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68Ga-BBN-RGD is a radiopharmaceutical agent designed for positron emission tomography (PET) imaging. It is a heterodimeric peptide that combines bombesin(7–14) (BBN), which targets the gastrin-releasing peptide receptor (GRPR), and a cyclic RGD peptide that targets integrin αvβ3. Both GRPR and integrin αvβ3 are overexpressed in various tumors, including prostate cancer and gliomas. The dual-receptor targeting approach aims to improve tumor detection sensitivity by binding to both receptors simultaneously. The compound is labeled with the radioisotope gallium-68 for PET imaging applications[4][6][8]. Preclinical and early clinical studies have demonstrated its safety, favorable pharmacokinetics, rapid renal clearance, and high uptake in GRPR/integrin-positive tumors[6][8]. Its primary indication under investigation is for the diagnosis and staging of cancers such as prostate cancer.
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