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LZU-WZLYFG001 is a novel FGFR3-targeted antibody-drug conjugate (ADC) designed for the treatment of bladder cancer. It comprises a humanized anti-FGFR3 IgG1 monoclonal antibody conjugated to the topoisomerase I inhibitor payload DXD (deruxtecan) via a cleavable GGFG linker, achieving a drug-to-antibody ratio (DAR) of eight. The mechanism of action involves the specific binding of the antibody to FGFR3-expressing tumor cells, followed by internalization and lysosomal cleavage of the linker to release the cytotoxic payload. Preclinical studies in bladder cancer cell lines, organoids, and patient-derived xenograft (PDX) models have demonstrated significant anti-tumor activity, including efficacy in models resistant to standard gemcitabine and cisplatin therapy, as well as a potent bystander effect.
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