DCC-2618, a pan KIT and PDGFR switch control inhibitor, achieves proof-of-concept in a first-in-human study
Janku F, George S, Razak A, Gordon M, Brooks D, Flynn DG, Kaufman M, Pitman J, Smith B, et al
European Journal of Cancer, 69, S4 (suppl-S4 (suppl (2016)
DCC-2618 is a potent inhibitor of wild-type and mutant KIT, including refractory Exon 17 D816 KIT mutations, and exhibits efficacy in refractory GIST and AML xenograft models, [abstract]
Smith BD, Hood MM, Wise SC, Kaufman MD, Lu WP, Rutkoski T, Flynn DL, Heinrich MC.
Cancer Research, 75 (15 Suppl), Abstract nr 2690-Abstract nr 2690 (2015)
Cancer discovery, 7(2), 121-122 (2017-01-13)
Tyrosine kinase inhibitors may initially control gastrointestinal stromal tumors, but most patients eventually experience disease progression due to activation loop mutations, which are resistant to approved drugs. However, phase I trials suggest that the cancer is sensitive to two new...
Mathias Schneeweiss et al.
Haematologica, 103(5), 799-809 (2018-02-14)
Systemic mastocytosis is a complex disease defined by abnormal growth and accumulation of neoplastic mast cells in various organs. Most patients exhibit a D816V-mutated variant of KIT, which confers resistance against imatinib. Clinical problems in systemic mastocytosis arise from mediator-related...