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ACS Medicinal Chemistry Letters, ISSN 1948-5875, 05/2017, Volume 8, Issue 5, pp. 486 - 491
A data-centric medicinal chemistry approach led to the invention of a potent and selective IDO1 inhibitor 4f, INCB24360 (epacadostat). The molecular structure... 
Epacadostat | data-centric medicinal chemistry | immuno-oncology | INCB24360 | IDO1
Journal Article
Clinical cancer research : an official journal of the American Association for Cancer Research, ISSN 1078-0432, 7/2017, Volume 23, Issue 13, pp. 3269 - 3276
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 11/2019, Volume 182, p. 111629
Targeting indoleamine 2,3-dioxygenase 1 (IDO1) has been identified as an attractive approach for the development of cancer immunotherapy. In this study, a... 
Epacadostat | Phosphonamidate ester | IDO2 | IDO1 inhibitors | TDO
Journal Article
Oncotarget, ISSN 1949-2553, 07/2018, Volume 9, Issue 56, pp. 30814 - 30820
Indoleamine 2,3-dioxygenase 1 (IDO1) is a new immune-oncology target and its inhibitors have shown promise in the clinic especially in combination with other... 
Epacadostat | Cell-based assay | BMS-986205 | IDO1
Journal Article
ACS MEDICINAL CHEMISTRY LETTERS, ISSN 1948-5875, 05/2017, Volume 8, Issue 5, pp. 486 - 491
A data-centric medicinal chemistry approach led to the invention of a potent and selective IDO1 inhibitor 41, INCB24360 (epacadostat). The molecular structure... 
TARGET | CHEMISTRY, MEDICINAL | INDOLEAMINE 2,3-DIOXYGENASE | DRUG DISCOVERY | Epacadostat | data-centric medicinal chemistry | TRYPTOPHAN CATABOLISM | COMBINATIONS | METABOLISM | IDO | immuno-oncology | ANTITUMOR IMMUNITY | TUMORAL IMMUNE RESISTANCE | INCB24360 | IPILIMUMAB | IDO1
Journal Article
Biochemical Pharmacology, ISSN 0006-2952, 10/2019, Volume 168, pp. 214 - 223
Targeting Trp-Kyn pathways has been identified as an attractive approach for the cancer immunotherapies. In this study, a novel phosphonamidate containing... 
Epacadostat | NSCLC | IDO1 inhibitors | Phosphonamidate | Trp-Kyn | Enzymes | Chemotherapy | Hydrogen | Analysis | Pharmacy | Immunotherapy | Tryptophan | Biological response modifiers | T cells | Interferon gamma | Cancer
Journal Article
Xenobiotica, ISSN 0049-8254, 11/2019, Volume 49, Issue 11, pp. 1338 - 1343
1. S-EPA is a sulfur-substitution analog of epacadostat (EPA), an effective small molecule indoleamine 2,3-dioxgenase1 (IDO) inhibitor. By in vitro and in vivo... 
Epacadostat | pharmacokinetics | blood cells distribution | S-EPA | pharmacodynamics | liver micosomes | PHARMACOLOGY & PHARMACY | TOXICOLOGY | 2,3-DIOXYGENASE
Journal Article
Journal of Pharmaceutical and Biomedical Analysis, ISSN 0731-7085, 06/2019, Volume 170, pp. 220 - 227
Indoleamine-2,3-dioxygénase (IDO1) is an enzyme which converts tryptophan (Trp) into kynurenine (Kyn). Having a critical role in tumor immune escape by... 
Epacadostat | Quantitative mass spectrometry imaging | Pharmacodynamics | Target exposure | Drug distribution | Indoleamine-2,3-dioxygenase | TRYPTOPHAN | PREDICTS | CHEMISTRY, ANALYTICAL | SECTIONS | REGIONAL QUANTITATIVE-DETERMINATION | DISCOVERY | LACTATE | PHARMACOLOGY & PHARMACY | H-1-MRS
Journal Article
Critical Reviews in Oncology / Hematology, ISSN 1040-8428, 01/2019, Volume 133, pp. 99 - 111
Journal Article
FRONTIERS IN IMMUNOLOGY, ISSN 1664-3224, 07/2019, Volume 10, p. 1801
Immunooncology is still a growing area in cancer therapy. Drugs within this therapeutic approach do not directly target/attack the tumor but interfere with... 
CELLS | ACID | TOLERANCE | arylhydrocarbon receptor | TRP mimetics | INDOLEAMINE 2,3-DIOXYGENASE | IDO inhibitors | IMMUNOLOGY | MTOR | IMMUNE | POTENT | ARYL-HYDROCARBON RECEPTOR | EPACADOSTAT | pharmakokinetics | EXPRESSION | immunooncology | Care and treatment | Usage | Analysis | Tryptophan | Oncology | Research | Cancer | Clinical trials
Journal Article
Gynecologic Oncology, ISSN 0090-8258, 09/2017, Volume 146, Issue 3, pp. 484 - 490
Indoleamine 2,3-dioxygenase-1 (IDO1) is a key regulator of immune tolerance in ovarian cancer. This study investigated efficacy and safety of the IDO1 enzyme... 
Epacadostat | IDO1 enzyme inhibitor | Tamoxifen | Ca-125 | Ovarian cancer | SURVIVAL | DIAGNOSIS | PROTEIN | PROGNOSIS | INDOLEAMINE 2,3-DIOXYGENASE | OBSTETRICS & GYNECOLOGY | ONCOLOGY | IMMUNOTHERAPY | EXPRESSION | T-CELLS | Recurrence | Neoplasms, Glandular and Epithelial - chemistry | Oximes - pharmacokinetics | Oximes - adverse effects | Peritoneal Neoplasms - blood | Humans | Middle Aged | Oximes - therapeutic use | Response Evaluation Criteria in Solid Tumors | Fatigue - chemically induced | Peritoneal Neoplasms - chemistry | Antineoplastic Agents, Hormonal - adverse effects | Early Termination of Clinical Trials | Fallopian Tube Neoplasms - blood | Neoplasms, Glandular and Epithelial - blood | Peritoneal Neoplasms - drug therapy | Fallopian Tube Neoplasms - chemistry | Exanthema - chemically induced | Antineoplastic Agents, Hormonal - therapeutic use | Adult | Female | Ovarian Neoplasms - drug therapy | Pruritus - chemically induced | Fallopian Tube Neoplasms - drug therapy | Drug Eruptions - etiology | Ovarian Neoplasms - chemistry | CA-125 Antigen - blood | Indoleamine-Pyrrole 2,3,-Dioxygenase - analysis | Ovarian Neoplasms - blood | Survival Rate | Sulfonamides - pharmacokinetics | Disease-Free Survival | Sulfonamides - therapeutic use | Tamoxifen - therapeutic use | Neoplasms, Glandular and Epithelial - drug therapy | Carcinoma, Ovarian Epithelial | Sulfonamides - adverse effects | Aged | Tamoxifen - adverse effects | Indoleamine-Pyrrole 2,3,-Dioxygenase - antagonists & inhibitors | Care and treatment | Chemotherapy | Enzyme inhibitors | Cancer | Medical research | Medicine, Experimental
Journal Article