Complementary activity of tyrosine kinase inhibitors against secondary kit mutations in imatinib-resistant gastrointestinal stromal tumours.
César SerranoAdrián Mariño-EnríquezDerrick L TaoJulia KetzerGrant EilersMeijun ZhuChanning YuAristotle M MannanBrian P RubinGeorge D DemetriChandrajit P RautAjia PresnellArin McKinleyMichael C HeinrichJeffrey T CzaplinskiEwa SicinskaSebastian BauerSuzanne GeorgeJonathan A FletcherPublished in: British journal of cancer (2019)
Our data highlight that heterogeneity of KIT secondary mutations is the main mechanism of tumour progression to KIT inhibitors in imatinib-resistant GIST patients. Therapeutic combinations of TKIs with complementary activity against resistant mutations may be useful to suppress growth of polyclonal imatinib-resistance in GIST.