PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 34023008-1 2021 BACKGROUND: Upadacitinib is an oral Janus kinase (JAK) inhibitor with greater inhibitory potency for JAK1 than JAK2, JAK3, and tyrosine kinase 2. upadacitinib 12-24 Janus kinase 1 Homo sapiens 101-105 34042156-0 2021 Randomized Controlled Trial Substudy of Cell-specific Mechanisms of Janus Kinase 1 Inhibition With Upadacitinib in the Crohn"s Disease Intestinal Mucosa: Analysis From the CELEST Study. upadacitinib 99-111 Janus kinase 1 Homo sapiens 68-82 34042156-2 2021 We aimed to provide mechanistic insights into the JAK1-selective inhibitor upadacitinib through a transcriptomics substudy on biopsies from patients with Crohn"s disease from CELEST. upadacitinib 75-87 Janus kinase 1 Homo sapiens 50-54 34023009-2 2021 Upadacitinib is an oral Janus kinase (JAK) inhibitor with greater inhibitory potency for JAK1 than JAK2, JAK3, or tyrosine kinase 2 that is being tested for atopic dermatitis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 89-93 33527177-3 2021 Upadacitinib is a once-daily, oral Janus kinase (JAK) inhibitor with increased selectivity for JAK1 over JAK2, JAK3, and tyrosine kinase 2. upadacitinib 0-12 Janus kinase 1 Homo sapiens 95-99 33950225-1 2021 Upadacitinib and filgotinib, two JAK1 selective drugs have undergone extensive phase III clinical trials in RA and have demonstrated rapid improvements in disease activity, function and patient reported outcomes. upadacitinib 0-12 Janus kinase 1 Homo sapiens 33-37 33950228-4 2021 With this proposal, early phase trials of selective JAK1 inhibitors, namely upadacitinib, filgotinib and itacitinib, were initiated in recent years to identify the efficacy and adverse effects of these agents and to define their potential role in treatment of inflammatory and autoimmune diseases. upadacitinib 76-88 Janus kinase 1 Homo sapiens 52-56 33950228-5 2021 Early phase (Phase I-II) studies of upadacitinib and filgotinib provided evidence for efficacy and safety of the selective JAK1 inhibitors in refractory populations of RA patients and allowed informed selection of the appropriate dose by balancing the optimal benefit-risk profile for further evaluation in the later successfully performed Phase III trials. upadacitinib 36-48 Janus kinase 1 Homo sapiens 123-127 33950230-2 2021 JAK1 selective drugs, upadacitinib and filgotinib, have broadly come with the same overarching safety recommendations as other immunosuppressive drugs for RA: caution is needed regarding infection risk; monitoring for laboratory abnormalities, including lipids and muscle enzymes, is indicated. upadacitinib 22-34 Janus kinase 1 Homo sapiens 0-4 33950231-2 2021 Newer generations of Jak inhibitors, like upadacitinib and filgotinib, target Jak 1 selectively with the aim of maximizing efficacy and to improve safety. upadacitinib 42-54 Janus kinase 1 Homo sapiens 78-83 33755884-1 2021 INTRODUCTION: In the phase 2 CELEST study, positive efficacy results were obtained with the Janus kinase 1 inhibitor upadacitinib for adult patients with moderate to severe Crohn"s disease. upadacitinib 117-129 Janus kinase 1 Homo sapiens 92-106 33129109-6 2021 Here, we demonstrated that Upadacitinib, a JAK-1 inhibitor, inhibited the proliferation of cytokine-dependent ATL cell lines and the expression of p-STAT5. upadacitinib 27-39 Janus kinase 1 Homo sapiens 43-48 33156550-1 2021 Upadacitinib is a selective Janus Kinase 1 inhibitor, which was recently approved for treatment of rheumatoid arthritis (RA) and is currently being evaluated for treatment of several other autoimmune diseases, including