Fully automated radiolabeling of [
PET imaging
[68Ga]Ga-EMP100
[68Ga]Ga-radiopharmaceuticals
c-MET
Journal
EJNMMI radiopharmacy and chemistry
ISSN: 2365-421X
Titre abrégé: EJNMMI Radiopharm Chem
Pays: England
ID NLM: 101714628
Informations de publication
Date de publication:
16 Oct 2023
16 Oct 2023
Historique:
received:
18
08
2023
accepted:
03
10
2023
medline:
16
10
2023
pubmed:
16
10
2023
entrez:
16
10
2023
Statut:
epublish
Résumé
c-MET is a transmembrane receptor involved in many biological processes and contributes to cell proliferation and migration during cancer invasion process. Its expression is measured by immunehistochemistry on tissue biopsy in clinic, although this technique has its limitations. PET-CT could allow in vivo mapping of lesions expressing c-MET, providing whole-body detection. A number of radiopharmaceuticals are under development for this purpose but are not yet in routine clinical use. EMP100 is a cyclic oligopeptide bound to a DOTA chelator, with nanomolar affinity for c-MET. The aim of this project was to develop an automated method for radiolabelling the radiopharmaceutical [ The main results showed an optimal pH range between 3.25 and 3.75 for the complexation reaction and a stabilisation of the temperature at 90 °C, resulting in an almost complete incorporation of gallium-68 after 10 min of heating. In these experiments, 90 µg of EMP-100 peptide were initially used and then lower amounts (30, 50, 75 µg) were explored to determine the minimum required for sufficient synthesis yield. Radiolysis impurities were identified by radio-HPLC and ascorbic acid and ethanol were used to improve the purity of the compound. Three batches of [ For the automated synthesis of [
Sections du résumé
BACKGROUND
BACKGROUND
c-MET is a transmembrane receptor involved in many biological processes and contributes to cell proliferation and migration during cancer invasion process. Its expression is measured by immunehistochemistry on tissue biopsy in clinic, although this technique has its limitations. PET-CT could allow in vivo mapping of lesions expressing c-MET, providing whole-body detection. A number of radiopharmaceuticals are under development for this purpose but are not yet in routine clinical use. EMP100 is a cyclic oligopeptide bound to a DOTA chelator, with nanomolar affinity for c-MET. The aim of this project was to develop an automated method for radiolabelling the radiopharmaceutical [
RESULTS
RESULTS
The main results showed an optimal pH range between 3.25 and 3.75 for the complexation reaction and a stabilisation of the temperature at 90 °C, resulting in an almost complete incorporation of gallium-68 after 10 min of heating. In these experiments, 90 µg of EMP-100 peptide were initially used and then lower amounts (30, 50, 75 µg) were explored to determine the minimum required for sufficient synthesis yield. Radiolysis impurities were identified by radio-HPLC and ascorbic acid and ethanol were used to improve the purity of the compound. Three batches of [
CONCLUSIONS
CONCLUSIONS
For the automated synthesis of [
Identifiants
pubmed: 37843660
doi: 10.1186/s41181-023-00213-3
pii: 10.1186/s41181-023-00213-3
pmc: PMC10579204
doi:
Types de publication
Journal Article
Langues
eng
Pagination
30Informations de copyright
© 2023. Springer Nature Switzerland AG.
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