Radiolabeled GRPR-Antagonists for Diagnostic Imaging and Treatment of GRPR-Positive Cancer
AssigneeAdvanced Accelerator Applications International SA
InventorsTheodosia Maina-Nock, Berthold Artur Nock, Marion de Jong Hendriks
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Abstract
The present invention relates to probes for use in the detection, imaging, diagnosis, targeting, treatment, etc. of cancers expressing the gastrin releasing peptide receptor (GRPR). For example, such probes may be molecules conjugated to detectable labels which are preferably moieties suitable for detection by gamma imaging and SPECT or by positron emission tomography (PET) or magnetic resonance imaging (MRI) or fluorescence spectroscopy or optical imaging methods.
Claims13
1-19. (canceled)
A radiolabeled GRPR-antagonist of the general formula MC-S-P wherein:
- M is a radiometal and C is a metal chelator that stably binds M,
- S is a spacer covalently linked between C and P of the following formula,
- wherein S is covalently attached to the N-terminus of P;
- and P is DPhe-Gln-Trp-Ala-Val-Gly-His-NH—CH[CH2—CH(CH3)2]2 (SEQ ID NO:
- 1);
- wherein M is 177Lu,
- wherein the metal chelator C is DOTA.
A radiolabeled GRPR-antagonist of the following formula:
A radiolabeled GRPR-antagonist of the following formula:
Dependencies are inferred from the claim text.