Indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors in clinical trials for cancer immunotherapy

Interferon-induced IDO1 mediates radiation resistance and is a therapeutic target in colorectal cancer

(2020) Baosheng Chen et al.   Cancer Immunology Research

Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2, 3-dioxygenase 1

(2020) Mingxing Hu et al.   Acta Pharmaceutica Sinica B

A phase 1 study of PF-06840003, an oral indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor in patients with recurrent malignant glioma

(2020) David A. Reardon et al.   INVESTIGATIONAL NEW DRUGS

Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to in Vivo Pharmacodynamic Activity

(2020) Marta Serafini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cell Intrinsic and Systemic Metabolism in Tumor Immunity and Immunotherapy

(2020) Michael F. Coleman et al.   Cancers

Discovery of indoximod prodrugs and characterization of clinical candidate NLG802

(2020) Sanjeev Kumar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Indoximod opposes the immunosuppressive effects mediated by IDO and TDO via modulation of AhR function and activation of mTORC1

(2020) Erik L. Brincks et al.   Oncotarget

PROTACs: New method to degrade transcription regulating proteins

(2020) Beichen Hu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

(2020) Shenxin Zeng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

PROTACs to address the challenges facing small molecule inhibitors

(2020) Pedro Martín-Acosta et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Phase 1/2 study of epacadostat in combination with ipilimumab in patients with unresectable or metastatic melanoma

(2019) Geoffrey T. Gibney et al.   Journal for ImmunoTherapy of Cancer

BMS-986205, an indoleamine 2, 3-dioxygenase 1 inhibitor (IDO1i), in combination with nivolumab (nivo): Updated safety across all tumor cohorts and efficacy in advanced bladder cancer (advBC).

(2019) Jason J. Luke et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Study of the Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Navoximod (GDC-0919) Administered with PD-L1 Inhibitor (Atezolizumab) in Advanced Solid Tumors

(2019) Kyung Hae Jung et al.   CLINICAL CANCER RESEARCH

IDO1 and Kynurenine Pathway Metabolites Activate PI3K-Akt Signaling in the Neoplastic Colon Epithelium to Promote Cancer Cell Proliferation and Inhibit Apoptosis

(2019) Kumar S. Bishnupuri et al.   CANCER RESEARCH

Discovery of Clinical Candidate (1R,4r)-4-((R)-2-((S)-6-Fluoro-5H-imidazo[5,1-a]isoindol-5-yl)-1-hydroxyethyl)cyclohexan-1-ol (Navoximod), a Potent and Selective Inhibitor of Indoleamine 2,3-Dioxygenase 1

(2019) Sanjeev Kumar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition Mechanisms of Indoleamine 2,3-Dioxygenase 1 (IDO1)

(2019) Ute F. Röhrig et al.   JOURNAL OF MEDICINAL CHEMISTRY

Epacadostat plus pembrolizumab versus placebo plus pembrolizumab in patients with unresectable or metastatic melanoma (ECHO-301/KEYNOTE-252): a phase 3, randomised, double-blind study

(2019) Georgina V Long et al.   LANCET ONCOLOGY

ENERGIZE: a Phase III study of neoadjuvant chemotherapy alone or with nivolumab with/without linrodostat mesylate for muscle-invasive bladder cancer

(2019) Guru Sonpavde et al.   Future Oncology

A multicomponent approach in the discovery of indoleamine 2,3-dioxygenase 1 inhibitors: Synthesis, biological investigation and docking studies

(2018) Alessia Griglio et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Tumor-Repopulating Cells Induce PD-1 Expression in CD8 + T Cells by Transferring Kynurenine and AhR Activation

(2018) Yuying Liu et al.   CANCER CELL

IDO1 in cancer: a Gemini of immune checkpoints

(2018) Lijie Zhai et al.   Cellular & Molecular Immunology

Indoleamine 2,3-dioxygenase 1 and programmed cell death-ligand 1 co-expression correlates with aggressive features in lung adenocarcinoma

(2018) Yuka Kozuma et al.   EUROPEAN JOURNAL OF CANCER

A patent review of IDO1 inhibitors for cancer

(2018) Jae Eun Cheong et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form

(2018) Micah T. Nelp et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting the IDO1/TDO2–KYN–AhR Pathway for Cancer Immunotherapy – Challenges and Opportunities

