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All about: Cetuximab

Big Image Pronouncation: (se-TUX-i-mab)
Class: Antineoplastic, Monoclonal antibody

Trade Names:
Erbitux
- Injection 100 mg (2 mg/mL)

Mechanism of Action

Pharmacology

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.

Pharmacokinetics

Absorption

C max is about 184 mcg/mL. Steady-state peak and trough values range from 168 to 235 mcg/mL and 41 to 85 mcg/mL, respectively.

Distribution

Vd is approximately 2 to 3 L/m 2 .

Elimination

Mean t ½ is about 114 h. The elimination t ½ is approximately 97 h.

Indications and Usage

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 EGF receptor–expressing, metastatic colorectal carcinoma in patients who are refractory to irinotecan-based chemotherapy; as single-agent treatment of EGF receptor–expressing, metastatic colorectal carcinoma in patients who are intolerant to irinotecan-based chemotherapy.

Contraindications

Standard considerations.

Dosage and Administration

Colorectal Cancer
Adults

IV 400 mg/m 2 as an initial loading dose administered as a 120-min infusion (max rate of infusion, 5 mL/min). The weekly maintenance dose is 250 mg/m 2 infused over 60 min (max rate of infusion, 5 mL/min).

Squamous Cell Carcinoma of the Head and Neck
Adults

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, 5 mL/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, 5 mL/min) weekly for the duration of radiation therapy (6 to 7 wk). As a single agent, the recommended initial dose is 400 mg/m 2 followed by 250 mg/m 2 weekly until disease progression or unacceptable toxicity.

Dose Modification
Adults Infusion reactions

IV Permanently reduce the infusion rate by 50% in patients experiencing mild or moderate (grade 1 or 2) infusion reactions; permanently discontinue in patients experiencing severe (grade 3 or 4) infusion reactions.

Dermatologic toxicity

IV If patient experiences severe acneform rash: First occurrence: Delay infusion 1 to 2 wk and, if improvement occurs, continue at 250 mg/m 2 . Discontinue if no improvement. Second occurrence: Delay infusion 1 to 2 wk and, if improvement occurs, reduce dose to 200 mg/m 2 . Discontinue if no improvement. Third occurrence: Delay infusion 1 to 2 wk and, if improvement occurs, reduce dose to 150 mg/m 2 . Discontinue if no improvement. Fourth occurrence: Discontinue.

General Advice

  • Follow institutional procedures for handling, administrating, and disposing of anticancer drugs.
  • Premedicate patient with antihistamine (eg, diphenhydramine IV).
  • Do not shake or dilute.
  • Do not mix with any other medications.
  • Do not administer if cloudiness or discoloration is noted. A small amount of white amorphous particulates is normal.
  • Administer prescribed dose using syringe pump or infusion pump following manufacturer's recommendations.
  • Administer with use of low protein binding 0.22 mcm in-line filter placed as proximal to the patient as possible.
  • Flush IV line with saline 0.9% solution at end of infusion.
  • Discard unused portion of vial. Do not save any unused portion for future use.

Storage/Stability

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.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Percentages for adverse reactions are for grades 1 to 4 toxicity with cetuximab monotherapy.

CNS

Asthenia/malaise (48%); asthenia (45%); headache (26%); insomnia (10%); depression (7%).

Dermatologic

Acneform rash (90%); nail disorder (16%); pruritus (11%); conjunctivitis (7%); alopecia, skin disorder (4%).

Electrolytes

Hypomagnesemia (50%).

GI

Nausea (29%); abdominal pain, constipation (26%); diarrhea, vomiting (25%); anorexia (23%); stomatitis (10%); dyspepsia (6%).

Genitourinary

Renal failure (2%).

Hematologic-Lymphatic

Anemia (9%).

Metabolic-Nutritional

Weight loss (27%); dehydration, peripheral edema (10%).

Musculoskeletal

Back pain (10%).

Respiratory

Dyspnea (17%); increased cough (11%); pulmonary embolus (1%).

Miscellaneous

Pain (28%); fever (27%); infusion reactions (21%; severe, 4%); infection (14%); non-neutralizing anti-cetuximab antibodies (5%); severe infusion reactions (4%); sepsis (3%).

Precautions

Warnings

Infusion reactions

Severe infusion reactions, characterized by rapid onset of airway obstruction, urticaria, and hypotension, occurred in approximately 3% of patients and were rarely fatal. About 90% were associated with first infusion. Severe infusion reactions require immediate interruption of infusion and permanent discontinuation of treatment.

Cardiopulmonary arrest

Cardiopulmonary arrest and sudden death occurred in 2% of patients with squamous cell carcinoma of the head and neck treated with radiation therapy and cetuximab. Fatal events occurred within 1 to 43 days after the last cetuximab treatment. Cetuximab, in combination with radiation therapy, should be used with caution in head and neck cancer patients with known coronary artery disease, CHF, or arrhythmias.


Monitor

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).

Cardiopulmonary arrest

Closely monitor serum electrolytes, including serum magnesium, potassium, and calcium, during and after cetuximab therapy.


Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hypersensitivity

Use with caution in patients hypersensitive to cetuximab, murine proteins, or any component of this product.

Combination therapy

Safety of cetuximab in combination with radiation therapy and cisplatin has not been established.

Dermatologic toxicity

Reactions, including acneform rash, skin drying and fissuring, and inflammatory and infectious sequelae, 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.

IV antihistamine

Ensure that premedication with IV antihistamine (eg, diphenhydramine) has been ordered for each infusion.

Pulmonary toxicity

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.

Sun exposure

Because sunlight can exacerbate any skin reactions, instruct patients to use sunscreen and wear hats and limit sun exposure.

Overdosage

Symptoms

No data available.

Patient Information

  • Advise patient, family, or caregiver that medication will be prepared and administered by health care provider in a health care setting.
  • Review dosing schedule with patient, family, or caregiver.
  • Advise patient, family, or caregiver to immediately report any of the following to health care provider: acne-like rash, skin drying or splitting, inflammation or infection; unexplained shortness of breath or difficulty breathing; fever.
  • Advise patient, family, or caregiver to report any of the following to health care provider: persistent nausea, vomiting, diarrhea, or appetite loss; sores in mouth; persistent or worsening general body weakness or fatigue.
  • Advise patient to avoid unnecessary exposure to sunlight or tanning lamps and to use sunscreen and wear protective clothing to reduce risk of worsening any skin reactions.
  • Caution women of childbearing potential to avoid becoming pregnant during therapy.

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