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
References
1. Chen H, Mester T, Raychaudhuri N, Kauh CY, Gupta S, Smith TJ, Douglas RS. (2014)
Teprotumumab, an IGF-1R blocking monoclonal antibody inhibits TSH and IGF-1 action in fibrocytes.
J Clin Endocrinol Metab, 99 (9): E1635-40. [PMID:24878056]
2. Douglas RS. (2019)
Teprotumumab, an insulin-like growth factor-1 receptor antagonist antibody, in the treatment of active thyroid eye disease: a focus on proptosis.
Eye (Lond.), 33 (2): 183-190. [PMID:30575804]
3. Feldon SE, Park DJ, O'Loughlin CW, Nguyen VT, Landskroner-Eiger S, Chang D, Thatcher TH, Phipps RP. (2005)
Autologous T-lymphocytes stimulate proliferation of orbital fibroblasts derived from patients with Graves' ophthalmopathy.
Invest Ophthalmol Vis Sci, 46 (11): 3913-21. [PMID:16249464]
4. Graus Y, Kopetzki E, Kuenkele K-P, Mundigl O, Parren P, Rebers F, Schumacher R, Van De Winkel J, Van Vugt M. (2005)
Antibodies against insulin-like growth factor i receptor and uses thereof.
Patent number: WO2005005635A2. Assignee: Hoffmann-La Roche Ag. Priority date: 10/07/2003. Publication date: 20/01/2005.
5. Huang HJ, Angelo LS, Rodon J, Sun M, Kuenkele KP, Parsons HA, Trent JC, Kurzrock R. (2011)
R1507, an anti-insulin-like growth factor-1 receptor (IGF-1R) antibody, and EWS/FLI-1 siRNA in Ewing's sarcoma: convergence at the IGF/IGFR/Akt axis.
PLoS ONE, 6 (10): e26060. [PMID:22022506]
6. Huang Y, Fang S, Li D, Zhou H, Li B, Fan X. (2019)
The involvement of T cell pathogenesis in thyroid-associated ophthalmopathy.
Eye (Lond.), 33 (2): 176-182. [PMID:30531993]
7. Kurzrock R, Patnaik A, Aisner J, Warren T, Leong S, Benjamin R, Eckhardt SG, Eid JE, Greig G, Habben K et al.. (2010)
A phase I study of weekly R1507, a human monoclonal antibody insulin-like growth factor-I receptor antagonist, in patients with advanced solid tumors.
Clin Cancer Res, 16 (8): 2458-65. [PMID:20371689]
8. Mahadevan D, Sutton GR, Arteta-Bulos R, Bowden CJ, Miller PJ, Swart RE, Walker MS, Haluska P, Munster PN, Marshall J et al.. (2014)
Phase 1b study of safety, tolerability and efficacy of R1507, a monoclonal antibody to IGF-1R in combination with multiple standard oncology regimens in patients with advanced solid malignancies.
Cancer Chemother Pharmacol, 73 (3): 467-73. [PMID:24390424]
9. Qu X, Wu Z, Dong W, Zhang T, Wang L, Pang Z, Ma W, Du J. (2017)
Update of IGF-1 receptor inhibitor (ganitumab, dalotuzumab, cixutumumab, teprotumumab and figitumumab) effects on cancer therapy.
Oncotarget, 8 (17): 29501-29518. [PMID:28427155]
10. Ramalingam SS, Spigel DR, Chen D, Steins MB, Engelman JA, Schneider CP, Novello S, Eberhardt WE, Crino L, Habben K et al.. (2011)
Randomized phase II study of erlotinib in combination with placebo or R1507, a monoclonal antibody to insulin-like growth factor-1 receptor, for advanced-stage non-small-cell lung cancer.
J Clin Oncol, 29 (34): 4574-80. [PMID:22025157]