PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 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 35189270-3 2022 The impact of upadacitinib, a selective JAK1-inhibitory anti-inflammatory agent, on cisplatin-induced adverse effects, histopathologic changes, kidney and liver functions, oxidative stress, and inflammatory biomarkers were investigated compared to silymarin and losartan in male Wistar rats. upadacitinib 14-26 Janus kinase 1 Rattus norvegicus 40-44 35189270-8 2022 Upadacitinib also attenuated cisplatin-induced hepatic and renal inflammatory events, as indicated by the reduction of MDA and TNFalpha levels. upadacitinib 0-12 tumor necrosis factor Homo sapiens 127-135 35189270-11 2022 Western blotting of NF-kB and p-Akt confirmed the renoprotective effect of upadacitinib. upadacitinib 75-87 AKT serine/threonine kinase 1 Homo sapiens 32-35 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 35262646-1 2022 Importance: Primary results from the Measure Up 1 and Measure Up 2 studies demonstrated upadacitinib efficacy and safety through 16 weeks in patients with atopic dermatitis. upadacitinib 88-100 heterogeneous nuclear ribonucleoprotein A1 Homo sapiens 45-49 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 35262646-1 2022 Importance: Primary results from the Measure Up 1 and Measure Up 2 studies demonstrated upadacitinib efficacy and safety through 16 weeks in patients with atopic dermatitis. upadacitinib 88-100 uroplakin 2 Homo sapiens 62-66 35472808-0 2022 Intermediate Uveitis in an HLA-B27-Positive Patient Treated with Upadacitinib. upadacitinib 65-77 major histocompatibility complex, class I, B Homo sapiens 27-34 35142908-4 2022 The filgotinib 200 mg + MTX and upadacitinib 15 mg + MTX groups showed a significantly higher DAS28-CRP < 2.6 than adalimumab 40 mg + MTX. upadacitinib 32-44 C-reactive protein Homo sapiens 100-103 35141743-5 2022 RESULTS: Over 12 weeks, the median NNT and the median CPR to achieve DAS28-CRP remission were 4.3 and JPY 1,799,696 (USD 16,361), respectively, for upadacitinib 15mg + csDMARD. upadacitinib 148-160 C-reactive protein Homo sapiens 75-78 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 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 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 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 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 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 2 Homo sapiens 111-115 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 3 Homo sapiens 117-121 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 tyrosine kinase 2 Homo sapiens 127-144 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 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 2 Homo sapiens 99-103 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 3 Homo sapiens 105-109 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 tyrosine kinase 2 Homo sapiens 114-131 35121639-9 2022 Consistent with earlier results, herpes zoster, lymphopaenia, hepatic disorder and CPK elevation were reported at higher rates with upadacitinib versus adalimumab. upadacitinib 132-144 phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha Homo sapiens 83-86 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 34042156-11 2021 Notably, upadacitinib reversed overexpression of inflammatory fibroblast and interferon-gamma effector signature markers. upadacitinib 9-21 interferon gamma Homo sapiens 77-93 34042156-12 2021 CONCLUSIONS: Upadacitinib modulates inflammatory pathways in mucosal lesions of patients with anti-TNF-refractory Crohn"s disease, including inflammatory fibroblast and interferon-gamma-expressing cytotoxic T cell compartments. upadacitinib 13-25 tumor necrosis factor Homo sapiens 99-102 34042156-12 2021 CONCLUSIONS: Upadacitinib modulates inflammatory pathways in mucosal lesions of patients with anti-TNF-refractory Crohn"s disease, including inflammatory fibroblast and interferon-gamma-expressing cytotoxic T cell compartments. upadacitinib 13-25 interferon gamma Homo sapiens 169-185 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 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 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 2 Homo sapiens 105-109 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 3 Homo sapiens 111-115 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 tyrosine kinase 2 Homo sapiens 121-138 32648334-0 2021 Characterization of the Effect of Upadacitinib on the Pharmacokinetics of Bupropion, a Sensitive Cytochrome P450 2B6 Probe Substrate. upadacitinib 34-46 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 97-116 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 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 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 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 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 154-179 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 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 33129109-7 2021 Combinations of Upadacitinib with either AZD8055 or Sapanisertib, mTORC1/C2 inhibitors, showed anti-proliferative effects against cytokine-dependent ATL cell lines and synergistic effect with reducing tumor growth in NSG mice bearing IL-2 transgenic tumors. upadacitinib 16-28 CREB regulated transcription coactivator 1 Mus musculus 66-72 33129109-7 