RO5083945 (or GA201, RG7160) is the first glycosylation-modified monoclonal antibody (mAb) directed against the epidermal growth factor receptor (EGFR) for the treatment of cancer and autoimmune diseases. RO5083945 has a fully human glycosylation pattern and is optimized for glycosylation in its Fc domain to promote antibody-dependent cell-mediated cytotoxicity (ADCC). EGFR is overexpressed on the cell surface in a variety of tumor types and acts under several anti-tumor mechanisms: strong ADCC, inhibition of proliferation by receptor blockade, and induction of apoptosis. A clinical phase I dose escalation study involving RO5083945 is ongoing to investigate the efficacy of this antibody in the treatment of solid tumors, including KRAS mutant CRC.
RO5083945 is derived by glycosylation of the parental cetuximab. The glycosylation process used to develop this agent is achieved by altering the glycosylation profile in the Fc region of the mAb molecule, resulting in a significant enhancement of immunogenicity and thus, a stronger ADCC response.
Fig.1 Site-specific glycoengineering of cetuximab for enhanced ADCC activity.
Glyco-engineered RO5083945 is thought to have therapeutic activity against EGFR-positive tumors because of:
Fig.2 Mechanism of action of RO5083945.
|NCT ID||Status||Conditions||Lead Sponsor||Phase||Update Time|
|NCT00721266||Completed||Neoplasms||Glycotope GmbH||Phase 1||November 2, 2016|
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Creative Biolabs provides luciferase-based ADCC assay. This Jurkat cell based assay is pioneered by Creative Biolabs, and the methodology is very well accepted by the field. See attached ADCC Reporter Assay Protocol for further details.
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