Article
Intracellular concentration of the tyrosine kinase inhibitor imatinib in gastrointestinal stromal tumor cells.
Anti-cancer drugs - 1 Apr 2014
Berglund Erik, Ubhayasekera Sarojini Jayantha Kumari A, Karlsson Fredrik, Akcakaya Pinar, Aluthgedara Warunika, Ahlen Jan, Fröbom Robin, Nilsson Inga-Lena, Lui Weng-Onn, Larsson Catharina, Zedenius Jan, Bergquist Jonas, Bränström Robert
Abstract excerpt
Gastrointestinal stromal tumor (GIST) is the most common mesenchymal neoplasm in the gastrointestinal tract. In most GISTs, the underlying mechanism is a gain-of-function mutation in the KIT or the PDGFRA gene. Imatinib is a tyrosine kinase inhibitor that specifically blocks the intracellular ATP-binding sites of these receptors. A correlation exists between plasma levels of imatinib and progression-free...
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