atopic dermatitis (AD). upadacitinib 0-12 Janus kinase 1 Homo sapiens 28-42 33909185-3 2021 Upadacitinib, a JAK1 inhibitor, has also been evaluated in a phase III trial for its efficacy and safety in AS. upadacitinib 0-12 Janus kinase 1 Homo sapiens 16-20 33741556-0 2021 JAK selectivity and the implications for clinical inhibition of pharmacodynamic cytokine signalling by filgotinib, upadacitinib, tofacitinib and baricitinib. upadacitinib 115-127 Janus kinase 1 Homo sapiens 0-3 32648334-1 2021 This phase 1 study characterized the effect of multiple doses of upadacitinib, an oral Janus kinase 1 selective inhibitor, on the pharmacokinetics of the cytochrome P450 (CYP) 2B6 substrate bupropion. upadacitinib 65-77 Janus kinase 1 Homo sapiens 87-101 32776305-0 2020 Selective JAK1 Inhibitors for the Treatment of Atopic Dermatitis: Focus on Upadacitinib and Abrocitinib. upadacitinib 75-87 Janus kinase 1 Homo sapiens 10-14 32776305-7 2020 Upadacitinib and abrocitinib are oral small molecules that inhibit the JAK/STAT pathway by selectively blocking JAK1. upadacitinib 0-12 Janus kinase 1 Homo sapiens 112-116 33354610-0 2021 Bridging to a selective Janus kinase 1 inhibitor in severe atopic dermatitis: An instructive case with upadacitinib. upadacitinib 103-115 Janus kinase 1 Homo sapiens 24-38 32530345-3 2020 Upadacitinib is a JAK inhibitor engineered to be selective for JAK1, and has recently been approved for use in patients with moderate-to-severe RA. upadacitinib 0-12 Janus kinase 1 Homo sapiens 63-67 33332480-3 2020 Upadacitinib tartrate (Rinvoq), a selective and reversible JAK1 inhibitor, inhibited interleukin (IL)-6 and IL-7 and ameliorated adjuvant-induced arthritis in preclinical studies. upadacitinib 23-29 Janus kinase 1 Homo sapiens 59-63 33193430-8 2020 Currently many trials with JAKinibs are ongoing for PsA and axSpA, with one phase III trial of upadacitinib (selective JAK1 inhibitor) showing good therapeutic response in active radiographic axSpA. upadacitinib 95-107 Janus kinase 1 Homo sapiens 119-123 32515665-2 2020 New compounds under investigation, like upadacitinib, with greater selectivity for JAK1 inhibition have recently been approved for the treatment of adults with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to conventional synthetic disease-modifying antirheumatic drugs. upadacitinib 40-52 Janus kinase 1 Homo sapiens 83-87 32515665-4 2020 EXPERT OPINION: Upadacitinib was able to accomplish all the primary and secondary end points in most of the trials, with a safety profile that is similar to the other JAK inhibitors. upadacitinib 16-28 Janus kinase 1 Homo sapiens 167-170 32092309-1 2020 BACKGROUND & AIMS: We evaluated the efficacy and safety of upadacitinib, an oral selective inhibitor of Janus kinase 1, as induction therapy for ulcerative colitis (UC). upadacitinib 59-71 Janus kinase 1 Homo sapiens 104-118 31786154-2 2020 OBJECTIVE: This study evaluated the safety and efficacy of multiple doses of the selective Janus kinase 1 inhibitor upadacitinib in patients with moderate-to-severe atopic dermatitis. upadacitinib 116-128 Janus kinase 1 Homo sapiens 91-105 31701537-1 2020 Upadacitinib (ABT-494) is a selective Janus kinase (JAK)1 inhibitor being developed for treatment of several inflammatory disorders. upadacitinib 0-12 Janus kinase 1 Homo sapiens 52-57 31867699-1 2020 Upadacitinib is a Janus kinase 1 inhibitor developed for treatment of moderate to severe rheumatoid arthritis (RA) and was recently approved by the US Food and Drug Administration for this indication in adults who have had an inadequate response or intolerance to