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Ripretinib in patients with advanced gastrointestinal stromal tumours (INVICTUS): a double-blind, randomised, placebo-controlled, phase 3 trial
Jean‐Yves Blay, César Serrano, Michael Charles Heinrich et al. · The Lancet Oncology
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5 Jun 2020 |
430 |
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Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers
Sheng-Bin Peng et al. · Cancer Cell
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Sep 2015 |
312 |
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Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants
Bryan D. Smith et al. · Cancer Cell
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May 2019 |
285 |
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Composite grading algorithm for the National Cancer Institute’s Patient-Reported Outcomes version of the Common Terminology Criteria for Adverse Events (PRO-CTCAE)
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Dec 2020 |
256 |
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Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036
Wayne W. Chan et al. · Cancer Cell
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Apr 2011 |
213 |
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The Selective Tie2 Inhibitor Rebastinib Blocks Recruitment and Function of Tie2Hi Macrophages in Breast Cancer and Pancreatic Neuroendocrine Tumors
Allison S. Harney, George S. Karagiannis, Jeanine Pignatelli et al. · Molecular Cancer Therapeutics
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24 Aug 2017 |
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Gemcitabine sensitization by checkpoint kinase 1 inhibition correlates with inhibition of a Rad51 DNA damage response in pancreatic cancer cells
Leslie A. Parsels, Meredith Ann Morgan, Daria M. Tanska et al. · Molecular Cancer Therapeutics
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2009 |
146 |
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Ripretinib Versus Sunitinib in Patients With Advanced Gastrointestinal Stromal Tumor After Treatment With Imatinib (INTRIGUE): A Randomized, Open-Label, Phase III Trial
Sebastian Bauer, Robin L. Jones, Jean‐Yves Blay et al. · Journal of Clinical Oncology
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10 Aug 2022 |
121 |
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The ABL Switch Control Inhibitor DCC-2036 Is Active against the Chronic Myeloid Leukemia Mutant BCR-ABLT315I and Exhibits a Narrow Resistance Profile
Christopher A. Eide, Lauren T. Adrian, Jeffrey Tyner et al. · Cancer Research
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19 Apr 2011 |
119 |
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Three novel patient‐derived BCR/ABL mutants show different sensitivity to second and third generation tyrosine kinase inhibitors
Sara Redaelli, Luca Mologni, Roberta Rostagno et al. · American Journal of Hematology
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AXL regulates mesothelioma proliferation and invasiveness
W-B Ou, Joseph M. Corson, Darren Flynn et al. · Oncogene
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6 Dec 2010 |
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Switch Control Inhibition of KIT and PDGFRA in Patients With Advanced Gastrointestinal Stromal Tumor: A Phase I Study of Ripretinib
Filip Jankú, Albiruni R. Abdul Razak, Ping Chi et al. · Journal of Clinical Oncology
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17 Aug 2020 |
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Multipolymer Solution-Phase Reactions: Application to the Mitsunobu Reaction
Andrew M. Harned, Helen Song He, Patrick H. Toy et al. · Journal of the American Chemical Society
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13 Dec 2004 |
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A Phase I Study of LY3009120, a Pan-RAF Inhibitor, in Patients with Advanced or Metastatic Cancer
Ryan Joseph Sullivan et al. · Molecular Cancer Therapeutics
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23 Oct 2019 |
89 |
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Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2
Bryan D. Smith et al. · Molecular Cancer Therapeutics
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18 Aug 2015 |
81 |
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Vimseltinib versus placebo for tenosynovial giant cell tumour (MOTION): a multicentre, randomised, double-blind, placebo-controlled, phase 3 trial
Hans A. J. Gelderblom et al. · The Lancet
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Jun 2024 |
79 |
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Vimseltinib: A Precision CSF1R Therapy for Tenosynovial Giant Cell Tumors and Diseases Promoted by Macrophages
Bryan D. Smith, Michael D. Kaufman, Scott Wise et al. · Molecular Cancer Therapeutics
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25 Aug 2021 |
74 |
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Targeted Inhibition of Multiple Receptor Tyrosine Kinases in Mesothelioma