(2018) Jae Eun Cheong et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

A phase-1/2 study of adenovirus-p53 transduced dendritic cell vaccine in combination with indoximod in metastatic solid tumors and invasive breast cancer

(2018) Hatem Soliman et al.   Oncotarget

High Indoleamine 2,3-Dioxygenase Is Correlated With Microvessel Density and Worse Prognosis in Breast Cancer

(2018) Lijuan Wei et al.   Frontiers in Immunology

The Role of Indoleamine-2,3-Dioxygenase in Cancer Development, Diagnostics, and Therapy

(2018) Lilla Hornyák et al.   Frontiers in Immunology

Phase Ia study of the indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor navoximod (GDC-0919) in patients with recurrent advanced solid tumors

(2018) Asha Nayak-Kapoor et al.   Journal for ImmunoTherapy of Cancer

Epacadostat Plus Pembrolizumab in Patients With Advanced Solid Tumors: Phase I Results From a Multicenter, Open-Label Phase I/II Trial (ECHO-202/KEYNOTE-037)

(2018) Tara C. Mitchell et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting the IDO1 pathway in cancer: from bench to bedside

(2018) Ming Liu et al.   Journal of Hematology & Oncology

Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy

(2018) Bruno Gomes et al.   MOLECULAR CANCER THERAPEUTICS

Indoximod: An Immunometabolic Adjuvant That Empowers T Cell Activity in Cancer

(2018) Eric Fox et al.   Frontiers in Oncology

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

(2018) Thomas A. Werfel et al.   CANCER RESEARCH

Mapping the Binding Trajectory of a Suicide Inhibitor in Human Indoleamine 2,3-Dioxygenase 1

(2018) Khoa N. Pham et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

High-resolution structures of inhibitor complexes of human indoleamine 2,3-dioxygenase 1 in a new crystal form

(2018) Shukun Luo et al.   Acta Crystallographica Section F-Structural Biology Communications

Cancer immunotherapy: Opportunities and challenges in the rapidly evolving clinical landscape

(2017) Leisha A. Emens et al.   EUROPEAN JOURNAL OF CANCER

Discovery and evaluation of inhibitors to the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1 (IDO1): Probing the active site-inhibitor interactions

(2017) Petr Tomek et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate

(2017) Stefano Crosignani et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2017) Eddy W. Yue et al.   ACS Medicinal Chemistry Letters

Structural insights into substrate and inhibitor binding sites in human indoleamine 2,3-dioxygenase 1

(2017) Ariel Lewis-Ballester et al.   Nature Communications

Blockade of IDO-kynurenine-AhR metabolic circuitry abrogates IFN-γ-induced immunologic dormancy of tumor-repopulating cells

(2017) Yuying Liu et al.   Nature Communications

Epacadostat Shows Value in Two SCCHN Trials

(2017)   Cancer Discovery

Blocking IDO1 Helps Shrink Bladder, Cervical Tumors

(2017)   Cancer Discovery

Small-Molecule PROTACS: New Approaches to Protein Degradation

(2016) Momar Toure et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Determination of epacadostat, a novel IDO1 inhibitor in mouse plasma by LC-MS/MS and its application to a pharmacokinetic study in mice

(2016) Vinay Dhiman et al.   BIOMEDICAL CHROMATOGRAPHY

Safety, immune and clinical responses in metastatic melanoma patients vaccinated with a long peptide derived from indoleamine 2,3-dioxygenase in combination with ipilimumab

(2016) Jon Bjoern et al.   CYTOTHERAPY

The IDO1 selective inhibitor epacadostat enhances dendritic cell immunogenicity and lytic ability of tumor antigen-specific T cells

(2016) Caroline Jochems et al.   Oncotarget

Catalytic activity of human indoleamine 2,3-dioxygenase (hIDO1) at low oxygen

(2015) Ayodele O. Kolawole et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Immune Checkpoint Targeting in Cancer Therapy: Toward Combination Strategies with Curative Potential

(2015) Padmanee Sharma et al.   CELL

Molecular Pathways: Targeting IDO1 and Other Tryptophan Dioxygenases for Cancer Immunotherapy

