Biodistribution and Dosimetry of 18 F-Meta-Fluorobenzylguanidine: A First-in-Human PET/CT Imaging Study of Patients with Neuroendocrine Malignancies
Open accessAbstract
123I-meta-iodobenzylguanidine (123I-MIBG) imaging is currently a mainstay in the evaluation of many neuroendocrine tumors, especially neuroblastoma. 123I-MIBG imaging has several limitations that can be overcome by the use of a PET agent. 18F-meta-fluorobenzylguanidine (18F-MFBG) is a PET analog of MIBG that may allow for single-day, high-resolution quantitative imaging. We conducted a first-in-human study of 18F-MFBG PET imaging to evaluate the safety, feasibility, pharmacokinetics, and dosimetry of 18F-MFBG in neuroendocrine tumors (NETs). Methods: Ten patients (5 with neuroblastoma and 5 with paraganglioma/pheochromocytoma) received 148–444 MBq (4–12mCi) of 18F-MFBG intravenously followed by serial whole-body imaging at 0.5–1, 1–2, and 3–4 after injection. Serial blood samples (a total of 6) were also obtained starting at 5 min after injection to as late as 4 h after injection; whole-body distribution and blood clearance data, lesion uptake, and normal-tissue uptake were determined, and radiation-absorbed doses to normal organs were calculated using OLINDA. Results: No side effects were seen in any patient after 18F-MFBG injection. Tracer distribution showed prominent activity in the blood pool, liver, and salivary glands that decreased with time. Mild uptake was seen in the kidneys and spleen, which also decreased with time. Urinary excretion was prominent, with an average of 45% of the administered activity in the bladder by 1 h after injection; whole-body clearance was monoexponential, with a mean biologic half-life of 1.95 h, whereas blood clearance was biexponential, with a mean biologic half-life of 0.3 h (58%) for the rapid α phase and 6.1 h (42%) for the slower β phase. The urinary bladder received the highest radiation dose with a mean absorbed dose of 0.186 ± 0.195 mGy/MBq. The mean total-body dose was 0.011 ± 0.011 mGy/MBq, and the effective dose was 0.023 ± 0.012 mSv/MBq. Both skeletal and soft-tissue lesions were visualized with high contrast. The SUVmax (mean ± SD ) of lesions at 1–2 h after injection was 8.6 ± 9.6. Conclusion: Preliminary data show that 18F-MFBG imaging is safe and has favorable biodistribution and kinetics with good targeting of lesions. PET imaging with 18F-MFBG allows for same-day imaging of NETs. 18F-MFBG appears highly promising for imaging of patients with NETs, especially children with neuroblastoma.
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18F-MFBG preliminary data report high accuracy and favorable dosimetry in a single-day protocol overcoming some limitations of other tracers.
“Recently an 18F-labeled analog of MIBG has been developed, meta-fluorobenzylguanidine (18F-MFBG); preliminary data report high accuracy and favorable dosimetry in a single-day protocol overcoming some of the limitations of other tracers and showing promise for the future (374).”
From Adrenal incidentaloma (2020) · cites this paper as [374]
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Sherlock, M., Scarsbrook, A., Abbas, A., Fraser, S., Limumpornpetch, P., Dineen, R., & Stewart, P. M. (2020) · Endocrine Reviews · doi:10.1210/endrev/bnaa008 · Cited by 347 · see citing works
“Recently an (18)F-labeled analog of MIBG has been developed, meta-fluorobenzylguanidine ((18)F-MFBG); preliminary data report high accuracy and favorable dosimetry in a single-day protocol overcoming some of the limitations of other tracers and showing promise for the future (374).”
Background
- Authors
- Pandit-Taskar, N., Zanzonico, P., Staton, K. D., Carrasquillo, J. A., Reidy-Lagunes, D., Lyashchenko, S., Burnazi, E., Zhang, H., Lewis, J. S., Blasberg, R., Larson, S. M., Weber, W. A., & Modak, S.
- Affiliations
- Memorial Sloan Kettering Cancer Center (US)
- ORCID
- Venue
- Journal of Nuclear Medicine
- Publisher
- Society of Nuclear Medicine
- Published
- 2017-07-13
- Volume
- 59
- Issue
- 1
- Pages
- 147-153
- ISSN
- 0161-5505 (ISSN-L)
- 2159-662X
- PMC
- PMC5750519
- OpenAlex
- W2735652803
- Cited by
- 136
- References
- 23
- Citations by year
- 2026: 15 · 2025: 19 · 2024: 9 · 2023: 18 · 2022: 22 · 2021: 13 · 2020: 16 · 2019: 13 · 2018: 10 · 2017: 1
- FWCI
- 8.40
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Journal of Nuclear Medicine (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- mediaTUM (Technical University of Munich) (submittedVersion)
- Funders
- National Cancer Institute (R01CA204093, P30CA008748)
- Topics
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Health Sciences › Medicine › Epidemiology › Neuroendocrine Tumor Research Advances
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Medical Imaging Techniques and Applications
- Keywords
- neuroendocrine tumors, neuroblastoma, paraganglioma, pheochromocytoma, tissue distribution, dosimetry, pharmacokinetics, body clearance, first-in-human imaging
- MeSH terms
- Positron Emission Tomography Computed Tomography, Adolescent, Child, Female, Humans, Kinetics, Male, Radiometry, Tissue Distribution, Neuroendocrine Tumors, 3-Iodobenzylguanidine, Young Adult
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