Trade Names:Erbitux- Injection, solution 2 mg/mL
Competitively inhibits binding of epidermal growth factor (EGF) to receptors, which blocks phosphorylation and activation of receptor-associated kinases, resulting in inhibition of cell growth.
Steady-state peak and trough values range from 168 to 235 mcg/mL and 41 to 85 mcg/mL, respectively.
Vd is approximately 2 to 3 L/m 2 .
Mean t ½ is about 112 h.
Women with colorectal cancer have a 25% lower intrinsic Cl than men; however, no changes in dosing are needed.
In combination with radiation therapy for the treatment of locally or regionally advanced squamous cell carcinoma of the head and neck; as single-agent treatment of recurrent or metastatic squamous cell carcinoma of the head and neck in patients in whom prior platinum-based therapy failed; in combination with irinotecan for the treatment of epidermal growth factor receptor (EGFR)–expressing metastatic colorectal carcinoma in patients who are refractory to irinotecan-based chemotherapy; as single-agent treatment of EGFR–expressing metastatic colorectal cancer after failure of both irinotecan- and oxaliplatin-based regimens and in patients who are intolerant to irinotecan-based regimens.
IV 400 mg/m 2 as an initial loading dose administered as a 120-min infusion (max rate of infusion, 10 mg/min). The weekly maintenance dose is 250 mg/m 2 infused over 60 min (max rate of infusion, 10 mg/min) until disease progression or unacceptable toxicity.Squamous Cell Carcinoma of the Head and NeckAdults
IV In combination with radiation therapy, the recommended dose is 400 mg/m 2 as a loading dose given as a 120-min infusion (max infusion rate, 10 mg/min) 1 wk prior to initiation of a course of radiation therapy. The recommended weekly maintenance dose is 250 mg/m 2 infused over 60 min (max infusion rate, 10 mg/min) weekly for the duration of radiation therapy (6 to 7 wk). Complete administration 1 h prior to radiation therapy. As a single agent, the recommended initial dose is 400 mg/m 2 followed by 250 mg/m 2 weekly (max infusion rate, 10 mg/min) until disease progression or unacceptable toxicity.Dose ModificationAdults Dermatologic toxicity
IV If patient experiences severe acneform rash: At first occurrence, delay infusion 1 to 2 wk and, if improvement occurs, continue at 250 mg/m 2 . Discontinue if no improvement. At second occurrence, delay infusion 1 to 2 wk and, if improvement occurs, reduce dose to 200 mg/m 2 . Discontinue if no improvement. At third occurrence, delay infusion 1 to 2 wk and, if improvement occurs, reduce dose to 150 mg/m 2 . Discontinue if no improvement. At fourth occurrence, discontinue.Infusion reactions
IV Reduce the infusion rate by 50% in patients experiencing mild or moderate (grade 1 or 2) or nonserious (grade 3 or 4) infusion reactions; permanently discontinue in patients experiencing severe (grade 3 or 4) infusion reactions.
Store unopened vials in refrigerator (36° to 46°F). Do not freeze. Preparations of cetuximab in infusion containers are stable for up to 8 h at controlled room temperature (68° to 77°F) or 12 h if refrigerated (36° to 46°F). Discard any remaining solution in infusion container after 8 h at controlled room temperature or after 12 h if refrigerated.
None well documented.
None well documented.
Adverse reaction percentages are for grades 1 to 4 toxicity with cetuximab monotherapy.
Fatigue (89%); headache (33%); insomnia (30%); confusion (15%); anxiety (14%); depression (13%).
Rash/desquamation (89%); dry skin (49%); pruritus (40%); nail changes (21%).
Abdominal pain (59%); constipation (46%); diarrhea (39%); vomiting (37%); stomatitis (25%); dry mouth (11%).
Bone pain (15%).
Dyspnea (48%); cough (29%).
Infection without neutropenia (35%); fever (30%); infusion reactions (20%); chills/rigors (13%).
Cardiopulmonary arrest and/or sudden death occurred in 2% of patients with squamous cell carcinoma of the head and neck treated with cetuximab plus radiation therapy. Fatal reactions occurred within 1 to 43 days after the last cetuximab treatment.Infusion reactions
Serious infusion reactions occurred in approximately 3% of patients in clinical trials, with fatal outcomes reported in fewer than 1 in 1,000. Immediately interrupt and permanently discontinue infusion for serious infusion reactions.
Closely monitor serum electrolytes, including serum calcium, magnesium, and potassium, during and after cetuximab therapy.Infusion reaction
Closely monitor patient during and for 1 h following each infusion for signs and symptoms of infusion reaction (eg, bronchospasm, hives, hoarseness, hypotension, stridor). If noted and severe, immediately discontinue infusion and be prepared to treat appropriately (eg, bronchodilators, corticosteroids, epinephrine, IV antihistamines, oxygen).
Category C .
Safety and efficacy not established.
No difference in safety and efficacy observed in patients 65 yr of age and older compared with younger patients.
Use with caution in patients who are hypersensitive to cetuximab, murine proteins, or any component of this product.
Safety of cetuximab in combination with radiation therapy and cisplatin has not been established.
Reactions, including acneform rash, inflammatory and infectious sequelae, and skin drying and fissuring, may occur. Monitor patient for dermatological toxicity (eg, acneform rash, infection, inflammation, skin drying and fissuring). Be prepared to treat infectious sequelae with topical and/or oral antibiotics.
The onset of hypomagnesemia and accompanying electrolyte abnormalities occurred days to months after initiation of cetuximab. Periodically monitor for hypomagnesemia, hypocalcemia, and hypokalemia during and for at least 8 weeks following the completion of cetuximab.
Ensure that premedication with IV antihistamine (eg, diphenhydramine) has been ordered for each infusion.
Interstitial lung disease has been reported. Monitor patient for signs and symptoms of interstitial lung disease (eg, acute onset or worsening of pulmonary symptoms). Interrupt therapy if noted.
Because sunlight can exacerbate any skin reactions, instruct patients to use sunscreen, wear hats, and limit sun exposure.
No data available.
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