fibatuzumab   

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].
No information available.
Summary of Clinical Use
A single Phase I/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
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.