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Cetuximab?
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| Therapeutic monoclonal antibody | |
| Source | chimeric |
| Target | EGF receptor |
| Identifiers | |
| CAS number | |
| ATC code | L01 |
| PubChem | ? |
| DrugBank | |
| Chemical data | |
| Formula | C6484H10042N1732O2023S36 |
| Mol. mass | 145781. Components Infix for origin/source The infix preceding the -mab suffix denotes the animal origin of the antibodies Monoclonal antibodies ( mAb or moAb) are monospecific antibodies that are identical because they are produced by one type of immune cell Monoclonal antibodies ( mAb or moAb) are monospecific antibodies that are identical because they are produced by one type of immune cell An antigen (from antibody-generating) or immunogen is a substance that prompts the generation of Antibodies and can cause an immune response CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the Sulfur or sulphur (ˈsʌlfɚ see spelling below) is the Chemical element that has the Atomic number 16 The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 6 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 114 hrs |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | ? |
Cetuximab (marketed under the name Erbitux) is a chimeric monoclonal antibody, an epidermal growth factor receptor (EGFR) inhibitor, given by intravenous injection for treatment of metastatic colorectal cancer and head and neck cancer. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction In Pharmacology and Toxicology, a route Monoclonal antibodies ( mAb or moAb) are monospecific antibodies that are identical because they are produced by one type of immune cell The epidermal growth factor receptor (EGFR ErbB-1 HER1 in humans is the cell-surface receptor for members of the Epidermal growth factor family (EGF-family Enzyme inhibitors are Molecules that bind to Enzymes and decrease their activity. Intravenous therapy or IV therapy is the giving of Liquid substances directly into a Vein. Colorectal cancer, also called colon cancer or large bowel cancer, includes Cancerous growths in the colon, Rectum and 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. ImClone Systems Incorporated ( is a Biopharmaceutical company dedicated to developing biologic medicines in the area of Oncology. Bristol-Myers Squibb ( colloquially referred to as BMS, is a Pharmaceutical Corporation, formed by a 1989 merger between pharmaceutical companies Merck KGaA (EMD Chemicals in the United States and Canada is a German -based chemical and Pharmaceutical company.
Cetuximab faces stiff competition from panitumumab (Vectibix), from Amgen approved by the FDA in November 2006. Panitumumab ( INN) also ABX-EGF, is a fully human Monoclonal antibody specific to the Epidermal growth factor receptor (also known as Amgen Inc () is an international Biotechnology company headquartered in Thousand Oaks California. One of the main differences is that Cetuximab is an IgG1 antibody, and Panitumumab an IgG2 one. Their properties are not absolutely identical. [1] Cetuximab costs $30,000 for eight weeks of treatment per patient. [2]
Contents |
Mode of action
Cetuximab is believed to operate by binding to the extracellular domain of the EGFR of all cells that express EGFR, which includes the subset "cancer cells", preventing ligand binding and activation of the receptor. The epidermal growth factor receptor (EGFR ErbB-1 HER1 in humans is the cell-surface receptor for members of the Epidermal growth factor family (EGF-family 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).
Clinical uses
Colorectal Cancer
Cetuximab is used in metastatic colon cancer and is given concurrently with the chemotherapy drug irinotecan (Camptosar), a form of chemotherapy that blocks the effect of DNA topoisomerase I, resulting in fatal damage to the DNA of affected cells. Colorectal cancer, also called colon cancer or large bowel cancer, includes Cancerous growths in the colon, Rectum and Colorectal cancer, also called colon cancer or large bowel cancer, includes Cancerous growths in the colon, Rectum and Irinotecan is a chemotherapy agent that is a topoisomerase 1 inhibitor. Chemotherapy, in its most general sense refers to treatment of disease by chemicals that kill cells specifically those of micro-organisms or Cancer. Topoisomerases (type I, type II) are Isomerase Enzymes that act on the topology of DNA. 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[3].
Head and neck cancer
Cetuximab was approved by the FDA in March 2006[4] 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. The term head and neck cancer refers to a group of biologically similar cancers originating from the upper aerodigestive tract including the Lip, Oral cavity ( Radiation therapy (or radiotherapy) is the medical use of Ionizing radiation as part of Cancer treatment to control Malignant In Medicine, squamous cell carcinoma (SCC is a form of Cancer of the Carcinoma type that may occur in many different organs including the Skin
One of the side effects of Cetuximab therapy is the incidence of, possibly severe, acne-like rash.
ImClone insider trading scandal
- Further information: ImClone Systems#Insider trading scandal
The initial failure of ImClone Systems to prepare an acceptable 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 FDA announced its refusal to approve the drug for public use. ImClone Systems Incorporated ( is a Biopharmaceutical company dedicated to developing biologic medicines in the area of Oncology. ImClone Systems Incorporated ( is a Biopharmaceutical company dedicated to developing biologic medicines in the area of Oncology. Martha Stewart (born Martha Helen Kostyra; August 3, 1941) is an American Business magnate, Television host, author Insider trading is the trading of a Corporation 's Stock or other securities (e 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. Samuel D Waksal, who was born September 8, 1947 in Paris France to Holocaust survivor parents is an Jewish American Immunologist ImClone shares dropped sharply in the aftermath of the insider trading scandal.
A new clinical trial and 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 FDA approval of the drug in 2004 for use in the treatment of colon cancer. Merck KGaA (EMD Chemicals in the United States and Canada is a German -based chemical and Pharmaceutical company.
References
- ^ IgG1_IgG2
- ^ Schrag, D (Jul 2004). "The price tag on progress – chemotherapy for colorectal cancer". New England Journal of Medicine 351 (4): 317-319. doi:. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document.
- ^ http://www.bms.com/cgi-bin/anybin.pl?sql=select%20PPI%20from%20TB_PRODUCT_PPI%20where%20PPI_SEQ=106&key=PPI
- ^ Cetuximab Beneficial in Head and Neck Cancer - National Cancer Institute
External links
- FDA Erbitux (cetuximab) Information Page
- Erbitux site from Bristol-Myers Squibb, ImClone Systems, and Merck KGaA
- Anti EGFreceptor monoclonals and small molecules on the web
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