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technetium Tc 99m demobesin-4
- Development stage
- Discontinued
- Lead developer
- Cancer Research UK
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
- Administration
- Intravenous
01
Overview
Technetium Tc 99m demobesin-4 is a diagnostic radiopharmaceutical designed for the molecular imaging of tumors that overexpress the gastrin-releasing peptide receptor (GRPR). The molecule is a bombesin-like peptide analogue, specifically an antagonist, which is conjugated to a tetraamine chelator (N4) for labeling with the radioisotope technetium-99m (99mTc). Unlike bombesin agonists, demobesin-4 does not trigger receptor internalization or agonist-induced side effects, but it exhibits high binding affinity and favorable pharmacokinetics for imaging. It was primarily developed for use with single-photon emission computed tomography (SPECT) to detect primary and metastatic prostate cancer. Clinical development was spearheaded by academic and non-profit institutions, including the National Center for Scientific Research Demokritos and Cancer Research UK.
- Other names
- technetium Tc 99m DB4^99mTc-demobesin-4^99mTc-DB4Technetium Tc 99m Demobesin-4
02
Targets
GRPR (Gastrin-releasing peptide receptor)
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