Vandetanib
| This article relies on references to primary sources or sources affiliated with the subject, rather than references from independent authors and third-party publications. Please add citations from reliable sources. (July 2009) |
| Systematic (IUPAC) name | |
|---|---|
| N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine | |
| Clinical data | |
| Trade names | Caprelsa |
| AHFS/Drugs.com | Consumer Drug Information |
| MedlinePlus | a611037 |
| Licence data | US FDA:link |
| Pregnancy cat. | D |
| Legal status | ℞-only (US) |
| Routes | Oral |
| Pharmacokinetic data | |
| Half-life | 19 days (mean) |
| Identifiers | |
| CAS number | 443913-73-3 |
| ATC code | L01XE12 |
| PubChem | CID 3081361 |
| DrugBank | DB08764 |
| ChemSpider | 2338979 |
| UNII | YO460OQ37K |
| ChEBI | CHEBI:49960 |
| ChEMBL | CHEMBL24828 |
| Chemical data | |
| Formula | C22H24BrFN4O2 |
| Mol. mass | 475.354 g/mol |
| SMILES | eMolecules & PubChem |
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Vandetanib (rINN, trade name Caprelsa), also known as ZD6474, is an antagonist of the vascular endothelial growth factor receptor (VEGFR) and the epidermal growth factor receptor (EGFR).[1] It is a tyrosine kinase inhibitor, being developed by AstraZeneca.
It has a third target: inhibiting RET-tyrosine kinase activity, an important growth driver in certain types of thyroid cancer
Contents |
[edit] Approvals and indications
In April 2011, Vandetanib became the first drug to be approved by FDA for treatment of late-stage (metastatic) medullary thyroid cancer in adult patients who are ineligible for surgery.[2] Vandetanib was first initially marketed without a tradename,[3] and is being marketed under the trade name Caprelsa since August 2011.[4]
[edit] Clinical trials
[edit] Non-small cell lung cancer
It is a medication currently undergoing clinical trials as a potential targeted treatment for non-small-cell lung cancer. There have been some promising results from a phase III trial with docetaxel.[5] There have also been ambivalent results when used with pemetrexed[6] Another trial with docetaxel was recruiting in July 2009.[7]
AstraZeneca withdrew EU regulatory submissions for Zactima in October 2009 after trials showed no benefit when the drug was administered alongside chemotherapy.[8]
[edit] External links
[edit] References
- ^ http://nci.nih.gov/Templates/drugdictionary.aspx?CdrID=269177
- ^ "FDA approves new treatment for rare form of thyroid cancer". http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm250168.htm. Retrieved 7 April 2011.
- ^ "FDA approves orphan drug vandetanib for advanced medullary thyroid cancer" (Press release). AstraZeneca. http://www.astrazeneca-us.com/about-astrazeneca-us/newsroom/all/12149869?itemId=12149869. Retrieved 2011-08-17.
- ^ "AstraZeneca announces trade name CAPRELSA® for vandetanib" (Press release). AstraZeneca. http://www.astrazeneca-us.com/about-astrazeneca-us/newsroom/all/12379191?itemId=12379191. Retrieved 2011-08-17.
- ^ http://www.sciencedaily.com/releases/2009/06/090601092237.htm "Vandetanib Shows Clinical Benefit When Combined With Docetaxel For Lung Cancer" June 2009
- ^ http://www.medpagetoday.com/MeetingCoverage/IASLC/15396 "IASLC: Vandetanib Fails to Improve NSCLC Outcomes with Pemetrexed" Aug 2009
- ^ http://clinicaltrials.gov/ct2/show/NCT00687297
- ^ http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/001194/wapp/Initial_authorisation/human_wapp_000025.jsp&murl=menus/medicines/medicines.jsp&mid=WC0b01ac058001d128&jsenabled=true
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