ArticleAmerican journal of nuclear medicine and molecular imaging2015
Dosimetry of [(177)Lu]-DO3A-VS-Cys(40)-Exendin-4 - impact on the feasibility of insulinoma internal radiotherapy.
Article in American journal of nuclear medicine and molecular imaging, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 29 citations in OpenAlex.
- Article
- Carrier systems of radiopharmaceuticals and the application in cancer therapy.Cell death discovery · 2024Review
- New Radiolabeled Exendin Analogues Show Reduced Renal Retention.Molecular pharmaceutics · 2023Article
- Peptide Radioligands in Cancer Theranostics: Agonists and Antagonists.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Role of Exendin-4 Functional Imaging in Diagnosis of Insulinoma: A Systematic Review.Life (Basel, Switzerland) · 2023Review
- Nuclear Medicine and Radiological Imaging of Pancreatic Neuroendocrine Neoplasms: A Multidisciplinary Update.Journal of clinical medicine · 2022Review
- Multivalent γ-PGA-Exendin-4 Conjugates to Target Pancreatic β-Cells.Chembiochem : a European journal of chemical biology · 2022Article
- Development and Validation of an Analytical HPLC Method to Assess Chemical and Radiochemical Purity of [Molecules (Basel, Switzerland) · 2022Article
- Role of PET/CT and Therapy Management of Pancreatic Neuroendocrine Tumors.Diagnostics (Basel, Switzerland) · 2020Review
- Beta Cell Imaging-From Pre-Clinical Validation to First in Man Testing.International journal of molecular sciences · 2020Review
- Advances in GLP-1 receptor targeting radiolabeled agent development and prospective of theranostics.Theranostics · 2020Review
- Increased Expression of GLP-1R in Proliferating Islets of Men1 Mice is Detectable by [Scientific reports · 2018Article
- Species differences in pancreatic binding of DO3A-VS-CysActa diabetologica · 2017Article
- Targets and probes for non-invasive imaging of β-cells.European journal of nuclear medicine and molecular imaging · 2017Review
- Current Status of Radiopharmaceuticals for the Theranostics of Neuroendocrine Neoplasms.Pharmaceuticals (Basel, Switzerland) · 2017Review
- Whole organ and islet of Langerhans dosimetry for calculation of absorbed doses resulting from imaging with radiolabeled exendin.Scientific reports · 2017Article
- Fully automated GMP production of [American journal of nuclear medicine and molecular imaging · 2017Article
- Quantification of β-Cell Mass in Intramuscular Islet Grafts Using Radiolabeled Exendin-4.Transplantation direct · 2016Article
- In vivo imaging of beta cells with radiotracers: state of the art, prospects and recommendations for development and use.Diabetologia · 2016Review
- Feasibility of Multiple Examinations Using (68)Ga-Labelled Collagelin Analogues: Organ Distribution in Rat for Extrapolation to Human Organ and Whole-Body Radiation Dosimetry.Pharmaceuticals (Basel, Switzerland) · 2016Article
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
[(68)Ga]-DO3A-VS-Cys(40)-Exendin-4 has been shown to be a promising imaging candidate for targeting glucagon like peptide-1 receptor (GLP-1R). In the light of radiotheranostics and personalized medicine the (177)Lu-labelled analogue is of paramount interest. In this study we have investigated the organ distribution of [(177)Lu]-DO3A-VS-Cys(40)-Exendin-4 in rat and calculated human dosimetry parameters in order to estimate the maximal acceptable administered radioactivity, and thus potential applicability of [(177)Lu]-DO3A-VS-Cys(40)-Exendin-4 for internal radiotherapy of insulinomas. Nine male and nine female Lewis rats were injected with [(177)Lu]-DO3A-VS-Cys(40)-Exendin-4 for ex vivo organ distribution study at nine time points. The estimation of human organ/total body absorbed and total effective doses was performed using Organ Level Internal Dose Assessment Code software (OLINDA/EXM 1.1). Six more rats (male: n = 3; female: n = 3) were scanned by single photon emission tomography and computed tomography (SPECT-CT). The renal function and potential cell dysfunction were monitored by creatinine ISTAT and glucose levels. The fine uptake structure of kidney and pancreas was investigated by ex vivo autoradiography. Blood clearance and washout from most of the organs was fast. The kidney was the dose-limiting organ with absorbed dose of 5.88 and 6.04 mGy/MBq, respectively for female and male. Pancreatic beta cells demonstrated radioactivity accumulation. Renal function and beta cell function remained unaffected by radiation. The absorbed dose of [(177)Lu]-DO3A-VS-Cys(40)-Exendin-4 to kidneys may limit the clinical application of the agent. However, hypothetically, kidney protection and peptidase inhibition may allow reduction of kidney absorbed dose and amplification of tumour absorbed doses.
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Identifiers
25973333PMC4396004W1577038563What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.