Resistance mutations to imatinib and successor compounds Kit kinase

2 Resistance mutations to imatinib and successor compounds (KIT kinase) 

Inhibitor resistance mutants have also been identified in tumors from patients with gastrointestinal stromal tumors (GISTs).38 These tumors are driven by activating mutations of KIT and PDGFRa receptor tyrosine kinases.39 Both imatinib and sunitinib are indicated to treat surgically inoperable GISTs. However, complete responses are rare and many patients go on to develop secondary resistance.40 

In one study, a total of 53 tumor samples were obtained from 14 patients that progressed on imatinib or sunitinib. These were subject to D-HPLC and mutation-specific PCR. KIT oncogenic mutations were found in 11 patients, and 

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