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68Ga-NOTA-MAL-Cys39-exendin-4

Development stage: Phase 1
Lead developer: Nanjing First Hospital
Modality: Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Peptides
Administration: Intravenous

Overview

68Ga-NOTA-MAL-Cys39-exendin-4 is a radiolabeled peptide tracer designed for positron emission tomography (PET) imaging of glucagon-like peptide-1 receptor (GLP-1R) positive tumors, particularly insulinoma. The tracer consists of exendin-4, a GLP-1R agonist, conjugated with NOTA-MAL at the Cys39 position and radiolabeled with gallium-68. Upon administration, the exendin-4 moiety binds to GLP-1R, allowing detection of GLP-1R-expressing tissues using PET/CT imaging. In preclinical studies, it demonstrated high tumor uptake with good contrast to background, favorable biodistribution, and high affinity to islet tumor cells. The tracer shows potential for the detection and localization of insulinoma and other GLP-1R positive tumors.

Other names: Gallium-68 NOTA-MAL-Cys39-exendin-4Gallium68 NOTA-MAL-Cys39-exendin-4Gallium 68 NOTA-MAL-Cys39-exendin-4

Targets

GLP1R (GLP-1R)

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