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.
Click here for help

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.

✖

View interactive charts of activity data across species
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
Insulin-like growth factor I receptor Primary target of this compound Hs Antibody Antagonist 9.3 – 12.2 pKd - 4
⤷ pKd 12.2 (Kd 6.95x10-13 M) [4]
Description: Dissociation constant for antibody 18; determined by SPR binding analysis using a Biacore assay.
pKd 9.3 (Kd 5.65x10-10 M) [4]
Description: Dissociation constant for antibody 22; determined by SPR binding analysis using a Biacore assay.