Thomas H. Marsilje

Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors

Yong Jia, Cai‐Hong Yun, Eunyoung Park et al. · Nature · 2016 · 851 citations · Full text

Molecular Pharmacology, Medicine, Pharmacology +4

Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro-<i>N</i>2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-<i>N</i>4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

Thomas H. Marsilje, Wei Pei, Bei Chen et al. · Journal of Medicinal Chemistry · 2013 · 405 citations · Full text

Chemoprevention Strategy, Pharmacotherapy, Structure–activity Relationships +21

EGF816 Exerts Anticancer Effects in Non–Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor

Yong Jia, Jose Juarez, Jie Li et al. · Cancer Research · 2016 · 120 citations · Full text

Discovery of (<i>R</i>,<i>E</i>)-<i>N</i>-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1<i>H</i>-benzo[<i>d</i>]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers

G. Lelais, Robert Epple, Thomas H. Marsilje et al. · Journal of Medicinal Chemistry · 2016 · 94 citations · Full text

Tumor Biology, Good Wt-egfr Selectivity, New Therapies +17

A Blueprint to Advance Colorectal Cancer Immunotherapies

Dung T. Le, Vanessa M. Hubbard-Lucey, Michael A. Morse et al. · Cancer Immunology Research · 2017 · 71 citations · Full text