(2015) L. Zhai et al.   CLINICAL CANCER RESEARCH

Role of indoleamine 2,3-dioxygenase in health and disease

(2015) Amanda W.S. Yeung et al.   CLINICAL SCIENCE

Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

(2015) Ute F. Röhrig et al.   JOURNAL OF MEDICINAL CHEMISTRY

IL-27 induces the expression of IDO and PD-L1 in human cancer cells

(2015) Grazia Carbotti et al.   Oncotarget

Cancer Immunotherapy by Targeting IDO1/TDO and Their Downstream Effectors

(2015) Michael Platten et al.   Frontiers in Immunology

Indoleamine 2,3-dioxygenase vaccination

(2015) Mads Hald Andersen et al.   OncoImmunology

Trial Watch: Peptide-based anticancer vaccines

(2015) Jonathan Pol et al.   OncoImmunology

Genentech dives deeper into the next wave of cancer immunotherapies

(2014) Sarah Crunkhorn   NATURE REVIEWS DRUG DISCOVERY

New Insights into IDO Biology in Bacterial and Viral Infections

(2014) Susanne V. Schmidt et al.   Frontiers in Immunology

Trial watch: IDO inhibitors in cancer therapy

(2014) Erika Vacchelli et al.   OncoImmunology

A Phase I study of NLG919 for adult patients with recurrent advanced solid tumors

(2014) Asha Nayak et al.   Journal for ImmunoTherapy of Cancer

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

(2014) Stefani Spranger et al.   Journal for ImmunoTherapy of Cancer

Indoleamine 2,3-dioxygenase 2 (IDO2) and the kynurenine pathway: characteristics and potential roles in health and disease

(2013) Amos A. Fatokun et al.   AMINO ACIDS

Long-lasting Disease Stabilization in the Absence of Toxicity in Metastatic Lung Cancer Patients Vaccinated with an Epitope Derived from Indoleamine 2,3 Dioxygenase

(2013) T. Z. Iversen et al.   CLINICAL CANCER RESEARCH

Oncology Meets Immunology: The Cancer-Immunity Cycle

(2013) Daniel S. Chen et al.   IMMUNITY

Indoleamine 2,3-dioxygenase is a critical resistance mechanism in antitumor T cell immunotherapy targeting CTLA-4

(2013) Rikke B. Holmgaard et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Systemic Delivery of Salmonella typhimurium Transformed with IDO shRNA Enhances Intratumoral Vector Colonization and Suppresses Tumor Growth

(2012) C. A. Blache et al.   CANCER RESEARCH

Tryptophan Catabolism in Cancer: Beyond IDO and Tryptophan Depletion

(2012) M. Platten et al.   CANCER RESEARCH

Persistent infectious diseases say – IDO. Role of indoleamine-2,3-dioxygenase in disease pathogenesis and implications for therapy

(2012) Heidi Barth et al.   CRITICAL REVIEWS IN MICROBIOLOGY

Indoleamine 2,3 dioxygenase and metabolic control of immune responses

(2012) David H. Munn et al.   TRENDS IN IMMUNOLOGY

An expanding range of targets for kynurenine metabolites of tryptophan

(2012) Trevor W. Stone et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

IDO inhibits a tryptophan sufficiency signal that stimulates mTOR: A novel IDO effector pathway targeted by D-1-methyl-tryptophan

(2012) Richard Metz et al.   OncoImmunology

The ICOS/ICOSL Pathway Is Required for Optimal Antitumor Responses Mediated by Anti-CTLA-4 Therapy

(2011) T. Fu et al.   CANCER RESEARCH

Rational Design of Indoleamine 2,3-Dioxygenase Inhibitors

(2010) Ute F. Röhrig et al.   JOURNAL OF MEDICINAL CHEMISTRY

Efficacy of Levo-1-Methyl Tryptophan and Dextro-1-Methyl Tryptophan in Reversing Indoleamine-2,3-Dioxygenase–Mediated Arrest of T-Cell Proliferation in Human Epithelial Ovarian Cancer

(2009) Feng Qian et al.   CANCER RESEARCH

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

(2009) Eddy W. Yue et al.   JOURNAL OF MEDICINAL CHEMISTRY

Monoclonal antibodies for cancer immunotherapy

(2009) Louis M Weiner et al.   LANCET