2021 Combinations of Upadacitinib with either AZD8055 or Sapanisertib, mTORC1/C2 inhibitors, showed anti-proliferative effects against cytokine-dependent ATL cell lines and synergistic effect with reducing tumor growth in NSG mice bearing IL-2 transgenic tumors. upadacitinib 16-28 interleukin 2 Mus musculus 234-238 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 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 interleukin 6 Homo sapiens 85-103 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 interleukin 7 Homo sapiens 108-112 33332480-6 2020 Upadacitinib has a good safety profile but it may increase the risk for herpes zoster, and as a substrate of cytochrome P450 (CYP) enzyme CYP3A4 it should not be coadministered with strong CYP3A4 inducers. upadacitinib 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 138-144 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 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 33053283-10 2020 CONCLUSIONS: In patients with rheumatoid arthritis refractory to biologic DMARDs, upadacitinib was superior to abatacept in the change from baseline in the DAS28-CRP and the achievement of remission at week 12 but was associated with more serious adverse events. upadacitinib 82-94 C-reactive protein Homo sapiens 162-165 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 32539713-5 2020 RESULTS: Treatment with JAKi (tofacitinib, baricitinib, upadacitinib) prevented GM-CSF-induced JAK2/STAT5 phosphorylation at higher concentrations (400 nM) in THP-1 cells. upadacitinib 56-68 Janus kinase 2 Homo sapiens 95-99 32367507-4 2020 While cytochrome P450 3A4-related inhibition or induction altered the exposures (area under the curve) of tofacitinib and upadacitinib, it did not impact the exposure of baricitinib. upadacitinib 122-134 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-25 32539713-5 2020 RESULTS: Treatment with JAKi (tofacitinib, baricitinib, upadacitinib) prevented GM-CSF-induced JAK2/STAT5 phosphorylation at higher concentrations (400 nM) in THP-1 cells. upadacitinib 56-68 colony stimulating factor 2 Homo sapiens 80-86 32699269-0 2020 Upadacitinib in MTX-naive RA. upadacitinib 0-12 metaxin 1 Homo sapiens 16-19 32539713-5 2020 RESULTS: Treatment with JAKi (tofacitinib, baricitinib, upadacitinib) prevented GM-CSF-induced JAK2/STAT5 phosphorylation at higher concentrations (400 nM) in THP-1 cells. upadacitinib 56-68 signal transducer and activator of transcription 5A Homo sapiens 100-105 32539713-11 2020 Although baricitinib and upadacitinib almost completely blocked GM-CSF-mediated JAK2/STAT5 signaling, the inhibitory effects of tofacitinib were weaker at lower concentrations suggesting that variation exists among these JAKi in the inhibition of JAK2 signaling pathways. upadacitinib 25-37 colony stimulating factor 2 Homo sapiens 64-70 32539713-11 2020 Although baricitinib and upadacitinib almost completely blocked GM-CSF-mediated JAK2/STAT5 signaling, the inhibitory effects of tofacitinib were weaker at lower concentrations suggesting that variation exists among these JAKi in the inhibition of JAK2 signaling pathways. upadacitinib 25-37 Janus kinase 2 Homo sapiens 80-84 32539713-11 2020 Although baricitinib and upadacitinib almost completely blocked GM-CSF-mediated JAK2/STAT5 signaling, the inhibitory effects of tofacitinib were weaker at lower concentrations suggesting that variation exists among these JAKi in the inhibition of JAK2 signaling pathways. upadacitinib 25-37 signal transducer and activator of transcription 5A Homo sapiens 85-90 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 31448433-5 2020 Upadacitinib (and tofacitinib) reversibly inhibited IL-6-induced pSTAT3 and IL-7-induced pSTAT5 in a concentration-dependent manner. upadacitinib 0-12 interleukin 6 Homo sapiens 52-56 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 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 31594037-4 2020 Upadacitinib exposures associated with 18 to 24 mg BID (IR formulation) or 45 to 60 mg QD (ER formulation) are estimated to have greater efficacy during 12-week induction in CD patients compared to lower doses. upadacitinib 0-12 BH3 interacting domain death agonist Homo sapiens 51-54 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 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 31448433-2 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 interleukin 6 Homo sapiens 77-95 31448433-5 2020 Upadacitinib (and tofacitinib) reversibly inhibited IL-6-induced pSTAT3 and IL-7-induced pSTAT5 in a concentration-dependent manner. upadacitinib 0-12 interleukin 7 Homo sapiens 76-80 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 signal transducer and activator of transcription 3 Homo sapiens 104-163 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 signal transducer and activator of transcription 3 Homo sapiens 165-170 31448433-6 2020 Model-estimated values of 50% of the maximum effect were 60.7 nM for upadacitinib and 119 nM for tofacitinib for IL-6-induced pSTAT3 inhibition, and 125 nM for upadacitinib and 79.1 nM for tofacitinib for IL-7-induced pSTAT5 inhibition. upadacitinib 69-81 interleukin 7 Homo sapiens 205-209 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 signal transducer and activator of transcription 5A Homo sapiens 214-219 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 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 