fresolimumab

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Ligands
fresolimumab

GtoPdb Ligand ID: 8264

Synonyms: GC1008 | PET1073G12 [1]

Comment: Fresolimumab is a monoclonal antibody targeting all isoforms of transforming growth factor beta (TGF-β1, -β2 and -β3.).
Annotated peptide sequence information for this antibody is available from its IMGT/mAb-DB link.
BLAST peptide sequence analysis reveals patent US7723486 as the covering document for fresolimumab [1].

No information available.

No information available.

Summary of Clinical Use
The EMA has granted fresolimumab orphan designation for the treatment of focal segmental glomerulosclerosis (FSG). Fresolimumab has reached Phase 2 clinical trial for glioma in addition to FSG. A phase 1 trial for diffuse systemic sclerosis has been completed. Unfortunately, inhibition of TGF-β1 (which exerts a potent cytostatic effect on premalignant cells) has been noted to induce squamous cell carcinoma development in Phase 1 clinical trial [3].

Summary of Clinical Use

The EMA has granted fresolimumab orphan designation for the treatment of focal segmental glomerulosclerosis (FSG).
Fresolimumab has reached Phase 2 clinical trial for glioma in addition to FSG. A phase 1 trial for diffuse systemic sclerosis has been completed.
Unfortunately, inhibition of TGF-β1 (which exerts a potent cytostatic effect on premalignant cells) has been noted to induce squamous cell carcinoma development in Phase 1 clinical trial [3].

Mechanism Of Action and Pharmacodynamic Effects
TGF-β is a key regulator of glomerular visceral epithelial cells which play a pivotal role in the pathogenesis of FSG [2]. Fresolimumab binds to all isoforms of TGF-β, effectively blocking TGF-β activity, thereby reducing the pathological tissue damage and scarring observed in FSG. In oncology, TGF-β is over-expressed in certain malignancies, playing an important role in facilitating growth, progression, and migration of tumour cells. By binding to and neutralising all isoforms of TGF-β, fresolimumab is expected to inhibit tumour cell growth, angiogenesis, and migration.

Mechanism Of Action and Pharmacodynamic Effects

TGF-β is a key regulator of glomerular visceral epithelial cells which play a pivotal role in the pathogenesis of FSG [2]. Fresolimumab binds to all isoforms of TGF-β, effectively blocking TGF-β activity, thereby reducing the pathological tissue damage and scarring observed in FSG.
In oncology, TGF-β is over-expressed in certain malignancies, playing an important role in facilitating growth, progression, and migration of tumour cells. By binding to and neutralising all isoforms of TGF-β, fresolimumab is expected to inhibit tumour cell growth, angiogenesis, and migration.