Article
Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumors.
Science translational medicine - 29 Apr 2020
Banks Erica, Grondine Michael, Bhavsar Deepa, Barry Evan, Kettle Jason G, Reddy Venkatesh Pilla, Brown Crystal, Wang Haiyun, Mettetal Jerome T, Collins Teresa, Adeyemi Oladipupo, Overman Ross, Lawson Deborah, Harmer Alexander R, Reimer Corinne, Drew Lisa, Packer Martin J, Cosulich Sabina, Jones Rhys DO, Shao Wenlin, Wilson David, Guichard Sylvie, Fawell Stephen, Anjum Rana
Abstract excerpt
Gastrointestinal stromal tumor (GIST) is the most common human sarcoma driven by mutations in KIT or platelet-derived growth factor α (PDGFRα). Although first-line treatment, imatinib, has revolutionized GIST treatment, drug resistance due to acquisition of secondary KIT/PDGFRα mutations develops in a majority of patients. Second- and third-line treatments, sunitinib and regorafenib, lack activity against a...
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