methotrexate. upadacitinib 0-12 Janus kinase 1 Homo sapiens 18-32 31448433-1 2020 Upadacitinib is a selective Janus kinase (JAK) 1 inhibitor being developed for treatment of rheumatoid arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 28-48 31448433-8 2020 This study confirms that in humans, upadacitinib has greater selectivity for JAK1 vs JAK3 relative to the rheumatoid arthritis approved dose of tofacitinib, and results from these analyses informed the selection of upadacitinib IR doses evaluated in phase 2. upadacitinib 36-48 Janus kinase 1 Homo sapiens 77-81 31448433-2 2020 This study characterizes the relationships between upadacitinib exposure and interleukin (IL)-6-induced signal transducer and activator of transcription proteins 3 (STAT3) phosphorylation (pSTAT3) and IL-7-induced STAT5 phosphorylation (pSTAT5) in the ex vivo setting as measures for JAK1 and JAK1/JAK3 inhibition, respectively, with comparison to tofacitinib. upadacitinib 51-63 Janus kinase 1 Homo sapiens 284-288 31448433-2 2020 This study characterizes the relationships between upadacitinib exposure and interleukin (IL)-6-induced signal transducer and activator of transcription proteins 3 (STAT3) phosphorylation (pSTAT3) and IL-7-induced STAT5 phosphorylation (pSTAT5) in the ex vivo setting as measures for JAK1 and JAK1/JAK3 inhibition, respectively, with comparison to tofacitinib. upadacitinib 51-63 Janus kinase 1 Homo sapiens 293-297 31732180-2 2019 This study assessed the efficacy and safety of upadacitinib, a selective JAK1 inhibitor, in patients with ankylosing spondylitis. upadacitinib 47-59 Janus kinase 1 Homo sapiens 73-77 31378969-1 2020 The aim of this study was to characterize the effects of upadacitinib, a Janus kinase 1 inhibitor, on in vivo activity of different cytochrome P450 (CYP) enzymes using a cocktail approach. upadacitinib 57-69 Janus kinase 1 Homo sapiens 73-87 30725185-1 2020 OBJECTIVES: We assessed the relative efficacy and safety of once-daily administration of 15 and 30 mg upadacitinib (a JAK1-selective inhibitor) in patients with active rheumatoid arthritis (RA). upadacitinib 102-114 Janus kinase 1 Homo sapiens 118-122 31642025-1 2019 Upadacitinib (Rinvoq ), an orally-administered Janus kinase 1 (JAK-1) inhibitor, is being developed by AbbVie for the treatment of rheumatoid arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 47-61 31791386-2 2019 We compared upadacitinib, an oral, selective JAK-1 inhibitor, with placebo to assess clinically meaningful improvements in PROs in patients with RA who have had inadequate responses to biologic disease-modifying antirheumatic drugs (bDMARD-IR). upadacitinib 12-24 Janus kinase 1 Homo sapiens 45-50 31287230-1 2019 OBJECTIVE: To evaluate the efficacy, including capacity for inhibition of radiographic progression, and safety of upadacitinib, a JAK1-selective inhibitor, as compared to placebo or adalimumab in patients with rheumatoid arthritis (RA) who have experienced an inadequate response to methotrexate (MTX). upadacitinib 114-126 Janus kinase 1 Homo sapiens 130-134 31642025-1 2019 Upadacitinib (Rinvoq ), an orally-administered Janus kinase 1 (JAK-1) inhibitor, is being developed by AbbVie for the treatment of rheumatoid arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 63-68 30973649-1 2019 Upadacitinib is a selective Janus kinase 1 inhibitor being developed for the treatment of several inflammatory autoimmune diseases, including rheumatoid arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 28-42 31654328-1 2019 Upadacitinib is a selective Janus Kinase 1 inhibitor which is being developed