Erbitux (cetuximab)

Antineoplastic - EGFR Inhibitors, Monoclonal Antibodies Intravenous Vial (Ml)

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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)
Drug class: Antineoplastic - EGFR Inhibitors, Monoclonal Antibodies
Therapeutic class: Antineoplastics

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

Today’s intelligence on Erbitux

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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.

Drug interactions

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Contraindications

The manufacturer states that there are no contraindications to the use of cetuximab.

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%).

Precautions

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ICD codes

CodeTypeDescription
Metastatic colorectal cancer with BRAF v600E mutation
C18ICD10CMMalignant neoplasm of colon
C18.0ICD10CMMalignant neoplasm of cecum
C18.2ICD10CMMalignant neoplasm of ascending colon
C18.3ICD10CMMalignant neoplasm of hepatic flexure
C18.4ICD10CMMalignant neoplasm of transverse colon
C18.5ICD10CMMalignant neoplasm of splenic flexure
C18.6ICD10CMMalignant neoplasm of descending colon
C18.7ICD10CMMalignant neoplasm of sigmoid colon
C18.8ICD10CMMalignant neoplasm of overlapping sites of colon
C18.9ICD10CMMalignant neoplasm of colon, unspecified
C19ICD10CMMalignant neoplasm of rectosigmoid junction
C20ICD10CMMalignant neoplasm of rectum
Squamous cell carcinoma of head and neck
C44.02ICD10CMSquamous cell carcinoma of skin of lip
C44.12ICD10CMSquamous cell carcinoma of skin of eyelid, including canthus
C44.121ICD10CMSquamous cell carcinoma of skin of unspecified eyelid, including canthus
C44.122ICD10CMSquamous cell carcinoma of skin of right eyelid, including canthus
C44.1221ICD10CMSquamous cell carcinoma of skin of right upper eyelid, including canthus
C44.1222ICD10CMSquamous cell carcinoma of skin of right lower eyelid, including canthus
C44.129ICD10CMSquamous cell carcinoma of skin of left eyelid, including canthus
C44.1291ICD10CMSquamous cell carcinoma of skin of left upper eyelid, including canthus
C44.1292ICD10CMSquamous cell carcinoma of skin of left lower eyelid, including canthus
C44.22ICD10CMSquamous cell carcinoma of skin of ear and external auricular canal
C44.221ICD10CMSquamous cell carcinoma of skin of unspecified ear and external auricular canal
C44.222ICD10CMSquamous cell carcinoma of skin of right ear and external auricular canal
C44.229ICD10CMSquamous cell carcinoma of skin of left ear and external auricular canal
C44.32ICD10CMSquamous cell carcinoma of skin of other and unspecified parts of face
C44.320ICD10CMSquamous cell carcinoma of skin of unspecified parts of face
C44.321ICD10CMSquamous cell carcinoma of skin of nose
C44.329ICD10CMSquamous cell carcinoma of skin of other parts of face
C44.42ICD10CMSquamous cell carcinoma of skin of scalp and neck
Wild-type KRAs, EGFr-positive colorectal cancer
C18.0ICD10CMMalignant neoplasm of cecum
C18.1ICD10CMMalignant neoplasm of appendix
C18.2ICD10CMMalignant neoplasm of ascending colon
C18.3ICD10CMMalignant neoplasm of hepatic flexure
C18.4ICD10CMMalignant neoplasm of transverse colon
C18.5ICD10CMMalignant neoplasm of splenic flexure
C18.6ICD10CMMalignant neoplasm of descending colon
C18.7ICD10CMMalignant neoplasm of sigmoid colon
C18.8ICD10CMMalignant neoplasm of overlapping sites of colon
C18.9ICD10CMMalignant neoplasm of colon, unspecified
C20ICD10CMMalignant neoplasm of rectum

ICD code information from First Databank (FDB).

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data