emibetuzumab   Click here for help

GtoPdb Ligand ID: 7748

Synonyms: LA480 | LY-2875358 | LY2875358
Compound class: Antibody
Comment: Emibetuzumab is an investigatonal monoclonal antibody designed as a potential treatment for advanced or metastatic solid tumors.
Peptide sequence information for this antibody is available from its IMGT/mAb-DB record.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
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Summary of Clinical Use Click here for help
Emibetuzumab, under its research code LY2875358, is being assessed in various clinical trials for cancers including advanced gastric adenocarcinoma and non-small-cell lung cancer. Click here to link to ClinicalTrials.gov's list of registered LY2875358 trials.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Emibetuzumab blocks the receptor for hepatocyte growth factor (HGF), which is the receptor tyrosine kinase MET, without causing any agonist-like activation of the receptor. In tumour cells MET can be activated by ligand-dependent or ligand-independent (eg receptor dimerisation in MET over-expressing tumours) mechanisms, both of which result in activation of downstream signalling pathways known to be involved in tumor cell proliferation and resistance [2,4-5]. Emibetuzumab blocks this signalling cascade [3].
The antibody's developer, Eli Lilly has produced a mechanism of action video for emibetuzumab, which you can access here.