for the treatment of several inflammatory diseases including rheumatoid arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 28-42 31401212-6 2019 Emerging data with selective JAK1 inhibitors upadacitinib and filgotinib looks very promising. upadacitinib 45-57 Janus kinase 1 Homo sapiens 29-33 31130260-1 2019 BACKGROUND: Upadacitinib, an oral Janus kinase (JAK)1-selective inhibitor, showed efficacy in combination with stable background conventional synthetic disease-modifying antirheumatic drugs (csDMARDs) in patients with rheumatoid arthritis who had an inadequate response to DMARDs. upadacitinib 12-24 Janus kinase 1 Homo sapiens 34-53 31375130-6 2019 For example, tofacitinib and upadacitinib were the most potent inhibitors of the JAK1/3-dependent cytokines tested (interleukin [IL]-2, IL-4, IL-15, and IL-21) with lower IC50 values and increased time above IC50 translating to a greater overall inhibition of STAT signaling during the dosing interval. upadacitinib 29-41 Janus kinase 1 Homo sapiens 81-85 30945116-1 2019 BACKGROUND AND OBJECTIVES: Upadacitinib is a selective Janus kinase (JAK) 1 inhibitor being developed as an orally administered treatment for patients with moderate to severe rheumatoid arthritis (RA) and other autoimmune disorders. upadacitinib 27-39 Janus kinase 1 Homo sapiens 55-75 31317509-10 2019 Several more selective JAK-1 inhibitors, including filgotinib and upadacitinib, have also shown positive results in phase II studies and are currently enrolling in phase III development programs. upadacitinib 66-78 Janus kinase 1 Homo sapiens 23-28 30500075-1 2019 Upadacitinib is a novel selective oral Janus kinase 1 (JAK) inhibitor being developed for treatment of several inflammatory diseases. upadacitinib 0-12 Janus kinase 1 Homo sapiens 39-53 30633369-1 2019 Upadacitinib is a novel selective Janus kinase 1 inhibitor developed for treatment of rheumatoid arthritis and other autoimmune diseases. upadacitinib 0-12 Janus kinase 1 Homo sapiens 34-48 30500075-1 2019 Upadacitinib is a novel selective oral Janus kinase 1 (JAK) inhibitor being developed for treatment of several inflammatory diseases. upadacitinib 0-12 Janus kinase 1 Homo sapiens 55-58 30394138-2 2019 Upadacitinib selectively inhibits Janus Kinase 1 (JAK1) which could potentially reduce JAK2 and JAK3-related side effects. upadacitinib 0-12 Janus kinase 1 Homo sapiens 34-48 31327403-2 2019 To date, three JAK inhibitors have been tested in patients with moderate-to-severe CD: tofacitinib (pan-JAK inhibitor), filgotinib (JAK1 inhibitor) and upadacitinib (JAK1 inhibitor). upadacitinib 152-164 Janus kinase 1 Homo sapiens 166-170 30394138-8 2019 Expert commentary: Upadacitinib has displayed a rapid and favorable efficacy profile in RA but despite being a selective JAK1 inhibitor appears to have a similar safety profile to less-selective Jakinibs. upadacitinib 19-31 Janus kinase 1 Homo sapiens 121-125 30394138-2 2019 Upadacitinib selectively inhibits Janus Kinase 1 (JAK1) which could potentially reduce JAK2 and JAK3-related side effects. upadacitinib 0-12 Janus kinase 1 Homo sapiens 50-54 29908669-1 2018 BACKGROUND: Upadacitinib is a selective inhibitor of Janus kinase 1 and was efficacious in phase 2 studies in patients with moderate-to-severe rheumatoid arthritis. upadacitinib 12-24 Janus kinase 1 Homo sapiens 53-67 29076110-1 2018 BACKGROUND AND OBJECTIVES: Upadacitinib is a janus kinase (JAK) 1 inhibitor being developed for the treatment of rheumatoid arthritis (RA) and other inflammatory diseases. upadacitinib 27-39 Janus kinase 1 Homo sapiens 45-65 29908670-1 2018 BACKGROUND: Phase 