teprotumumab   Click here for help

GtoPdb Ligand ID: 10612

Synonyms: R1507 | RG-1507 | RG1507 | RV 001 | RV-001 | Tepezza® | teprotumumab-trbw
Approved drug Immunopharmacology Ligand
teprotumumab is an approved drug (FDA (2020))
Compound class: Antibody
Comment: Teprotumumab is a fully human anti-insulin-like growth factor 1 receptor (IGF-1R) monoclonal antibody (antagonist) [2] that was originally developed in a collaboration between Genmab and Roche, and later licensed to Horizon Therapeutics who completed its advancement through clinical trials in thyroid eye disease. Heavy and light chain variable region peptide sequences for teprotumumab are 100% matches for SEQ IDs 1 and 2 (respectively) that are claimed in Hoffmann-La Roche patent WO2005005635A2 [4]. This patent claims two preferred antibodies, antibody 18 and antibody 22, but it is not clear which contains SEQ IDs 1 and 2.
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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
Teprotumumab (RG-1507) received FDA orphan drug designation in 2013 for the treatment of active thyroid eye disease (i.e. proptosis resulting from Graves' disease; Graves' ophthalmopathy). Following expedited review via the FDA Fast Track and Priority Review processes teprotumumab (Tepezza®) was granted full FDA approval in January 2020 for Graves' ophthalmopathy. A single Phase 1 trial in diabetic macular edema has been completed.
Prior to investigations for opthalmic diseases, RG-1507 was evaluated for oncology potential in a range of solid tumour types but did not advance beyond Phase 2 [5,7-10].