Article
Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients.
Clinical cancer research : an official journal of the American Association for Cancer Research - 15 Nov 2014
Garner Andrew P, Gozgit Joseph M, Anjum Rana, Vodala Sadanand, Schrock Alexa, Zhou Tianjun, Serrano Cesar, Eilers Grant, Zhu Meijun, Ketzer Julia, Wardwell Scott, Ning Yaoyu, Song Youngchul, Kohlmann Anna, Wang Frank, Clackson Tim, Heinrich Michael C, Fletcher Jonathan A, Bauer Sebastian, Rivera Victor M
Abstract excerpt
PURPOSE: KIT is the major oncogenic driver of gastrointestinal stromal tumors (GIST). Imatinib, sunitinib, and regorafenib are approved therapies; however, efficacy is often limited by the acquisition of polyclonal secondary resistance mutations in KIT, with those located in the activation (A) loop (exons 17/18) being particularly problematic. Here, we explore the KIT-inhibitory activity of ponatinib in...
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