2 studies with upadacitinib, a selective Janus kinase 1 (JAK1) inhibitor, have shown safety and efficacy in the treatment of patients with active rheumatoid arthritis. upadacitinib 33-45 Janus kinase 1 Homo sapiens 59-73 29908670-1 2018 BACKGROUND: Phase 2 studies with upadacitinib, a selective Janus kinase 1 (JAK1) inhibitor, have shown safety and efficacy in the treatment of patients with active rheumatoid arthritis. upadacitinib 33-45 Janus kinase 1 Homo sapiens 75-79 27272171-0 2016 Pharmacokinetics, Safety and Tolerability of ABT-494, a Novel Selective JAK 1 Inhibitor, in Healthy Volunteers and Subjects with Rheumatoid Arthritis. upadacitinib 45-52 Janus kinase 1 Homo sapiens 72-77 27389975-0 2016 A Phase IIb Study of ABT-494, a Selective JAK-1 Inhibitor, in Patients With Rheumatoid Arthritis and an Inadequate Response to Anti-Tumor Necrosis Factor Therapy. upadacitinib 21-28 Janus kinase 1 Homo sapiens 42-47 27389975-1 2016 OBJECTIVE: To compare the efficacy and safety of ABT-494, a novel selective JAK-1 inhibitor, with placebo in patients with moderate-to-severe rheumatoid arthritis (RA) and an inadequate response or intolerance to at least 1 anti-tumor necrosis factor (anti-TNF) agent. upadacitinib 49-56 Janus kinase 1 Homo sapiens 76-81 27390150-0 2016 Efficacy and Safety of ABT-494, a Selective JAK-1 Inhibitor, in a Phase IIb Study in Patients With Rheumatoid Arthritis and an Inadequate Response to Methotrexate. upadacitinib 23-30 Janus kinase 1 Homo sapiens 44-49 27390150-1 2016 OBJECTIVE: To evaluate the efficacy and safety of ABT-494, a selective JAK-1 inhibitor, in patients with moderate-to-severe rheumatoid arthritis (RA) and an inadequate response to methotrexate (MTX). upadacitinib 50-57 Janus kinase 1 Homo sapiens 71-76 28762476-3 2018 Upadacitinib is a Janus kinase 1 inhibitor currently being evaluated in phase III rheumatoid arthritis trials. upadacitinib 0-12 Janus kinase 1 Homo sapiens 18-32 28503781-0 2017 Assessment of effect of CYP3A inhibition, CYP induction, OATP1B inhibition, and high-fat meal on pharmacokinetics of the JAK1 inhibitor upadacitinib. upadacitinib 136-148 Janus kinase 1 Homo sapiens 121-125 27272171-1 2016 BACKGROUND: ABT-494 is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders, with potential for an improved safety profile compared with non-selective JAK inhibitors. upadacitinib 12-19 Janus kinase 1 Homo sapiens 46-66 34659493-4 2021 Upadacitinib, a JAK 1 selective molecule developed in this context has been evaluated in the SELECT phase-III study program and demonstrated a high and rapid efficacy in monotherapy as well as in combination with csDMARDs both in csDMARD-naive RA patients and in patients refractory to csDMARD and bDMARD treatments. upadacitinib 0-12 Janus kinase 1 Homo sapiens 16-21 34761860-0 2021 Alleviation of erosive oral and esophageal lichen planus by the JAK1 inhibitor upadacitinib. upadacitinib 79-91 Janus kinase 1 Homo sapiens 64-68 34871917-0 2022 Quantification of the janus kinase 1 inhibitor upadacitinib in human plasma by LC-MS/MS. upadacitinib 47-59 Janus kinase 1 Homo sapiens 22-36 34871917-1 2022 Upadacitinib is a selective janus-kinase-1 inhibitor effective in the treatment of autoimmune related diseases like rheumatoid arthritis or psoriatic arthritis. upadacitinib 0-12 Janus kinase 1 Homo sapiens 28-42 34645316-1 2021 Upadacitinib, a selective JAK 1 inhibitor, has been evaluated for efficacy and safety in the treatment of psoriatic arthritis (PsA). upadacitinib 0-12 Janus kinase 1 Homo sapiens 26-31 34894197-0 2021 Besserung eines oralen und osophagealen Lichen ruber mucosae