fibatuzumab   Click here for help

GtoPdb Ligand ID: 8925

Synonyms: KB-004 | KB004
Compound class: Antibody
Comment: Fibatuzumab is a humanised monoclonal antibody directed against the ephrin receptor A3 (EPHA3) [6], which is a receptor tyrosine kinase implicated in mediating nervous system development [2,7-8].
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
BLAST searches of patented peptide sequences using the variable domains of the light and heavy chain sequences of fibatuzumab reveal exact matches with sequences submitted with patent US8664365 B2 [6].
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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
A single Phase 1/II clinical trial evaluating fibatuzumab in patients with EPHA3-expressing hematologic malignancies (NCT01211691) has suspended patient recruitment, and the ClinicalTrials.gov record carries a note that the trial sponsor will be winding down operations.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Although EPHA3 is primarily involved in cell positioning during fetal development, in adults it acts as an oncogenic antigen, that is re-expressed in hematologic malignancies [3-4] and solid tumors [1,5,9]. EPHA3 is also upregulated in diseases characterized by abnormal proliferation and fibrosis, such as idiopathic pulmonary fibrosis and diabetic kidney disease. Fibatuzumab's interaction with EpPHA3 may have more than one possible molecular mechanism of action, including inducing direct apoptosis in tumor cells, activation of antibody-dependent cell-mediated cytotoxicity (ADCC) and disruption of tumor vasculature.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01211691 Study of KB004 in Subjects With Hematologic Malignancies (Myelodysplastic Syndrome, MDS, Myelofibrosis, MF) Phase 1/Phase 2 Interventional Humanigen, Inc.