cetuximab   Click here for help

GtoPdb Ligand ID: 6882

Synonyms: C225 | Erbitux® | IMC-225 | IMC-C225
Approved drug
cetuximab is an approved drug (Switzerland (2003), EMA & FDA (2004))
Compound class: Antibody
Comment: Cetuximab binds to and competitively inhibits the activity of the epidermal growth factor receptor (EGFR).
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.

Biosimilars:
As Bristol-Myers Squibb's original EU and US patents for cetuximab have expired, challengers of cetuximab's market position are developing biosimilar and/or biobetter cetuximab.
Celltrion's CT-P15 is a cetuximab biosimilar, intended for the treatment of colorectal cancer. MabTech-Sorrento's STI-001 is a proposed biobetter cetuximab (perhaps because synthesis in CHO cells creates a different glycosylation pattern to that of cetuximab which is made in mouse cells, and may be less likely to cause side-effects such as immunogenicity and hypersensitivity). STI-001 has completed Phase 3 clinical trial in China. Neither of these agents is associated with any clinical studies that are registered with ClinicalTrials.gov.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
Bioactivity Comments
Peptide sequence analysis matches the light chain variable region of cetuximab to patent US7060808 [1]. The Kd value provided in the interaction table below is taken from this patent for the C225 monoclonal presented therein.
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
epidermal growth factor receptor Primary target of this compound Hs Antibody Binding 9.4 pKd - 1
⤷ pKd 9.4 (Kd 3.9x10-10 M) [1]