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Drug intelligence / Profile preview
flotegatide (18F) + RGD (68Ga)
- Development stage
- Discontinued
- Lead developer
- Siemens Healthineers
- Modality
- Positron Emitters → Radiopharmaceuticals, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
- Administration
- Intravenous
01
Overview
A combination of two radiolabeled RGD peptides used for PET imaging of integrin αvβ3 expression. Flotegatide (18F) was developed by GE Healthcare with a core peptide sequence of ACDRGDCFCG, optimized through cyclization and introduction of two disulfide bonds. It shows highest binding affinity for integrin αvβ5 (IC50 0.1 nM), followed by integrin αvβ3 (IC50 11.1 nM). The 68Ga-labeled RGD peptides have similar dosimetry profiles but shorter physical half-life compared to 18F-labeled counterparts.
- Other names
- RGD F18Flotegatide F18RGD-F18RGD-F-18RGD-F 18
02
Targets
αVβ3 (Integrin αVβ3)αVβ5 (Integrin αVβ5)
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