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[68Ga]Ga-BCY18469 is a diagnostic radiopharmaceutical consisting of a phage display-derived bicyclic peptide (BCY18469) conjugated to the positron-emitting radioisotope Gallium-68 ([68Ga]). It is designed to target the Erythropoietin-producing hepatocellular receptor A2 (EphA2), a tyrosine kinase receptor that is frequently overexpressed in various solid malignancies, including pancreatic, lung, and breast cancers. The bicyclic peptide structure offers high binding affinity and specificity for EphA2, along with favorable proteolytic stability and rapid renal clearance, which facilitates high-contrast PET/CT imaging. Clinical data from first-in-human studies indicate that the tracer effectively visualizes primary tumors and metastatic lesions with low background uptake in the liver, supporting its development as a tool for patient stratification and tumor characterization in EphA2-positive cancers.
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