Sunitinib (Molecule of the Month for September 2007)
Sutent, SU11248
Sunitinib (marketed as Sutent) is an anti ancer drug.It is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) in 2006. Sunitinib was the first cancer drug simultaneously approved for two different indications. Sunitinib has since become the standard of care for both of these cancers, and is currently being studied for the treatment of many others.
Sunitinib inhibits cellular signaling by targeting multiple RTKs. These include all platelet-derived growth factor receptors (PDGF-R) and vascular endothelial growth factor receptors (VEGF-R), which play a role in both tumor angiogenesis and tumor cell proliferation. The simultaneous inhibition of these targets therefore leads to both reduced tumor vascularization and cancer cell death, and ultimately tumor shrinkage.
In September 2007, number of cancer patients denied Sunitinib by the UK NHS may get free treatment as part of a clinical trial taking place in Manchester. The drug Sutent can in some cases prolong the lives of patients with kidney cancer. The company, Oxford BioMedica, is funding the supply of the drug, at Christie hospital in Manchester. In return patients must agree to be involved in a trial of the firm's drug TroVax to see how it works with Sutent. The study will test if TroVax adds further benefit and help patients survive longer. Sutent was licensed for treatment of advanced kidney cancer in the UK by regulators a year ago, and is used as a standard therapy in many countries including the USA, France, Germany and Spain. However, it has not been approved by UK drugs watchdog body NICE, but a small number of Primary Care Trusts are funding it at a cost of about £3,000 a month.
Formal Chemical Name (IUPAC)
(Z)-N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide
References
click on the picture of Sunitinib above to interact
with the 3D model of the
Sunitinib structure
(this will open a new browser window)
C22 H27 F N4 O2
Update by Karl Harrison
(Molecule of the Month for
September 2007
)
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