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BAY86-4367 (riciguanine) is a synthetic, directly F-18 labeled bombesin analog with antagonistic properties that targets gastrin-releasing peptide receptors (GRPr). It was developed as a positron emission tomography (PET) imaging agent for the detection and localization of prostate cancer. The compound demonstrates high binding affinity and selectivity for GRPr, which are overexpressed in certain cancers such as prostate cancer. Preclinical studies showed specific and effective tumor targeting in xenograft models, rapid tumor uptake, fast renal excretion, and favorable safety profiles. In early clinical evaluation for primary and recurrent prostate cancer patients, BAY86-4367 was well tolerated but showed limited sensitivity in detecting recurrent disease compared to other tracers[2][3][4][5][7].
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