Erbitux

Head and neck squamous cell carcinoma — locally or regionally advanced (with radiation), recurrent locoregional or metastatic (with platinum-based therapy plus 5-FU, or as single agent after failure of platinum-based therapy); Metastatic colorectal cancer — KRAS wild-type (as determined by approved test), either with FOLFIRI (first-line), with irinotecan (after irinotecan failure), or as single agent (after failure of oxaliplatin- and irinotecan-based chemotherapy or in patients intolerant to irinotecan)

Initial dose: 400 mg/m² IV over 120 minutes
Subsequent doses: 250 mg/m² IV over 60 minutes weekly
Pre-medication: H1-receptor antagonist (e.g., diphenhydramine 50 mg IV) 30-60 minutes prior to first dose; pre-medication for subsequent doses based on clinical judgment
Maximum infusion rate: 10 mg/min

Injection: 2 mg/mL solution in 50 mL (100 mg) and 100 mL (200 mg) single-dose vials

None listed.

• Infusion Reactions: Fatal reactions (0.1%); severe reactions (3%). Most occur with first infusion. Pre-medicate and monitor for at least 1 hour post-infusion.
• Cardiopulmonary Arrest: Monitor electrolytes (magnesium, potassium, calcium) during and for 8 weeks after completion.
• Pulmonary Toxicity/ILD: Reported in <0.5%; fatal cases occurred.
• Dermatologic Toxicities: Acneiform rash in 76-88% of patients. May require dose modification. Sun-limiting measures recommended.
• Hypomagnesemia: Reported in 55% of patients. Monitor electrolytes for at least 8 weeks after last dose.
• KRAS Testing Required for CRC: Do not use for KRAS-mutant or unknown KRAS status CRC patients.

Acneiform rash (76-88%), fatigue (49%), hypomagnesemia (55%), headache (26%), diarrhea (25%), infection (13-44%), nausea (29%), pyrexia (22%), nail changes (21%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Cetuximab is a recombinant human/mouse chimeric IgG1 monoclonal antibody that binds specifically to the extracellular domain of the human epidermal growth factor receptor (EGFR/HER1/c-ErbB-1). It competitively inhibits EGF and other ligand binding, blocking receptor activation and downstream signaling (RAS/RAF/MAPK pathway). Cetuximab also mediates antibody-dependent cellular cytotoxicity (ADCC) against tumor cells.

Half-life: approximately 112 hours (range 63-230 hours). Vd: 2-3 L/m². Clearance: 0.02 L/h/m². Steady-state reached by third weekly infusion. Non-linear clearance at lower doses.

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• CRYSTAL — Cetuximab + FOLFIRI vs. FOLFIRI in 1L KRAS wild-type metastatic CRC. Phase III, n=1198.
  🔬 NCT00154102 ↗ 📄 Primary Publication ↗
• EXTREME — Cetuximab + platinum/5-FU vs. chemo in 1L recurrent/metastatic HNSCC. Phase III, n=442.
  🔬 NCT00122460 ↗ 📄 Primary Publication ↗

Erbitux has FDA-approved indications across the following cancer types covered on PipelineEvidence: