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BCG040 is a first-in-class, fully human IgG1κ biparatopic antibody-drug conjugate (ADC) targeting B7-H4 (VTCN1), developed by Biocytogen. The molecule features a biparatopic antibody that binds to two non-overlapping epitopes of B7-H4, which promotes receptor clustering and accelerated intracellular trafficking for enhanced payload delivery. It is conjugated to BCPT02, a potent topoisomerase I (TOP1) inhibitor, via a hydrophilic protease-cleavable linker with a drug-to-antibody ratio (DAR) of approximately 8. In preclinical studies, BCG040 has demonstrated superior efficacy and a favorable safety profile in models of ovarian, breast, biliary tract, and pancreatic cancers, outperforming several benchmark B7-H4 ADCs.
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