Vandetanib

Vandetanib
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.  ?
Legal status ℞-only (US)
Routes Oral
Pharmacokinetic data
Half-life 5 days (mean)
Identifiers
CAS number 443913-73-3 Y
ATC code L01XE12
PubChem CID 3081361
DrugBank DB08764
ChemSpider 2338979 Y
UNII YO460OQ37K N
ChEBI CHEBI:49960 N
ChEMBL CHEMBL24828 Y
Chemical data
Formula C22H24BrFN4O2 
Mol. mass 475.354 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

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

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]

Clinical trials

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]

External links

References

  1. ^ http://nci.nih.gov/Templates/drugdictionary.aspx?CdrID=269177
  2. ^ "FDA approves new treatment for rare form of thyroid cancer". http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm250168.htm. Retrieved 7 April 2011. 
  3. ^ "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. 
  4. ^ "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. 
  5. ^ http://www.sciencedaily.com/releases/2009/06/090601092237.htm "Vandetanib Shows Clinical Benefit When Combined With Docetaxel For Lung Cancer" June 2009
  6. ^ http://www.medpagetoday.com/MeetingCoverage/IASLC/15396 "IASLC: Vandetanib Fails to Improve NSCLC Outcomes with Pemetrexed" Aug 2009
  7. ^ http://clinicaltrials.gov/ct2/show/NCT00687297
  8. ^ 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
CI monoclonal antibodies ("-mab")
Others for solid tumors
Tyrosine-kinase inhibitors ("-nib")
Other

M: NEO

tsoc, mrkr

tumr, epon, para

drug (L1i/1e/V03)