Wen‐Bin Ou, Christopher G. Hubert, Jonathan Alfred Fletcher et al. · Neoplasia
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2011 |
72 |
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Novel MET/TIE2/VEGFR2 inhibitor altiratinib inhibits tumor growth and invasiveness in bevacizumab-resistant glioblastoma mouse models
Yuji Piao, Soon Young Park, Verlene K. Henry et al. · Neuro-Oncology
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9 Mar 2016 |
69 |
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NTRK kinase domain mutations in cancer variably impact sensitivity to type I and type II inhibitors
Romel Somwar, Nicolle E. Hofmann, Bryan D. Smith et al. · Communications Biology
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16 Dec 2020 |
62 |
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Ripretinib versus sunitinib in gastrointestinal stromal tumor: ctDNA biomarker analysis of the phase 3 INTRIGUE trial
Michael Charles Heinrich et al. · Nature Medicine
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5 Jan 2024 |
61 |
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Effective inhibition of c-MET-mediated signaling, growth and migration of ovarian cancer cells is influenced by the ovarian tissue microenvironment
Youngjoo Kwon, Barbara D. Smith, Yan Zhou et al. · Oncogene
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23 Dec 2013 |
60 |
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Intrigue: Phase III Study of Ripretinib Versus Sunitinib in Advanced Gastrointestinal Stromal Tumor After Imatinib
John J. Nemunaitis, Sebastian Bauer, Jean‐Yves Blay et al. · Future Oncology
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22 Nov 2019 |
56 |
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Application of the Lugano Classification for Initial Evaluation, Staging, and Response Assessment of Hodgkin and Non-Hodgkin Lymphoma: The PRoLoG Consensus Initiative (Part 1—Clinical)
Fabien Ricard et al. · Journal of Nuclear Medicine
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14 Jul 2022 |
55 |
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Perturbed myoepithelial cell differentiation in BRCA mutation carriers and in ductal carcinoma in situ
Lina Ding et al. · Nature Communications
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13 Sep 2019 |
54 |
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Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia
Jörge E. Cortes, Moshe Talpaz, Hedy Patricia Smith et al. · Haematologica
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7 Dec 2016 |
53 |
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Clinical Activity of Ripretinib in Patients with Advanced Gastrointestinal Stromal Tumor Harboring Heterogeneous KIT/PDGFRA Mutations in the Phase III INVICTUS Study
Sebastian Bauer, Michael Charles Heinrich, Suzanne George et al. · Clinical Cancer Research
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9 Sep 2021 |
45 |
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Randomized Phase II Study Evaluating the Addition of Pembrolizumab to Radium-223 in Metastatic Castration-resistant Prostate Cancer
Atish Dipankar Choudhury et al. · Cancer Immunology Research
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29 Mar 2024 |
44 |
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Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT)
Timothy M. Caldwell, Yu Mi Ahn, Stacie L. Bulfer et al. · Bioorganic & Medicinal Chemistry Letters
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10 Aug 2022 |
44 |
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Oligomeric Benzylsulfonium Salts: Facile Benzylation via High-Load ROMP Reagents
Mianji Zhang, Daniel Lee Flynn, Paul R. Hanson · The Journal of Organic Chemistry
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Ring-Opening Metathesis Phase-Trafficking (ROMpt) Synthesis: Multistep Synthesis on Soluble ROM Supports
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40 |
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Targeting the KIT activating switch control pocket: a novel mechanism to inhibit neoplastic mast cell proliferation and mast cell activation
Yun Bai, Geethani Bandara, Eunice Ching Chan et al. · Leukemia
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31 Jul 2012 |
40 |
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The hnRNP RALY regulates transcription and cell proliferation by modulating the expression of specific factors including the proliferation marker E2F1
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3 Oct 2017 |
37 |
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Inhibition of D-2HG leads to upregulation of a proinflammatory gene signature in a novel HLA-A2/HLA-DR1 transgenic mouse model of IDH1R132H-expressing glioma
Pavlina Chuntova, Akane Yamamichi, Tiffany Chen et al. · Journal for ImmunoTherapy of Cancer
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May 2022 |
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Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region
Yu Mi Ahn, Michael Andrew Clare, Carol L. Ensinger et al. · Bioorganic & Medicinal Chemistry Letters
