cetuximab, Erbitux

 Indications

Locally or regionally advanced squamous cell carcinoma

of the head and neck with radiation. Recurrent or

metastatic squamous cell carcinoma of the head and

neck progressing after platinum-based therapy. Recurrent

or metastatic squamous cell carcinoma of the head

and neck in combination with platinum-based therapy

with 5-fluorouracil. K-ras wild-type, epidermal

growth factor receptor (EGFR)-expressing metastatic

colorectal cancer in patients who have not responded

to irinotecan and oxaliplatin or are intolerant to irinotecan.

In combination with irinotecan in patients with

K-ras wild-type, EGFR-expressing metastatic colorectal

cancer who have not responded to irinotecan alone.

First-line treatment of K-ras wild-type, EGFR-expressing

metastatic colorectal cancer in combination with irinotecan,

5-fluorouracil, and leucovorin (FOLFIRI).

Action

Binds specifically to EGFR, thereby preventing the

binding of endogenous epidermal growth factor (EGF).

This prevents cell growth and differentiation processes.

Combination with irinotecan enhances antitumor effects

of irinotecan. Therapeutic Effects: Decreased

tumor growth and spread.

Pharmacokinetics

Absorption: IV administration results in complete

bioavailability.

Distribution: Unknown.

Metabolism and Excretion: Unknown.

Half-life: 97–114 hr.

TIME/ACTION PROFILE

ROUTE ONSET PEAK DURATION

IV unknown unknown unknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity to cetuximab

or murine (mouse) proteins; RAS-mutant metastatic

colorectal cancer or unknown RAS mutation status (q

mortality and tumor progression); OB, Lactation: Pregnancy

or lactation.

Use Cautiously in: Exposure to sunlight (may exacerbate

dermatologic toxicity); Pedi: Safety not established.

Adverse Reactions/Side Effects

Most adverse reactions reflect combination therapy

with irinotecan.

CNS: malaise, depression, headache, insomnia.

EENT: conjunctivitis, ulcerative keratitis. Resp:

cough, dyspnea, interstitial lung disease. CV: CARDIOPULMONARY

ARREST, PULMONARY EMBOLISM, SUDDEN CARDIAC

DEATH. GI: abdominal pain, constipation, diarrhea,

nausea, vomiting, anorexia, stomatitis. GU: renal

failure. Derm: STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL

NECROLYSIS, acneform dermatitis, hypertrichosis,

nail disorder, pruritus, skin desquamation, skin

infection. F and E: dehydration, hypomagnesemia, peripheral edema. Hemat: anemia, leukopenia. MS:

back pain.Metab: weight loss. Misc: INFUSION REACTIONS,

fever, desquamation of mucosal epithelium.

Interactions

Drug-Drug: None noted.

Route/Dosage

Head & Neck Cancer with Radiation or in

Combination with Platinum-Based Therapy

with 5-Fluorouracil

IV (Adults): 400 mg/m2 administered 1 wk prior to initiation

of radiation therapy or on the day of initiation of

platinum-based therapy with 5-fluorouracil (complete

infusion 1 hr to prior to starting platinum-based therapy

with 5-fluorouracil), followed by weekly maintenance

doses of 250 mg/m2 for the duration of radiation

therapy or until disease progression or unacceptable

toxicity with platinum-based therapy with 5-fluorouracil

(complete infusion 1 hr prior to radiation therapy or

platinum-based therapy with 5-fluorouracil). Dose

modification recommended for dermatologic toxicity.

Head and Neck Cancer Monotherapy

IV (Adults): 400 mg/m2 initial loading dose, followed

by weekly maintenance doses of 250 mg/m2 until disease

progression or unacceptable toxicity; dose modification

recommended for dermatologic toxicity.

Colorectal Cancer

IV (Adults): 400 mg/m2 initial loading dose, followed

by weekly maintenance doses of 250 mg/m2 until disease

progression or unacceptable toxicity; dose modification

recommended for dermatologic toxicity.

Availability

Solution for injection: 2 mg/mL.