3E5

3E5 is an experimental monoclonal antibody and the targeting component of a novel antibody-drug conjugate (ADC) designed for the treatment of hepatocellular carcinoma (HCC). It specifically binds to fibroblast growth factor receptor 4 (FGFR4), a receptor tyrosine kinase that is highly expressed in HCC and associated with poor clinical outcomes. In its ADC form, 3E5 is conjugated to sulfasalazine, a small molecule ferroptosis inducer, via a cathepsin B-cleavable GGFG linker. The mechanism of action involves the selective binding of the 3E5 antibody to FGFR4 on the surface of tumor cells, followed by receptor-mediated endocytosis. Once internalized, the linker is cleaved to release sulfasalazine, which inhibits the xC- cystine/glutamate antiporter (SLC7A11). This inhibition leads to the depletion of intracellular glutathione and the accumulation of iron-dependent lipid peroxides, ultimately triggering ferroptotic cell death.

Other names

anti-FGFR4 antibody 3E5anti-FGFR-4 antibody 3E5anti-FGFR 4 antibody 3E53E5-GGFG-SSZ3E5-SSZ