Saturday, 30 January 2016

Fresolimumab


Fresolimumab
GC 1008, GC1008
UNII-375142VBIA
cas 948564-73-6
Structure
  • immunoglobulin G4, anti-(human transforming growth factors beta-1, beta-2 (G-TSF or cetermin) and beta-3), human monoclonal GC-1008 γ4 heavy chain (134-215′)-disulfide with human monoclonal GC-1008 κ light chain, dimer (226-226”:229-229”)-bisdisulfide
  • immunoglobulin G4, anti-(transforming growth factor β) (human monoclonal GC-1008 heavy chain), disulfide with human monoclonal GC-1008 light chain, dimer
For Idiopathic Pulmonary Fibrosis, Focal Segmental Glomerulosclerosis,and Cancer
An anti-TGF-beta antibody in phase I clinical trials (2011) for treatment-resistant primary focal segmental glomerulosclerosis.
A pan-specific, recombinant, fully human monoclonal antibody directed against human transforming growth factor (TGF) -beta 1, 2 and 3 with potential antineoplastic activity. Fresolimumab binds to and inhibits the activity of all isoforms of TGF-beta, which may result in the inhibition of tumor cell growth, angiogenesis, and migration. TGF-beta, a cytokine often over-expressed in various malignancies, may play an important role in promoting the growth, progression, and migration of tumor cells.


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 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]
http://ryo1m.cocolog-nifty.com/photos/uncategorized/2014/05/13/igan_cjasn02.jpg


References


1 WHO Drug Information
2 National Cancer Institute: Fresolimumab


Fresolimumab
Monoclonal antibody
Type Whole antibody
Source Human
Target TGF beta 1, 2 and 3
Clinical data
Legal status
  • Investigational
Identifiers
CAS Number 948564-73-6 
ATC code None
ChemSpider none
KEGG D09620 Yes
Chemical data
Formula C6392H9926N1698O2026S44
Molar mass 144.4 kDa
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