tarextumab   Click here for help

GtoPdb Ligand ID: 8453

Synonyms: OMP-59R5
Compound class: Antibody
Comment: Tarextumab is fully human IgG2 monoclonal antibody targeting Notch receptors 2 and 3.
Peptide sequence information for this antibody is available from its IMGT/mAb-DB record. A BLAST search using the peptide sequence of the variable region of the heavy chain of tarextumab reveals 100% match with sequences patented in US8226943 B2 [1].
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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
Tarextumab (OMP-59R5) was progressed to clinical trial for a selection of advanced solid tumours. In January 2015 the US FDA granted tarextumab orphan drug designation for the treatment of pancreatic cancer and small cell lung cancer. However, development appears to have been discontinued, likely due to a failure to show efficacy.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Tarextumab binds to Notch 2 and Notch 3 receptors, thereby prevenitng activation of the Notch signalling pathway. Notch pathway inhibition has anti-cancer effects.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01277146 A Dose Escalation Study of OMP-59R5 in Subjects With Solid Tumors Phase 1 Interventional Mereo BioPharma 3
NCT00001693 Phase I-II Multiple-Dose Safety and Efficacy Study of a Selective Inhibitor of Cyclooxygenase - 2 (SC-58635) in Hereditary Non-Polyposis Colorectal Cancer (HNPCC) Patients and Carriers Phase 1 Interventional National Institutes of Health Clinical Center (CC) 2