enable the possibility to considerably simplify the synthesis of a positron emission tomography (PET) tracer for FR imaging. In this work, DO3A-EA-Pte was successfully synthesized and labeled with (68)Ga. It is stable for up to 3 h in PBS and against transchelation by transferrin. It also displays a lipophilicity that allows the assumption that it will show favorable in vivo characteristics for FR imaging via PET.
Insights
Researchers developed a new positron emission tomography (PET) tracer for folate receptor (FR) imaging by simplifying folic acid (FA) structure. This novel tracer shows stability and favorable characteristics for cancer imaging.
Area of Science:
- Oncological imaging
- Radiopharmaceutical chemistry
- Molecular imaging
Background:
- Folate receptor (FR) is overexpressed in many cancers, making it an attractive target for oncological imaging.
- Current folate-derived tracers require complex synthesis, limiting the use of native folic acid (FA).
Purpose of the Study:
- To simplify the synthesis of a positron emission tomography (PET) tracer for FR imaging.
- To evaluate a novel tracer based on pteroic acid (Pte) for FR-targeted PET imaging.
Main Methods:
- Synthesis of DO3A-EA-Pte, a simplified folic acid derivative.
- Radiolabeling of the tracer with Gallium-68 ((68)Ga).
- Assessment of tracer stability in phosphate-buffered saline (PBS) and against transchelation by transferrin.
Main Results:
- Successful synthesis and (68)Ga labeling of DO3A-EA-Pte.
- The tracer demonstrated stability in PBS for up to 3 hours.
- The tracer exhibited stability against transchelation by transferrin.
- The tracer's lipophilicity suggests favorable in vivo characteristics for FR imaging.
Conclusions:
- DO3A-EA-Pte is a stable and potentially effective (68)Ga-labeled PET tracer for FR-targeted imaging.
- Simplifying the FA structure to pteroic acid facilitates tracer synthesis.
- This approach holds promise for improved FR-based cancer imaging via PET.
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