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| {{drugbox-mab |
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| | image =
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| | source = chimeric
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| | target = EGF receptor
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| | CAS_number = 205923-56-4 | ATC_prefix = L01 | ATC_suffix = XC06 | ATC_supplemental = | PubChem = | DrugBank = BTD00071 | C=6484 | H=10042 | N=1732 | O=2023 | S=36 | molecular_weight = 145781.6 g/mol | bioavailability = | protein_bound = | metabolism = | elimination_half-life = 114 hrs | pregnancy_category = | legal_status = | routes_of_administration = }}
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| {{SI}}
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| {{CMG}}
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| ==Overview==
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| '''Cetuximab''' (marketed under the name '''Erbitux''') is a chimeric [[monoclonal antibody]], an [[epidermal growth factor receptor]] (EGFR) [[enzyme inhibitor|inhibitor]], given by [[intravenous therapy|intravenous injection]] for treatment of metastatic [[colorectal cancer]] and head and neck cancer. Cetuximab was discovered by [[ImClone Systems]] and is distributed in North America by ImClone and [[Bristol-Myers Squibb]], while in the rest of the world distribution is by [[Merck KGaA]].
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| Cetuximab faces stiff competition from [[bevacizumab]] (Avastin), from [[Genentech]] and Roche, and from [[panitumumab]] (Vectibix), from [[Amgen]] approved by the FDA in November 2006. One of the main differences is that Cetuximab is an IgG1 antibody, and Panitumumab an IgG2 one. Their properties are not absolutely identical[http://www.healthvalue.net/IgG1_IgG2.html]. Cetuximab costs $30,000 for eight weeks of treatment per patient.<ref name="Schrag">{{cite journal | last =Schrag | first =D | authorlink = | coauthors = | title =The price tag on progress – chemotherapy for colorectal cancer | journal =New England Journal of Medicine | volume =351 | issue =4 | pages =317-319 | publisher = | date =Jul 2004 | url =http://content.nejm.org/cgi/content/extract/351/4/317 | doi = | id = | accessdate = }}</ref>
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| ==Mode of action==
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| Cetuximab is believed to operate by binding to the extracellular domain of the [[epidermal growth factor receptor|EGFR]] of all cells that express EGFR, which includes the subset "cancer cells", preventing ligand binding and activation of the receptor. This blocks the downstream signaling of EGFR resulting in impaired cell growth and proliferation. Cetuximab has also been shown to mediate antibody dependent cellular cytotoxicity ([[ADCC]]).
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| ==Clinical uses==
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| ===[[Colorectal Cancer]]===
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| Cetuximab is used in metastatic [[Colorectal cancer|colon cancer]] and is given concurrently with the chemotherapy drug [[irinotecan]] (Camptosar®), a form of [[chemotherapy]] that blocks the effect of [[DNA topoisomerase|DNA topoisomerase I]], resulting in fatal damage to the DNA of affected cells. While there remains some scientific controversy on this, assessment for EGFR expression is required for use in Colorectal Cancer, but not in Head & Neck Cancer. It is best to refer to updated Prescription Information [http://www.bms.com/cgi-bin/anybin.pl?sql=select%20PPI%20from%20TB_PRODUCT_PPI%20where%20PPI_SEQ=106&key=PPI].
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| ===[[Head and neck cancer]]===
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| Cetuximab was approved by the [[Food and Drug Administration|FDA]] in March 2006[http://www.cancer.gov/clinicaltrials/results/head-neck-cetuximab0604] for use in combination with [[radiation therapy]] for treating [[squamous cell carcinoma]] of the head and neck (SCCHN) or as a single agent in patients who have had prior platinum-based therapy.
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| One of the side effects of Cetuximab therapy is the incidence of, possibly severe, acne-like rash.
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| ==ImClone insider trading scandal ==
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| {{see|ImClone Systems#Insider trading scandal}}
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| The initial failure of [[ImClone Systems]] to prepare an acceptable [[Food and Drug Administration|FDA]] filing led to the infamous Martha Stewart [[insider trading]] scandal when ImClone's CEO sold ImClone shares and this information was leaked to Stewart before the [[Food and Drug Administration|FDA]] announced its refusal to approve the drug for public use. Martha Stewart, Samuel D. Waksal (the founder and former CEO of ImClone), and their broker were indicted, and Stewart and Waksal were sentenced to prison. ImClone shares dropped sharply in the aftermath of the insider trading scandal.
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| A new clinical trial and [[Food and Drug Administration|FDA]] filing prepared by Imclone's partner [[Merck KGaA]] ("German Merck," not to be confused with the US company of similar name) resulted in an [[Food and Drug Administration|FDA]] approval of the drug in 2004 for use in colon cancer.
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| == References ==
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| <references/>
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| ==External links==
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| * [http://www.fda.gov/cder/drug/infopage/erbitux/default.htm FDA Erbitux (cetuximab) Information Page]
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| * [http://www.erbitux.com/ Erbitux site from Bristol-Myers Squibb, ImClone Systems, and Merck KGaA ]
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| * [http://www.healthvalue.net/EGFR-engl.html Anti EGFreceptor monoclonals and small molecules on the web ]
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| {{Chemotherapeutic agents}}
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| {{Chimericmonoclonals}}
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| [[Category:Cancer treatments]]
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| [[Category:Monoclonal antibodies]]
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| [[de:Cetuximab]]
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| [[fr:Cetuximab]]
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| [[he:ארביטוקס]]
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| [[ja:セツキシマブ]]
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