Cetuximab (Erbitux)

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General information

Class/mechanism: EGFR antagonist; monoclonal antibody that binds to the EGFR/HER1/c-ErbB-1 receptor tyrosine kinase, competitively inhibiting binding of epidermal growth factor (EGF) and other ligands, such as transforming growth factor-alpha. This results in inhibition of cell growth, induction of apoptosis, decreased matrix metalloproteinase, and decreased vascular endothelial growth factor production.[1][2][3]
Route: IV
Extravasation: neutral

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Resistance mechanisms

  • Karapetis CS, Khambata-Ford S, Jonker DJ, O'Callaghan CJ, Tu D, Tebbutt NC, Simes RJ, Chalchal H, Shapiro JD, Robitaille S, Price TJ, Shepherd L, Au HJ, Langer C, Moore MJ, Zalcberg JR. K-ras mutations and benefit from cetuximab in advanced colorectal cancer. N Engl J Med. 2008 Oct 23;359(17):1757-65. link to original article PubMed

Diseases for which it is used

Patient drug information

History of changes in FDA indication

Colorectal cancer

  • 2/12/2004: Initial accelerated FDA approval:
  • 10/2/2007: Granted regular approval for the treatment of patients with EGFR-expressing metastatic colorectal cancer (mCRC) after failure of both irinotecan- and oxaliplatin-based chemotherapy regimens. (Approval changed from accelerated to regular)
  • 11/7/2011: Retrospective subset analyses of metastatic or advanced colorectal cancer trials have not shown a treatment benefit for Erbitux in patients whose tumors had KRAS mutations in codon 12 or 13. Use of Erbitux is not recommended for the treatment of colorectal cancer with these mutations. (New recommendation based on KRAS mutant status)
  • 7/6/2012: FDA indication changed:

Head and neck cancer

Also known as

  • Code name: C225
  • Brand names: Cetuxim, Erbitux

References