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4 Aug 2010 |
35 |
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Clinical Benefit of Ripretinib Dose Escalation After Disease Progression in Advanced Gastrointestinal Stromal Tumor: An Analysis of the INVICTUS Study
John Raymond Zalcberg, Michael Charles Heinrich, Suzanne George et al. · The Oncologist
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27 Jul 2021 |
34 |
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High-Load, Oligomeric Dichlorotriazine: A Versatile ROMP-Derived Reagent and Scavenger
Alan Rolfe, Donald A. Probst, Kelly A. Volp et al. · The Journal of Organic Chemistry
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21 Oct 2008 |
34 |
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Non-clinical Pharmacology of YTX-7739: a Clinical Stage Stearoyl-CoA Desaturase Inhibitor Being Developed for Parkinson’s Disease
Daniel F. Tardiff, Matthew C. Lucas, Iwona E. Wrona et al. · Molecular Neurobiology
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20 Jan 2022 |
32 |
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Ripretinib intrapatient dose escalation after disease progression provides clinically meaningful outcomes in advanced gastrointestinal stromal tumour
Suzanne George, Ping Chi, Michael Charles Heinrich et al. · European Journal of Cancer
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12 Aug 2021 |
31 |
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CSF1R Inhibition in Patients with Advanced Solid Tumors or Tenosynovial Giant Cell Tumor: A Phase I Study of Vimseltinib
Hans A. J. Gelderblom et al. · Clinical Cancer Research
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12 Jul 2024 |
30 |
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Switch Pocket Inhibitors of the ABL Tyrosine Kinase: Distinct Kinome Inhibition Profiles and in Vivo Efficacy in Mouse Models of CML and B-Lymphoblastic Leukemia Induced by BCR-ABL T315I
Richard A. Van Etten, Wayne W. Chan, Virginia M. Zaleskas et al. · Blood
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16 Nov 2008 |
27 |
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Ripretinib and MEK Inhibitors Synergize to Induce Apoptosis in Preclinical Models of GIST and Systemic Mastocytosis
Anu Gupta, Jarnail Singh, Alfonso García‐Valverde et al. · Molecular Cancer Therapeutics
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4 May 2021 |
24 |
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Ex vivo drug testing of patient-derived lung organoids to predict treatment responses for personalized medicine
Josephine Amalia Taverna, Chia‐Nung Hung, Madison H. Williams et al. · Lung Cancer
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14 Mar 2024 |
23 |
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Initial results of phase I study of DCC-2618, a broad-spectrum KIT and PDGFRa inhibitor, in patients (pts) with gastrointestinal stromal tumor (GIST) by number of prior regimens
Suzanne George, Michael Charles Heinrich, Ping Chi et al. · Annals of Oncology
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Oct 2018 |
22 |
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Inhibition of ULK1/2 and KRASG12C controls tumor growth in preclinical models of lung cancer
Phaedra C. Ghazi, Kayla T. O’Toole, Sanjana Srinivas Boggaram et al. · eLife
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30 Aug 2024 |
21 |
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System X−c Antiporter Inhibitors: Azo-Linked Amino-Naphthyl-Sulfonate Analogues of Sulfasalazine
M. Nehser, John G. Dark, D. Schweitzer et al. · Neurochemical Research
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21 Nov 2019 |
20 |
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The INSIGHT study: a randomized, Phase III study of ripretinib versus sunitinib for advanced gastrointestinal stromal tumor with KIT exon 11 + 17/18 mutations
Suzanne George, Jean‐Yves Blay, Ping Chi et al. · Future Oncology
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26 Aug 2024 |
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Opportunities and Challenges in Implementation of Multiparameter Single Cell Analysis Platforms for Clinical Translation
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2 Mar 2018 |
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1540P Ripretinib as ≥4th-line treatment in patients with advanced gastrointestinal stromal tumor: Long-term update from the phase III INVICTUS study
Margaret von Mehren, Michael Charles Heinrich, Suzanne George et al. · Annals of Oncology
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Sep 2021 |
18 |
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INVICTUS: A phase III, interventional, double-blind, placebo-controlled study to assess the safety and efficacy of ripretinib as ≥ 4th-line therapy in patients with advanced gastrointestinal stromal tumors (GIST) who have received treatment with prior anticancer therapies (NCT03353753)
Margaret von Mehren, César Serrano, Sebastian Bauer et al. · Annals of Oncology
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Oct 2019 |
18 |