Automated Radiosynthesis of [
FAPI
cancer-associated fibroblast
fibroblast activation protein
radioflourination
Journal
Pharmaceuticals (Basel, Switzerland)
ISSN: 1424-8247
Titre abrégé: Pharmaceuticals (Basel)
Pays: Switzerland
ID NLM: 101238453
Informations de publication
Date de publication:
25 Jun 2024
25 Jun 2024
Historique:
received:
26
05
2024
revised:
17
06
2024
accepted:
20
06
2024
medline:
27
7
2024
pubmed:
27
7
2024
entrez:
27
7
2024
Statut:
epublish
Résumé
Cancer-associated fibroblasts have become a new target for therapy. Fibroblasts present within malignancies express the fibroblast activation protein (FAP). Inhibitors to FAP (FAPI) are small molecules recently developed as a theranostic agents for imaging and radiotherapy. All currently used FAPI rely on a linker-chelator complex attached to the 'inhibitor'. We describe a new automated method of the direct attachment of the radioisotope to the inhibitor, resulting in a >50% MW reduction with the hope of an improved tumor-to-background ratio and tumor uptake. [ The synthesis of the Sn precursor for FluorFAPI and the automated synthesis of [ With the successful development of an automated synthesis of [
Sections du résumé
BACKGROUND
BACKGROUND
Cancer-associated fibroblasts have become a new target for therapy. Fibroblasts present within malignancies express the fibroblast activation protein (FAP). Inhibitors to FAP (FAPI) are small molecules recently developed as a theranostic agents for imaging and radiotherapy. All currently used FAPI rely on a linker-chelator complex attached to the 'inhibitor'. We describe a new automated method of the direct attachment of the radioisotope to the inhibitor, resulting in a >50% MW reduction with the hope of an improved tumor-to-background ratio and tumor uptake.
METHODS
METHODS
[
RESULTS
RESULTS
The synthesis of the Sn precursor for FluorFAPI and the automated synthesis of [
CONCLUSIONS
CONCLUSIONS
With the successful development of an automated synthesis of [
Identifiants
pubmed: 39065684
pii: ph17070833
doi: 10.3390/ph17070833
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Neuroendocrine Tumor Research Foundation
ID : 2023 NETRF Investigator Award 23-PAF08146