3 Homo sapiens 85-89 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 3 Homo sapiens 298-302 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 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 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 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 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 132-147 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 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 149-152 31378969-6 2020 Upadacitinib 30 mg once daily (a dose that is twice the optimal dose in rheumatoid arthritis based on phase 3 results) has a limited effect on CYP3A activity (26% decrease in exposure of midazolam, a sensitive CYP3A substrate) and no relevant effects on CYP1A2, CYP2C9, CYP2C19, or CYP2D6 activity in vivo. upadacitinib 0-12 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 210-215 31378969-6 2020 Upadacitinib 30 mg once daily (a dose that is twice the optimal dose in rheumatoid arthritis based on phase 3 results) has a limited effect on CYP3A activity (26% decrease in exposure of midazolam, a sensitive CYP3A substrate) and no relevant effects on CYP1A2, CYP2C9, CYP2C19, or CYP2D6 activity in vivo. upadacitinib 0-12 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 254-260 31378969-6 2020 Upadacitinib 30 mg once daily (a dose that is twice the optimal dose in rheumatoid arthritis based on phase 3 results) has a limited effect on CYP3A activity (26% decrease in exposure of midazolam, a sensitive CYP3A substrate) and no relevant effects on CYP1A2, CYP2C9, CYP2C19, or CYP2D6 activity in vivo. upadacitinib 0-12 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 262-268 31378969-6 2020 Upadacitinib 30 mg once daily (a dose that is twice the optimal dose in rheumatoid arthritis based on phase 3 results) has a limited effect on CYP3A activity (26% decrease in exposure of midazolam, a sensitive CYP3A substrate) and no relevant effects on CYP1A2, CYP2C9, CYP2C19, or CYP2D6 activity in vivo. upadacitinib 0-12 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 270-277 31378969-6 2020 Upadacitinib 30 mg once daily (a dose that is twice the optimal dose in rheumatoid arthritis based on phase 3 results) has a limited effect on CYP3A activity (26% decrease in exposure of midazolam, a sensitive CYP3A substrate) and no relevant effects on CYP1A2, CYP2C9, CYP2C19, or CYP2D6 activity in vivo. upadacitinib 0-12 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 282-288 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 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 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 31375130-9 2019 Notably, baricitinib inhibited JAK1/3 signaling to a lesser extent than upadacitinib and tofacitinib, while upadacitinib, baricitinib, and tofacitinib inhibited the signaling of JAK2/2-dependent cytokines, including GM-CSF and IL-3, as well as the signaling of the JAK2/TYK2-dependent cytokine G-CSF. upadacitinib 108-120 Janus kinase 2 Homo sapiens 178-182 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 interleukin 4 Homo sapiens 136-140 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 interleukin 15 Homo sapiens 142-147 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 interleukin 21 Homo sapiens 153-158 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 30945116-5 2019 RESULTS: A two-compartment model with first-order absorption with lag time for the IR formulation, mixed zero- and first-order absorption with lag time for the ER formulation, and linear elimination, adequately described upadacitinib plasma concentration-time profiles. upadacitinib 221-233 epiregulin Homo sapiens 160-162 30945116-6 2019 Population estimates of upadacitinib apparent oral clearance and steady-state volume of distribution in healthy volunteers for the ER formulation were 53.7 L/h and 294 L, respectively. upadacitinib 24-36 epiregulin Homo sapiens 131-133 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 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 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 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 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 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 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 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 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 30394138-2 2019 Upadacitinib selectively inhibits Janus Kinase 1 (JAK1) which could potentially reduce JAK2 and JAK3-related side effects. upadacitinib 0-12 Janus kinase 2 Homo sapiens 87-91 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 3 Homo sapiens 96-100 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 30886973-0 2018 In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). upadacitinib 65-77 Janus kinase 1 Rattus norvegicus 45-49 30886973-4 2018 Upadacitinib (ABT-494) is a selective JAK1 inhibitor that was engineered to address the hypothesis that greater JAK1 selectivity over other JAK family members will translate into a more favorable benefit:risk profile. upadacitinib 0-12 Janus kinase 1 Rattus norvegicus 38-42 30886973-4 2018 Upadacitinib (ABT-494) is a selective JAK1 inhibitor that was engineered to address the hypothesis that greater JAK1 selectivity over other JAK family members will translate into a more favorable