Drug intelligence / Profile preview

LY3076226

Development stage
Phase 1
Lead developer
Eli Lilly
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

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].

Other names
anti-FGFR3 antibody-drug conjugateanti-FGFR-3 antibody-drug conjugateanti-FGFR 3 antibody-drug conjugateanti-fibroblast growth factor receptor 3 antibody-drug conjugate
02

Targets

FGFR3 (Fibroblast growth factor receptor 3)TUBB (Tubulin (alpha and beta subunits))

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