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An Automated Radiosynthesis of [68Ga]Ga-FAPI-46 for Routine Clinical Use
Published on: May 24, 2024
FAPI PET: Fibroblast Activation Protein Inhibitor Use in Oncologic and Nononcologic Disease
Yuriko Mori1, Katharina Dendl1, Jens Cardinale1
1From the Department of Nuclear Medicine, Medical Faculty of Heinrich Heine University, University Hospital Düsseldorf, Düsseldorf, Germany (Y.M., K.D., J.C., F.L.G.); Department of Nuclear Medicine, University Hospital Heidelberg, Im Neuenheimer Feld 400, 69120 Heidelberg, Germany (K.D., J.C., C.K., F.L.G., U.H.); and Clinical Cooperation Unit Nuclear Medicine, German Cancer Research Center (DKFZ), Heidelberg, Germany (F.L.G., U.H.).
Abstract:
Gallium 68 (68Ga)-labeled fibroblast activation protein (FAP) inhibitor (FAPI) PET is based on the molecular targeting of the FAP, which is known to be highly expressed in the major cell population in tumor stroma, termed cancer-associated fibroblasts. Among many FAP-targeted radiopharmaceuticals developed so far, 68Ga-FAPI exhibits rapid tracer accumulation in target lesions and low background signal, which results in excellent imaging features. FAPI PET can be integrated in the clinical workflow and enables the detection of small primary or metastatic lesions, especially in the brain, liver, pancreas, and gastrointestinal tract due to the low tracer accumulation in these organs. Moreover, the DOTA (1,4,7,10-tetraazacylclododecane-1,4,7,10-tetrayl tetraacetic acid) chelator in the molecular structure allows coupling of the FAPI molecules with therapeutic emitters such as yttrium 90 for theranostic applications. This review provides an overview of the state of the art in FAP imaging, summarizes the current knowledge of relevant cancer biology, and highlights the latest findings in the clinical use of 68Ga-FAPI PET and other current FAPI tracers. Published under a CC BY 4.0 license.
Insights
Gallium 68 (68Ga)-labeled fibroblast activation protein (FAP) inhibitor (FAPI) PET offers excellent imaging for detecting small lesions. This FAP imaging technique shows promise for early cancer diagnosis and potential theranostic applications.
Area of Science:
- Nuclear Medicine
- Oncology
- Radiopharmaceutical Chemistry
Background:
- Fibroblast Activation Protein (FAP) is highly expressed in cancer-associated fibroblasts within tumor stroma.
- 68Ga-labeled FAP inhibitors (FAPI) target FAP for molecular imaging.
- 68Ga-FAPI PET demonstrates rapid tracer uptake and low background, yielding superior imaging characteristics.
Purpose of the Study:
- To review the current state of FAP imaging.
- To summarize cancer biology relevant to FAP targeting.
- To highlight recent clinical findings on 68Ga-FAPI PET and other FAPI tracers.
Main Methods:
- Review of existing literature on FAP imaging and cancer biology.
- Analysis of clinical data regarding the efficacy of 68Ga-FAPI PET.
- Discussion of radiopharmaceutical development for FAP targeting.
Main Results:
- 68Ga-FAPI PET enables detection of small primary and metastatic lesions, particularly in the brain, liver, pancreas, and gastrointestinal tract.
- The DOTA chelator facilitates theranostic applications by enabling coupling with therapeutic radioisotopes like yttrium 90.
- FAPI PET integrates well into clinical workflows, offering excellent imaging features.
Conclusions:
- 68Ga-FAPI PET is a valuable tool for cancer imaging due to its high specificity and sensitivity.
- The theranostic potential of FAPI tracers opens new avenues for personalized cancer treatment.
- Continued research into FAP-targeted radiopharmaceuticals is crucial for advancing cancer diagnostics and therapeutics.
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