benefit:risk profile. upadacitinib 0-12 Janus kinase 1 Rattus norvegicus 112-116 30886973-4 2018 Upadacitinib (ABT-494) is a selective JAK1 inhibitor that was engineered to address the hypothesis that greater JAK1 selectivity over other JAK family members will translate into a more favorable benefit:risk profile. upadacitinib 14-21 Janus kinase 1 Rattus norvegicus 38-42 30886973-4 2018 Upadacitinib (ABT-494) is a selective JAK1 inhibitor that was engineered to address the hypothesis that greater JAK1 selectivity over other JAK family members will translate into a more favorable benefit:risk profile. upadacitinib 14-21 Janus kinase 1 Rattus norvegicus 112-116 30886973-5 2018 Upadacitinib selectively targets JAK1 dependent disease drivers such as IL-6 and IFNgamma, while reducing effects on reticulocytes and natural killer (NK) cells, which potentially contributed to the tolerability issues of tofacitinib. upadacitinib 0-12 Janus kinase 1 Rattus norvegicus 33-37 30886973-5 2018 Upadacitinib selectively targets JAK1 dependent disease drivers such as IL-6 and IFNgamma, while reducing effects on reticulocytes and natural killer (NK) cells, which potentially contributed to the tolerability issues of tofacitinib. upadacitinib 0-12 interleukin 6 Rattus norvegicus 72-76 30886973-5 2018 Upadacitinib selectively targets JAK1 dependent disease drivers such as IL-6 and IFNgamma, while reducing effects on reticulocytes and natural killer (NK) cells, which potentially contributed to the tolerability issues of tofacitinib. upadacitinib 0-12 interleukin 18 Rattus norvegicus 81-89 30886973-6 2018 Methods: Structure-based hypotheses were used to design the JAK1 selective inhibitor upadacitinib. upadacitinib 85-97 Janus kinase 1 Rattus norvegicus 60-64 30886973-10 2018 Results: Here, we show the structural basis for the JAK1 selectivity of upadacitinib, along with the in vitro JAK family selectivity profile and subsequent in vivo physiological consequences. upadacitinib 72-84 Janus kinase 1 Rattus norvegicus 52-56 30886973-11 2018 Upadacitinib is ~ 60 fold selective for JAK1 over JAK2, and > 100 fold selective over JAK3 in cellular assays. upadacitinib 0-12 Janus kinase 1 Rattus norvegicus 40-44 30886973-11 2018 Upadacitinib is ~ 60 fold selective for JAK1 over JAK2, and > 100 fold selective over JAK3 in cellular assays. upadacitinib 0-12 Janus kinase 2 Rattus norvegicus 50-54 30886973-11 2018 Upadacitinib is ~ 60 fold selective for JAK1 over JAK2, and > 100 fold selective over JAK3 in cellular assays. upadacitinib 0-12 Janus kinase 3 Rattus norvegicus 89-93 30886973-12 2018 While both upadacitinib and tofacitinib demonstrated efficacy in a rat model of arthritis, the increased selectivity of upadacitinib for JAK1 resulted in a reduced effect on reticulocyte deployment and NK cell depletion relative to efficacy. upadacitinib 120-132 Janus kinase 1 Rattus norvegicus 137-141 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 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 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 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 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 28503781-8 2017 Ketoconazole (strong CYP3A inhibitor) increased upadacitinib Cmax and AUC by 70% and 75%, respectively. upadacitinib 48-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-26 28503781-12 2017 CONCLUSIONS: Strong CYP3A inhibition and broad CYP induction result in a weak and moderate effect, respectively, on upadacitinib exposures. upadacitinib 116-128 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-25 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 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 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 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 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 34937767-10 2021 Upadacitinib ranked first for clinical remission in both patients naive to anti-TNF-alpha drugs (RR 0.69; 95% CI 0.61 to 0.78, P-score 0.99) and previously exposed (RR 0.78; 95% CI 0.72 to 0.85, P-score 0.99). upadacitinib 0-12 tumor necrosis factor Homo sapiens 80-89 34937767-15 2021 CONCLUSION: In a network meta-analysis, upadacitinib 45 mg once daily ranked first for clinical remission in all patients, patients naive to anti-TNF-alpha drugs and patients previously exposed. upadacitinib 40-52 tumor necrosis factor Homo sapiens 146-155 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 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 34716775-8 2021 CONCLUSION: Based on the ACR response rates, filgotinib 200 mg and upadacitinib 30 mg were the most effective, whereas tofacitinib 10 mg was the most effective treatment for PsA based on PASI75. upadacitinib 67-79 acrosin Homo sapiens 25-28 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 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 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 34471993-11 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 2 Homo sapiens 162-169 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 tyrosine kinase 2 Homo sapiens 271-275 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 34248953-11 2021 OSM-induced secretion of MCP-1 and IL-6 was inhibited by all JAKi with Peficitinib, Baricitinib and Upadacitinib showing the greatest effect. upadacitinib 100-112 C-C motif chemokine ligand 2 Homo sapiens 25-30