Teprotumumab

Teprotumumab
Monoclonal antibody
Type Whole antibody
Source Human
Target IGF-1R
Clinical data
ATC code
  • none
Identifiers
CAS Number
ChemSpider
  • none
UNII
KEGG
ECHA InfoCard 100.081.384 Edit this at Wikidata
Chemical and physical data
Formula C6476H10012N1748O2000S40
Molar mass 145.6 kg/mol
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Teprotumumab (RG-1507) is an experimental human monoclonal antibody developed by Genmab and Roche. It binds to IGF-1R.

Teprotumumab was first investigated for the treatment of solid and hematologic tumors, including breast cancer, Hodgkin's and non-Hodgkin's lymphoma, non-small cell lung cancer and sarcoma.[1][2] Although results of phase I and early phase II trials showed promise, research for these indications were discontinued in 2009 by Roche. Phase II trials still in progress were allowed to complete, as the development was halted due to business prioritization rather than safety concerns.

Teprotumumab was subsequently licensed to River Vision Development Corporation in 2012 for research in the treatment of ophthalmic conditions. Horizon Pharma acquired RVDC in 2017, and will continue clinical trials.[3] It is in phase II trials for Graves' ophthalmopathy and phase I for diabetic macular edema.[4] It was granted Orphan Drug Status by the FDA for Graves' ophthalmopathy.[5]

In a multicenter randomized trial in patients with active Graves' ophthalmopathy Teprotumumab was more effective than placebo in reducing the clinical activity score and proptosis.[6]

References

  1. ↑ https://clinicaltrials.gov/ct2/show/NCT01868997
  2. ↑ http://adisinsight.springer.com/drugs/800015801
  3. ↑ http://www.genmab.com/product-pipeline/products-in-development/teprotumumab
  4. ↑ http://adisinsight.springer.com/drugs/800015801
  5. ↑ http://www.genmab.com/product-pipeline/products-in-development/teprotumumab
  6. ↑ Smith, TJ; Kahaly, GJ; Ezra, DG; Fleming, JC; Dailey, RA; Tang, RA; Harris, GJ; Antonelli, A; Salvi, M; Goldberg, RA; Gigantelli, JW; Couch, SM; Shriver, EM; Hayek, BR; Hink, EM; Woodward, RM; Gabriel, K; Magni, G; Douglas, RS (4 May 2017). "Teprotumumab for Thyroid-Associated Ophthalmopathy". The New England Journal of Medicine. 376 (18): 1748–1761. doi:10.1056/NEJMoa1614949. PMC 5718164. PMID 28467880.


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