Definition: Sunitinib (marketed as Sutent, and previously known as SU11248) is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTKs) inhibitor (multiRTKs inhibitors).
Sunitinib was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006.
The concept was of a ATP analogue that would compete with ATP for binding to the catalytic site of receptor tyrosine kinases. This concept led (...)
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Small molecule
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sunitinib
2 June 2009 -
dasatinib
2 September 2008WP
Definition: Dasatinib is a dual inhibitor of the src and abl tyrosine kinases. It was approved by the Federal Drug Administration for the treatment of imatinib mesylate-resistant chronic myeloid leukemia.
Dasatinib inhibits juxtamembrane domain mutant KIT-D816V autophosphorylation and KIT-dependent activation of down stream signaling important for cell growth and survival of neoplastic cells.
Additionally, dasatinib induces apoptosis in mast cell and leukemia cell lines expressing (...) -
crizotinib
10 June 2010Pfizer drug crizotinibPF-02341066 or 1066, PF-02341066, Xalkori Wikipedia
Molecular target: ALK
Definition: Crizotinib is an ALK inhibitor , ROS1 inhibitor and MET inhibitor .
Crizotinib is undergoing clinical trials testing its safety and efficacy in anaplastic large cell lymphoma, neuroblastoma, advanced non-small cell lung carcinoma (NSCLC ).
Crizotinib is an oral ALK (anaplastic lymphoma kinase) inhibitor under study in patients with advanced NSCLC carrying the echinoderm (...)