Erbitux (cetuximab)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Cetuximab, a recombinant chimeric (human-murine) monoclonal antibody that binds to epidermal growth factor receptors (EGFR), is an antineoplastic agent.
Cetuximab, a recombinant chimeric (human-murine) monoclonal antibody, is an antineoplastic agent. The drug is an immunoglobulin containing human framework (i.e., IgG1 heavy and kappa light constant regions) and murine Fv regions.
Cetuximab binds specifically to the extracellular domain of the human epidermal growth factor receptor (EGFR, HER1, c-erbB-1) on both normal and tumor cells and competitively blocks the cellular action of EGF and other ligands (e.g., transforming growth factor (TGF)-alpha). EGFR is a transmembrane glycoprotein that belongs to the subfamily of type I receptor tyrosine kinases, which includes EGFR (HER1), HER2, HER3, and HER4. While EGFR is expressed in many normal epithelial tissues (e.g., skin, hair follicle), overexpression of the glycoprotein is detected in human carcinomas (e.g., colon, rectum, head and neck).
In vitro assays and in vivo animal studies have shown that binding of cetuximab to EGFR blocks phosphorylation and activation of receptor-associated kinases; this results in inhibition of cell growth, induction of apoptosis (programmed cell death), and decreased matrix metalloproteinase and vascular endothelial growth factor production. Signal transduction through EGFR leads to activation of the wild-type (nonmutated) KRAS gene. However, the presence of an activating somatic mutation of the KRAS gene (mutated KRAS) in a cancer cell can lead to dysregulation of signaling pathways and resistance to EGFR inhibitor therapy (e.g., cetuximab, panitumumab).
In vitro, cetuximab can mediate antibody-dependent cellular cytotoxicity against certain types of human tumors.
In vitro tests and in vivo animal studies have suggested that cetuximab inhibits growth and survival of tumor cells that express EGFR, while such antitumor effects were not observed in human cancer xenografts that lacked EGFR expression. In xenograft models for human tumors in mice, addition of cetuximab to radiation therapy or irinotecan resulted in an increased antitumor effect when compared with radiation therapy or chemotherapy alone.
The pharmacokinetic disposition of cetuximab was similar in patients receiving the drug for head and neck cancer or colorectal cancer. Following administration of the recommended regimen of cetuximab (initial dose, followed by subsequent weekly doses), steady-state cetuximab concentrations are achieved by the third weekly infusion; the mean half-life of cetuximab following multiple dosing is approximately 112 hours. The major route of clearance from the circulation is believed to be through internalization of the cetuximab EGFR complex on hepatocytes and skin.
USES: Cetuximab is used to treat certain types of cancer (such as colon/rectum, head and neck). Cetuximab works by slowing or stopping the growth of cancer cells. It binds to a certain protein (epidermal growth factor receptor-EGFR) in some tumors.
Cetuximab is a man-made protein (monoclonal antibody).
Generic name: cetuximab
Pronunciation: (se-TUX-i-mab)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Erbitux
Indications
The following indications are listed for Erbitux:
- Metastatic Colorectal Cancer With Braf V600e Mutation
- Squamous Cell Carcinoma Of Head And Neck
- Wild-Type Kras, Egfr-Positive Colorectal Cancer
Also known as: Epidermoid Carcinoma Of The Head And Neck, Wild-Type Kras, Egfr-Expressing Colorectal Cancer.
Dosing
No dosing information is available for this tab.
Cetuximab is administered by IV infusion. The drug should not be administered by rapid IV injection, such as IV push or bolus. The initial dose of cetuximab is administered over 2 hours, and the subsequent weekly dose is administered over 1 hour. The maximum infusion rate should not exceed 10 mg/minute.
Cetuximab injection should be inspected visually for particulate matter and discoloration whenever solution and container permit. Cetuximab injection for IV infusion should be clear and colorless and may contain a small amount of easily visible, white, amorphous cetuximab particulates. Cetuximab injection for IV infusion should not be diluted, and vials should not be shaken.
Cetuximab may be administered using either an infusion pump or a syringe pump. The drug must be administered through a low-protein-binding 0.22-mcm inline filter. Patients should be monitored for signs of infusion reactions during and for 1 hour following cetuximab infusion. For patients experiencing infusion reactions requiring treatment, monitoring should be continued until the event is resolved. (See Infusion-related Effects under Warnings/Precautions: Warnings, in Cautions.)
Cetuximab solution should be stored in unopened vials under refrigeration at 2-8degreesC and protected from freezing. Preparations of cetuximab solution in infusion containers are chemically and physically stable for up to 12 hours at 2-8degreesC and up to 8 hours at controlled room temperature (20-25degreesC); any solution remaining in the infusion container after 8 hours (if stored at room temperature) or after 12 hours (if refrigerated) should be discarded. Cetuximab contains no preservatives; any unused portion of the vial should be discarded.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
The manufacturer states that there are no contraindications to the use of cetuximab.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects, observed in at least 25% of patients receiving cetuximab, are adverse dermatologic effects (including rash, pruritus, and nail changes), headache, diarrhea, and infection. Across studies, infection occurred in 13-35% of patients receiving cetuximab.
The most common adverse effects in patients receiving cetuximab in combination with irinotecan for advanced colorectal cancer include acneiform rash (88%), asthenia/malaise (73%), diarrhea (72%), and nausea (55%); the most common grade 3 or 4 adverse effects include diarrhea (22%), leukopenia (17%), asthenia/malaise (16%), and acneiform rash (14%).
The most common adverse effects in patients receiving cetuximab and best supportive care for advanced colorectal cancer include rash/desquamation (89%), fatigue (89%), abdominal pain (59%), pain (51%), dry skin (49%), dyspnea (48%), and constipation (46%).
The most common adverse effects in patients receiving cetuximab in combination with radiation therapy for advanced head and neck cancer include acneiform rash (87%); radiation dermatitis (86%); weight loss (84%); asthenia (56%); nausea (49%); and elevated serum ALT (43%), AST (38%), and alkaline phosphatase concentrations (33%).
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of cetuximab have not been established in pediatric patients.
Category C. (See Users Guide.)
It is not known whether cetuximab is distributed into milk; however, human immunoglobulin G1 (IgG1) is distributed into milk. Because of the potential for distribution of IgG antibodies such as cetuximab into milk and the risks for serious adverse reactions from cetuximab in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman. Based on the long half-life of cetuximab, women should be advised to discontinue nursing while receiving cetuximab therapy and for at least 60 days following the last dose of the drug (see Description).
Approximately 34% of the 1062 patients receiving cetuximab (alone or in combination with irinotecan) in clinical studies for advanced colorectal cancer were 65 years of age or older. No overall differences in safety and efficacy relative to younger adults were observed.
Clinical studies of cetuximab for head and neck cancer did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger patients. Of 208 patients with advanced head and neck cancer receiving cetuximab and radiation therapy in a clinical trial, 45 patients (22%) were 65 years of age or older.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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