Bevacizumab
From Wikipedia, the free encyclopedia
| Image:Bevacizumab.png | |
| Bevacizumab
| |
| Systematic (IUPAC) name | |
| (not applicable) | |
| Identifiers | |
| CAS number | 216974-75-3 |
| ATC code | L01XC07 |
| PubChem | (none) |
| DrugBank | BTD00087 |
| Chemical data | |
| Formula | ? |
| Mol. weight | 149,000 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 100% (IV only) |
| Metabolism | ? |
| Half life | 20 days (range: 11–50 days) |
| Excretion | ? |
| Therapeutic considerations | |
| Licence data | |
| Pregnancy cat. |
C(US) |
| Legal status |
℞ Prescription only |
| Routes | Intravenous |
Bevacizumab (trade name Avastin®) is an anti-angiogenesis drug used in treatment of cancer.
It is used in combination with standard chemotherapy drugs in patients with metastatic colorectal cancer. The U.S. Food and Drug Administration approved bevacizumab for use in colon cancer 2004. The medicine was developed by Genentech and is marketed, in the United States by Genentech and elsewhere by Roche (Genentech's parent company), under the brand name Avastin.
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[edit] Background
Bevacizumab is a humanized monoclonal antibody, and was the first commercially available angiogenesis inhibitor. It stops tumor growth by preventing the formation of new blood vessels by targeting and inhibiting the function of a natural protein called vascular endothelial growth factor (VEGF) that stimulates new blood vessel formation.
The drug was first developed as a genetically engineered version of a mouse antibody that contains both human and mouse components. Genentech is able to produce the antibody in production-scale quantities.
[edit] Clinical use
Bevacizumab was approved by the Food and Drug Administration (FDA) in February 2004 for use in colorectal cancer when used with standard chemotherapy treatment. It was approved by the EMEA in January 2005 for use in colorectal cancer. Israel has also approved the use of bevacizumab.
Bevacizumab is usually given intravenously through the arm every 14 days. In colon cancer, it is given in combination with the chemotherapy drug 5-FU (5-fluorouracil), leucovorin, and oxaliplatin or irinotecan.
Bevacizumab has also demonstrated activity in renal cell cancer and ovarian cancer when used as a single agent, and in lung cancer and breast cancer when combined with chemotherapy.
[edit] Non oncologic uses
Bevacizumab has recently been used by ophthalmologists as an intravitreal agent in the treatment of proliferative (neovascular) eye diseases, particularly for choroidal neovascular membrane (CNV) in age-related macular degeneration (AMD). Although not currently approved by the FDA for such use, the injection of 1.25-2.5 mg of bevacizumab into the vitreous cavity has been performed without significant intraocular toxicity. Many retina specialists have noted impressive results in the setting of CNV, proliferative diabetic retinopathy, neovascular glaucoma, diabetic macular edema, and macular edema secondary to retinal vein occlusions.
A modified fragment of the bevacizumab antibody (the FAB fragment) has been developed by Genentech (by the same scientist Napoleone Ferrara) for intraocular use. This drug, ranibizumab (Lucentis®), now has FDA approval. It has undergone extensive clinical trials. Reports indicate substantially better outcomes in patients treated with inravitreal Lucentis than conventional treatments in people with choroidal neovascularization (wet age related macular degeneration). Most patients with choroidal neovascularization lose vision or at best maintain vision despite treatment with laser, photodynamic therapy or Macugen. A much larger proportion (up to 54%) gained vision with Lucentis. Lucentis is however very expensive ($1500-2000 per injection, - the studies were done with monthly intravitreal injections). Bevacizumab is significantly cheaper (<$100 a shot versus >$1500) it appears to be safe (at least in the short term) and many doctors have noticed improvements in vision and outcomes similar to those seen with Lucentis. As Genentech has developed both drugs it has little interest in seeing Bevacizumab use in the eye and it is likely to remain off label. The off-label use of this medication has created significant controversy in medical retina and vitreo-retinal surgery.
[edit] Side effects
Several adverse side effects have occurred due to the drug, with two of the most common being hypertension and blood clots. Neutropenia, neuropathy, and proteinuria also occurred at times.
Bowel perforation has also rarely been reported.
[edit] External links
- Avastin.com
- Avastin-info.com Information for healthcare professionals outside of the US
- Avastin Information from Chemocare.com
- A Cancer Drug Shows Promise, at a Price That Many Can't Pay New York Times, February 15, 2006, Alex Berenson
- Drugs firm blocks cheap blindness cure The Guardian, June 17, 2006, Sarah Boseley
