Fresolimumab

Monoclonal antibody
  • none
Legal statusLegal status
  • Investigational
IdentifiersCAS Number
  • 948564-73-6 ☒N
ChemSpider
  • none
UNII
  • 375142VBIA
KEGG
  • D09620 checkY
Chemical and physical dataFormulaC6392H9926N1698O2026S44Molar mass144388.22 g·mol−1 ☒NcheckY (what is this?)  (verify)

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).

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

References

  1. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN)" (PDF). WHO Drug Information. 23 (2). 2009.
  2. ^ a b "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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TGFβ receptor superfamily modulators
Type I
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