Drug intelligence / Profile preview

68Ga-BNOTA-PRGD2

Development stage
Phase 1
Lead developer
Peking Union Medical College Hospital
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration
Intravenous
01

Overview

68Ga-BNOTA-PRGD2 is a radiopharmaceutical agent used as a positron emission tomography (PET) imaging tracer. It consists of the cyclic RGD peptide motif conjugated to the chelator BNOTA and labeled with the radioisotope gallium-68. After intravenous administration, it binds specifically to integrin alphaVbeta3 (αvβ3) on cell membranes via its RGD motif. Integrin αvβ3 is highly expressed in angiogenic blood vessels and certain tumor cells. This makes 68Ga-BNOTA-PRGD2 useful for non-invasive imaging of angiogenesis in cancer and other diseases characterized by neovascularization or inflammation. The agent is primarily excreted through the urinary system and has an acceptable radiation dosimetry profile for clinical use[1][5][10]. Clinical studies have demonstrated its utility in diagnosing lung cancer—where it shows high specificity for lymph node metastasis compared to standard FDG PET/CT—and glioma grading[8][10]. It has also been investigated for imaging rheumatoid arthritis due to its ability to visualize synovial angiogenesis[6].

Brand names
68Ga-Alfatide II
Other names
gallium Ga 68-labeled BNOTA-PRGD2gallium Ga 68-NOTA-RGDNOTA-PEG4-E[c(RGDfK)]2
02

Targets

αVβ3 (Integrin αVβ3)

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