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LY3076226 is an investigational antibody-drug conjugate (ADC) developed by Eli Lilly. It consists of a human IgG1 monoclonal antibody targeting fibroblast growth factor receptor 3 (FGFR3), conjugated via a cleavable linker to the cytotoxic agent DM4, a maytansine derivative that inhibits tubulin dynamics. The ADC selectively binds to both wild-type and mutant forms of FGFR3, including TACC3 fusion proteins, leading to internalization and targeted delivery of the cytotoxin into cancer cells with aberrant FGFR3 activation. This results in inhibition of cell division and induction of apoptosis in tumor cells. LY3076226 has been evaluated in phase I clinical trials for advanced or metastatic cancers, including urothelial carcinoma with FGFR3 alterations[1][2][4][5][6].
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