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hu5B1-TCO is a chemically modified, humanized monoclonal antibody targeting the tumor-associated carbohydrate antigen CA19-9. The antibody is conjugated with trans-cyclooctene (TCO), enabling it to participate in bioorthogonal "click chemistry" reactions for pretargeted imaging and therapy. In clinical studies, hu5B1-TCO is administered first to bind CA19-9–expressing tumor cells; after sufficient time for unbound antibody clearance, a radiolabeled tetrazine compound (such as 64Cu-Tz-SarAr) is injected and rapidly reacts with the TCO tag on the tumor-bound antibody via an in vivo click reaction. This approach allows highly specific PET imaging of CA19-9–positive cancers—primarily pancreatic cancer—by reducing background signal and improving detection sensitivity. The technology represents an innovative pretargeting strategy for both diagnostic imaging and potential future theranostic applications[3][6][8].
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