Generic Name: Trastuzumab Brand Name(s): Herceptin® IUPAC: Humanized anti-HER2 antibody FDA Approval: yes Manufacturer Link
Usage: Herceptin® is used to treat breast cancer. Trastuzumab (Herceptin®) is given both alone and in combination with other treatments. In many cases, combination treatment with chemotherapy has been found to yield better results. (1) Herceptin® is given via intravenous infusion in the arm or hand."
Mechanism: Trastuzumab binds to the extracellular segment of the epidermal growth factor receptor ( also called HER2, HER-2, HER2/neu). The binding blocks signals that would otherwise result in cell division. The result is a reduction in reproduction of cells treated with the drug. Note that the image shown is a general structure of an antibody. There are four proteins bound together in a 'Y' shape. The two top tips of the Y are where the antibody binds with its target. This means that each antibody molecule can bind to two identical target regions.
Side Effects: Common side effects include fever, diarrhea, headache, cough, lightheadedness, nausea, pain at the tumor site, skin inflammation, vomiting, weakness. These side effects are usually mild and decrease in severity with each administration of the drug. Herceptin® can cause more serious problems in patients with other pre-existing conditions, such as heart and lung disorders. (2)
When taken in conjunction with chemotherapy the side effects of those drugs must also be taken into consideration.
For many patients, the efficacy of Herceptin® is limited by the development of resistance, often after about one year of treatment. It is thought that the production of a different growth factor,insulin-like growth factor-I (IGF-I), may be responsible for this resistance. In an effort to bypass resistance researchers have created Herceptin-DM1®. DM1 is a chemotherapy drug that when attached to Herceptin® not only has anti-tumor effects on resistant cancers but perhaps may also be more effective than Herceptin® alone.
2001 Molecular Targets and Cancer Therapeutics. "Conjugated Herceptin Dramatically Improves Herceptin-Alone Results Against Breast Cancer." AACR, 2001. (April 2001). [http://www.aacr.org./1000/1100/1131x.html]