Fresolimumab

Fresolimumab (GC1008) is a human monoclonal antibody[1] and an immunomodulator. It is intended for the treatment of idiopathic pulmonary fibrosis (IPF), focal segmental glomerulosclerosis, and cancer[2][3] (kidney cancer and melanoma).

Fresolimumab
Monoclonal antibody
TypeWhole antibody
SourceHuman
TargetTGF beta 1, 2 and 3
Clinical data
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC6392H9926N1698O2026S44
Molar mass144388.22 g·mol−1
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It binds to and inhibits all isoforms of the protein transforming growth factor beta (TGF-β).[2]

History

Fresolimumab was discovered by Cambridge Antibody Technology (CAT) scientists[4] and was one of a pair of candidate drugs that were identified for the treatment of the fatal condition scleroderma. CAT chose to co-develop the two drugs metelimumab (CAT-192) and fresolimumab with Genzyme. During early development, around 2004, CAT decided to drop development of metelimumab in favour of fresolimumab.[5]

In February 2011 Sanofi-Aventis agreed to buy Genzyme for US$20.1 billion.[6]

As of June 2011 the drug was being tested in humans (clinical trials) against IPF, renal disease, and cancer.[7][8] On 13 August 2012, Genzyme applied to begin a Phase 2 clinical trial in primary focal segmental glomerulosclerosis[9] comparing fresolimumab versus placebo.

As of July 2014, Sanofi-Aventis continue to list fresolimumab in their research and development portfolio under Phase II development.[10]

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References
  1. "International Nonproprietary Names for Pharmaceutical Substances (INN)" (PDF). WHO Drug Information. 23 (2). 2009.
  2. "Fresolimumab". NCI Drug Dictionary. National Cancer Institute.
  3. "Fresolimumab" (PDF). Statement on a Nonproprietary Name Adopted by the USAN Council.
  4. Grütter C, Wilkinson T, Turner R, Podichetty S, Finch D, McCourt M, et al. (December 2008). "A cytokine-neutralizing antibody as a structural mimetic of 2 receptor interactions". Proceedings of the National Academy of Sciences of the United States of America. 105 (51): 20251–6. Bibcode:2008PNAS..10520251G. doi:10.1073/pnas.0807200106. PMC 2600578. PMID 19073914.
  5. Foley S (10 February 2004). "CAT may abandon skin drug after trial results disappoint". The Independent. Archived from the original on 3 November 2012.
  6. "Sanofi-Aventis to buy Genzyme in search for new sales". BBC News. 16 February 2011.
  7. "Scientists Trigger White Fat to Become Brown Fat-Like to Treat Obesty and Type 2 Diabetes". Genetic Engineering & Biotechnology News. July 5, 2011.
  8. "Studies found for Fresolimumab". Clinicaltrials.gov.
  9. Clinical trial number NCT01665391 for "A Study of Fresolimumab in Patients With Steroid-Resistant Primary Focal Segmental Glomerulosclerosis (FSGS)" at ClinicalTrials.gov
  10. "R&D Portfolio". Sanofi. Archived from the original on 28 June 2014.
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