unter dem JAK1-Inhibitor Upadacitinib. upadacitinib 86-98 Janus kinase 1 Homo sapiens 71-75 34514265-4 2021 In this work, GraphGMVAE was validated by rapidly hopping the scaffold from FDA-approved upadacitinib, which is an inhibitor of human Janus kinase 1 (JAK1), to generate more potent molecules with novel chemical scaffolds. upadacitinib 89-101 Janus kinase 1 Homo sapiens 134-148 34629864-1 2021 Background: Upadacitinib, a novel selective Janus kinase 1 (JAK1) inhibitor, has been recently approved by the US FDA for the treatment of adult patients with moderately to severely active rheumatoid arthritis (RA). upadacitinib 12-24 Janus kinase 1 Homo sapiens 44-58 34629864-1 2021 Background: Upadacitinib, a novel selective Janus kinase 1 (JAK1) inhibitor, has been recently approved by the US FDA for the treatment of adult patients with moderately to severely active rheumatoid arthritis (RA). upadacitinib 12-24 Janus kinase 1 Homo sapiens 60-64 34471993-6 2021 Concentrations providing half-maximal inhibition (IC50) in these assays were determined for deucravacitinib and the JAK 1/2/3 inhibitors tofacitinib, upadacitinib, and baricitinib. upadacitinib 150-162 Janus kinase 1 Homo sapiens 116-125 34471993-11 2021 Simulations indicated that tofacitinib, upadacitinib, and baricitinib at steady state exhibited varying degrees of JAK 1/3 (daily average inhibition, 70-94%) and JAK 2/2 (23%-67%) inhibition at therapeutic concentrations, with Cmax values 17- to 33-fold lower than their TYK2 IC50 levels. upadacitinib 40-52 Janus kinase 1 Homo sapiens 115-122 34471993-13 2021 Tofacitinib, upadacitinib, and baricitinib variably inhibit JAK 1/2/3 but not TYK2. upadacitinib 13-25 Janus kinase 1 Homo sapiens 60-69 34532638-5 2021 The clinical development program of the JAK1 selective inhibitors upadacitinib and abrocitinib is finalized with positive results for AD. upadacitinib 66-78 Janus kinase 1 Homo sapiens 40-44 34514265-4 2021 In this work, GraphGMVAE was validated by rapidly hopping the scaffold from FDA-approved upadacitinib, which is an inhibitor of human Janus kinase 1 (JAK1), to generate more potent molecules with novel chemical scaffolds. upadacitinib 89-101 Janus kinase 1 Homo sapiens 150-154 35437207-10 2022 Dexamethasone (a corticosteroid) significantly inhibited, while ABT494 (a JAK1 inhibitor) partially inhibited, EKH"s induction of cytokines in fibroblasts. upadacitinib 64-70 Janus kinase 1 Homo sapiens 74-78 35446502-0 2022 Ansprechen eines mit rheumatoider Arthritis assoziierten Pyoderma gangraenosum auf den JAK1-Inhibitor Upadacitinib. upadacitinib 102-114 Janus kinase 1 Homo sapiens 87-91 35267240-0 2022 Response of rheumatoid arthritis-associated pyoderma gangrenous to the JAK1 inhibitor upadacitinib. upadacitinib 86-98 Janus kinase 1 Homo sapiens 71-75 35014922-4 2022 AREAS COVERED: This paper explores the use of upadacitinib (a selective JAK1 inhibitor) for the treatment of psoriatic arthritis. upadacitinib 46-58 Janus kinase 1 Homo sapiens 72-76 35224383-6 2022 In the current study, we investigated the mechanism of binding of baricitinib, filgotinib, itacitinib, and upadacitinib to JAK1 using a combined method of molecular docking, molecular dynamics simulation, and binding free energy calculation via the molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) scheme. upadacitinib 107-119 Janus kinase 1 Homo sapiens 123-127 35224383-8 2022 Due to the increased favorable intermolecular electrostatic contribution, upadacitinib is more selective to JAK1 compared to the other three inhibitors. upadacitinib 74-86 Janus kinase 1 Homo sapiens 108-112