205923-56-4

Usage

Uses

Used in Oncology:
Cetuximab is used as a targeted therapy for the treatment of EGF receptor-expressing cancers. It is particularly effective in combination with irinotecan for patients with colorectal cancer who no longer respond to standard chemotherapy. The binding of cetuximab to EGFR on both normal and tumor cells prevents growth factors from binding to the receptor, thereby inhibiting cell growth and inducing apoptosis.
The therapeutic regimen of cetuximab consists of an initial loading dose of 400 mg/m2 administered as a 120-min IV infusion, followed by a weekly maintenance dose of 250 mg/m2 infused over 60 min. The steady-state plasma concentrations of cetuximab are reached by the third weekly infusion, and the mean elimination half-life is 114 hours. Cetuximab is eliminated by binding to EGFRs in various tissues, followed by internalization of the antibody-EGFR complex. Systemic clearance of the antibody is saturated at higher doses, which correlates with saturation of EGFR binding.
In a multicenter clinical trial involving more than 300 patients with advanced metastatic colorectal cancer, the combination therapy with cetuximab and irinotecan produced a response in more than half of the patients, shrinking tumors in 23% and stopping tumor growth in an additional 33% of the patients.
Common adverse reactions associated with cetuximab include acneform rash, asthenia/malaise, fever, nausea, abdominal pain, constipation, and vomiting. Serious adverse events such as infusion reaction, fever, sepsis, kidney failure, dehydration, and diarrhea were experienced by less than 10% of the patients.

Originator

ImClone (US)

Clinical Use

Monoclonal antibody: Treatment of EGFR-expressing metastatic colorectal cancer in combination with irinotecan after failure of irinotecan-including cytotoxic therapy Treatment of head and neck cancer

Toxicology

The majority of skin toxicities were mild to moderate, symptomatic treatments were effective in controlling them. The skin discomfort caused by cetuximab can?affect the quality of life temporarily; with long term treatment, severity of skin toxicity?may decrease.

Drug interactions

Potentially hazardous interactions with other drugs Avoid with live vaccines.

Metabolism

Several pathways have been described that may contribute to the metabolism of antibodies. All of these pathways involve the biodegradation of the antibody to smaller molecules, i.e. small peptides or amino acids.