Cetuximab
- Atc Codes:L01XC06
- CAS Codes:205923-56-4
- PHARMGKB ID:205923-56-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Erbitux; Belgium: Erbitux; Bulgaria: Erbitux; Czech Republic: Erbitux; Denmark: Erbitux; Estonia: Erbitux; Finland: Erbitux; France: Erbitux; Germany: Erbitux; Greece: Erbitux; Hungary: Erbitux; Ireland: Erbitux; Italy: Erbitux; Latvia: Erbitux; Lithuania: Erbitux; Luxembourg: Erbitux; Malta: Erbitux; Netherlands: Erbitux; Poland: Erbitux; Portugal: Erbitux; Romania: Erbitux; Slovakia: Erbitux; Spain: Erbitux; Sweden: Erbitux; UK: Erbitux.
North America
Canada: Erbitux; USA: Erbitux.
Latin America
Argentina: Erbitux; Mexico: Erbitux.
Drug combinations
Chemistry
Cetuximab: Mw: approx. 170000.01. (1) Immunoglobulin G~1~, anti-(human epidermal growth factor receptor)(human-mouse monoclonal C225 γ~1~-chain), disulfide with human-mouse monoclonal C225 κ-chain, dimer; (2) Immunoglobulin G~1~ (human-mouse monoclonal C225 γ~1~-chain anti-human epidermal growth factor receptor), disulfide with human-mouse monoclonal C225 κ-chain, dimer. CAS-205923-56-4 (1999).
Pharmacologic Category
Other Antineoplastic Agents; Monoclonal Antibodies. Epidermal Growth Factor Receptor (EGFR) Inhibitor. (ATC-Code: L01XC06).
Mechanism of action
Recombinant human/mouse chimeric monoclonal antibody which contains human framework regions and murine Fv regions. Binds specifically to the epidermal growth factor receptor (EGFR, HER1, c-ErbB-1) and competitively inhibits the binding of epidermal growth factor (EGF) and other ligands, blocking phosphorylation and activation of receptor-associated kinases, and resulting in inhibition of cell growth, induction of apoptosis, and decreased matrix metalloproteinase and vascular endothelial growth factor production. Can also mediate antibody-dependent cellular cytotoxicity against certain tumor types in vitro.
Therapeutic use
Metastatic colorectal cancer. Squamous cell cancer of the head and neck.
Pregnancy and lactiation implications
Teratogenic effects were not observed in animal studies, but increases in embryolethality and fetal loss were noted. There are no adequate studies in pregnant women. Use only if the potential benefit to the woman justifies the potential risk to the fetus. Not recommended during lactation.
Unlabeled use
Contraindications
Warnings and precautions
Cardiopulmonary arrest reported in patients receiving radiation therapy in combination with cetuximab (caution with history of coronary artery disease, heart failure, and arrhythmias). Acneiform rash is common. Severe infusion reactions (bronchospasm, stridor, hoarseness, urticaria, hypotension, loss of consciousness, cardiac arrest) reported. Interstitial lung disease reported (caution in pre-existing lung disease). Non-neutralizing anticetuximab antibodies detected in 5% of evaluable patients (relationship unknown).