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INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology

ACS medicinal chemistry letters, 2017-05, Vol.8 (5), p.486-491

2017

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Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity

Blood, 2010-04, Vol.115 (17), p.3520-3530

2010

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Characterization of human cancer xenografts in humanized mice

Journal for immunotherapy of cancer, 2020-03, Vol.8 (1), p.e000416

2020

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Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors

Molecular cancer therapeutics, 2010-02, Vol.9 (2), p.489-498

2010

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Mechanism of tumor rejection with doublets of CTLA-4, PD-1/PD-L1, or IDO blockade involves restored IL-2 production and proliferation of CD8(+) T cells directly within the tumor microenvironment

Journal for immunotherapy of cancer, 2014-01, Vol.2 (1), p.3-3

2014

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Treatment-Induced Tumor Cell Apoptosis and Secondary Necrosis Drive Tumor Progression in the Residual Tumor Microenvironment through MerTK and IDO1

Cancer research (Chicago, Ill.), 2019-01, Vol.79 (1), p.171-182

2019

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A Novel Kinase Inhibitor, INCB28060, Blocks c-MET-Dependent Signaling, Neoplastic Activities, and Cross-Talk with EGFR and HER-3

Clinical cancer research, 2011-11, Vol.17 (22), p.7127-7138

2011

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A Humanized Animal Model Predicts Clonal Evolution and Therapeutic Vulnerabilities in Myeloproliferative Neoplasms

Cancer discovery, 2021-12, Vol.11 (12), p.3126-3141

2021

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Discovery of Potent Competitive Inhibitors of Indoleamine 2,3-Dioxygenase with in Vivo Pharmacodynamic Activity and Efficacy in a Mouse Melanoma Model

Journal of medicinal chemistry, 2009-12, Vol.52 (23), p.7364-7367

2009

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Dihydroquinone Ansamycins: Toward Resolving the Conflict between Low in Vitro Affinity and High Cellular Potency of Geldanamycin Derivatives

Biochemistry (Easton), 2006-05, Vol.45 (17), p.5678-5685

2006

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INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3‑Kinase Delta (PI3Kδ)

ACS medicinal chemistry letters, 2019-11, Vol.10 (11), p.1554-1560

2019

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Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells

Journal of medicinal chemistry, 2005-02, Vol.48 (4), p.909-912

2005

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Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists

Bioorganic & medicinal chemistry letters, 2005-04, Vol.15 (7), p.1857-1861

2005

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The pan-PIM inhibitor INCB053914 displays potent synergy in combination with ruxolitinib in models of MPN

Blood advances, 2019-11, Vol.3 (22), p.3503-3514

2019

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Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo

Molecular cancer therapeutics, 2006-01, Vol.5 (1), p.160-169

2006

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The synthesis and SAR of 2-amino-pyrrolo[2,3- d]pyrimidines: A new class of Aurora-A kinase inhibitors

Bioorganic & medicinal chemistry letters, 2006-11, Vol.16 (22), p.5778-5783

2006

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Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein–protein interaction through structure-based drug design

Bioorganic & medicinal chemistry letters, 2006-06, Vol.16 (12), p.3310-3314

2006

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Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity

Bioorganic & medicinal chemistry letters, 2006-07, Vol.16 (13), p.3463-3468

2006

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Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists

Bioorganic & medicinal chemistry letters, 2006-06, Vol.16 (12), p.3115-3120

2006

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Hypoxia-mediated apoptosis from angiogenesis inhibition underlies tumor control by recombinant interleukin 12

Cancer research (Chicago, Ill.), 1999-10, Vol.59 (19), p.4882-4889

1999

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Cytokine Activation of JAK Kinases Rescues FLT3-Mutant AML from FLT3 Inhibition and Requires PIM Kinases

Blood, 2017-12, Vol.130, p.1250-1250

2017

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The Pan-PIM Inhibitor INCB053914 Displays Potent Synergy at Low Doses in Combination with Ruxolitinib in Pre-Clinical Models of MPNs

Blood, 2017-12, Vol.130, p.1661-1661

2017

Volltextzugriff (PDF)

Bromodomain and Extra Terminal Domain (BET) Inhibitors Sensitize Chronic Myelomonocytic Leukemia (CMML) to PIM Inhibition Via Downregulation of Mir-33a

Blood, 2019-11, Vol.134 (Supplement_1), p.4220-4220

2019

Volltextzugriff (PDF)

Abstract 2618: Agonist antibodies targeting OX40 and GITR enhance the activity of the IDO1-selective inhibitor epacadostat in preclinical models

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.2618-2618

2017

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Abstract 1336: Novel immunotherapeutic activity of JAK and PI3Kδ inhibitors in a model of pancreatic cancer

Cancer research (Chicago, Ill.), 2015-08, Vol.75 (15_Supplement), p.1336-1336

2015

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INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity

Characterization of human cancer xenografts in humanized mice

Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors

Mechanism of tumor rejection with doublets of CTLA-4, PD-1/PD-L1, or IDO blockade involves restored IL-2 production and proliferation of CD8(+) T cells directly within the tumor microenvironment

Treatment-Induced Tumor Cell Apoptosis and Secondary Necrosis Drive Tumor Progression in the Residual Tumor Microenvironment through MerTK and IDO1

A Novel Kinase Inhibitor, INCB28060, Blocks c-MET-Dependent Signaling, Neoplastic Activities, and Cross-Talk with EGFR and HER-3

A Humanized Animal Model Predicts Clonal Evolution and Therapeutic Vulnerabilities in Myeloproliferative Neoplasms

Discovery of Potent Competitive Inhibitors of Indoleamine 2,3-Dioxygenase with in Vivo Pharmacodynamic Activity and Efficacy in a Mouse Melanoma Model

Dihydroquinone Ansamycins: Toward Resolving the Conflict between Low in Vitro Affinity and High Cellular Potency of Geldanamycin Derivatives

INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3‑Kinase Delta (PI3Kδ)

Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells

Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists

The pan-PIM inhibitor INCB053914 displays potent synergy in combination with ruxolitinib in models of MPN

Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo

The synthesis and SAR of 2-amino-pyrrolo[2,3- d]pyrimidines: A new class of Aurora-A kinase inhibitors

Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein–protein interaction through structure-based drug design

Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity

Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists

Hypoxia-mediated apoptosis from angiogenesis inhibition underlies tumor control by recombinant interleukin 12

Cytokine Activation of JAK Kinases Rescues FLT3-Mutant AML from FLT3 Inhibition and Requires PIM Kinases

The Pan-PIM Inhibitor INCB053914 Displays Potent Synergy at Low Doses in Combination with Ruxolitinib in Pre-Clinical Models of MPNs

Bromodomain and Extra Terminal Domain (BET) Inhibitors Sensitize Chronic Myelomonocytic Leukemia (CMML) to PIM Inhibition Via Downregulation of Mir-33a

Abstract 2618: Agonist antibodies targeting OX40 and GITR enhance the activity of the IDO1-selective inhibitor epacadostat in preclinical models

Abstract 1336: Novel immunotherapeutic activity of JAK and PI3Kδ inhibitors in a model of pancreatic cancer

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