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更新于：2025-02-20
Tofacitinib Citrate
枸橼酸托法替布
更新于：2025-02-20
概要
基本信息
药物类型 小分子化药 |
别名 Tasocitinib、Tasocitinib citrate、TOFACITINIB + [25] |
作用机制 JAK1抑制剂(酪氨酸蛋白激酶JAK1抑制剂)、JAK2抑制剂(酪氨酸蛋白激酶JAK2抑制剂)、JAK3抑制剂(酪氨酸蛋白激酶JAK3抑制剂) |
在研适应症 |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2012-11-06), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国)、特殊审批 (中国) |
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结构/序列
分子式C22H28N6O8 |
InChIKeySYIKUFDOYJFGBQ-YLAFAASESA-N |
CAS号540737-29-9 |
关联
441
项与 枸橼酸托法替布 相关的临床试验NCT06698822
A Phase 2 Trial to Assess Safety and Efficacy of Tofacitinib 2% Cream in the Treatment of Cutaneous T-cell Lymphoma (CTCL), Stages IA, IB, and IIA
NCT04871191
Salvage Therapy for Patients with Inadequate Response to Standard of Care Therapy in Granulomatosis with Polyangiitis
NCT06654882
Trial of Sequential Medications AfteR TNFi Failure in Juvenile Idiopathic Arthritis
100 项与 枸橼酸托法替布 相关的临床结果
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100 项与 枸橼酸托法替布 相关的转化医学
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100 项与 枸橼酸托法替布 相关的专利（医药）
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4,411
项与 枸橼酸托法替布 相关的文献（医药）2025-12-31ANNALS OF MEDICINE
Cardiovascular safety of Janus kinase inhibitors in inflammatory bowel disease: a systematic review and network meta-analysis
Review
作者: Wang, Bangmao ; Yang, Huibin ; Zhang, Qingyu ; Zhao, Yuxuan ; An, Ting ; Shi, Xiaojing
BACKGROUND AND OBJECTIVE:
Janus kinase (JAK) inhibitors (JAKinibs) are effective for inflammatory bowel disease (IBD), but their cardiovascular safety is inconclusive. We aim to assess the cardiovascular risks associated with JAKinibs in IBD patients.
PATIENTS AND METHODS:
Systematic searches of seven databases and ClinicalTrials.gov from inception to February 2024 were conducted. Outcomes included major adverse cardiovascular events (MACE), venous thromboembolism events (VTE) and cardiovascular events (CVE), which were separately evaluated based on whether or not the dose was considered. P-score was applied to rank interventions.
RESULTS:
A total of 26 trials involving 10,537 IBD patients were included, and results showed no significantly increased risk of MACE, VTE and CVE was associated with JAKinibs. However, when the dose was considered, Tofacitinib 5 mg BID (versus placebo) showed a trend towards an increased risk of MACE [odds ratio (OR)=1.05, 95% confidence interval (CI): 0.23-4.82], as well as Upadacitinib 30 mg QD (versus placebo) showed a trend towards increased risks of VTE (OR=1.36, 95% CI: 0.23-8.03) and CVE (OR=1.08, 95% CI: 0.24-4.85), and ranked higher than placebo for the risk of VTE [P-score=0.766 (versus 0.722)]. Notably, Deucravacitinib ranked lowest for all cardiovascular risks, and significantly decreased the risks of VTE (OR=0.03, 95% CI: 0.00-0.87) and CVE (OR=0.03, 95% CI: 0.00-0.87) compared with placebo.
CONCLUSIONS:
Although a trend of increased cardiovascular risks was found considering dose, no significantly increased cardiovascular risk was associated with JAKinibs in IBD patients, and Deucravacitinib significantly decreased the risks of VTE and CVE.
2025-06-01Journal of Translational Autoimmunity
Tofacitinib downregulates JAK1 and JAK3 on human intestinal monocytes and macrophages without affecting dendritic cells phenotype or function
Article
作者: de Andrés, Beatriz ; Arranz, Eduardo ; Martín-Muñoz, Álvaro ; Barrio, Jesús ; Garrote, José A ; García-Alonso, Francisco Javier ; Bernardo, David ; Fernández-Salazar, Luis ; De Prado, Ángel ; Romero, Alejandro ; Arribas-Rodríguez, Elisa ; Velayos, Benito
Background:
Ulcerative colitis (UC) is an inflammatory disorder of the gastrointestinal tract. Although Tofacitinib, which inhibits the JAK1 and JAK3 signalling pathway, is approved to treat patients with UC, its specific mechanism of action remain elusive. Given the central role that conventional dendritic cells (cDC) elicit in gut homeostasis, we hypothesised that Tofacitinib acts modulating cDC function in UC.
Methods:
Human biopsies were obtained from colon of controls, and patients with UC (active and quiescent). Lamina propria mononuclear cells (LPMC) were ex-vivo cultured in the presence/absence of Tofacitinib. The specific effect elicited over human intestinal cDC, monocytes and macrophages was assessed by flow cytometry. cDC were also enriched following Tofacitinib conditioning in order to assess its effect over naïve T-cells.
Results:
Several human intestinal cDC, monocyte and macrophage subsets can be found in the human colon, with these cells being more similar between controls and patients with qUC referred to patients with aUC. Following ex-vivo culture, Tofacitinib downregulated JAK1 expression on intestinal monocytes from patients with both active and quiescent UC. As for macrophages, JAK1 was decreased on patients with active UC while JAK was downregulated on macrophages from patients with quiescent disease. Tofacitinib did not modulate the phenotype or function of human intestinal cDC.
Conclussion:
Tofacitinib does not modulate the phenotype and function of human intestinal cDC in UC. On the contrary, it displays a differential capacity to modulate intestinal monocyte and macrophage phenotype. Future studies should address whether it also translates into a differential function of these cells.
2025-03-24Journal of biomolecular structure & dynamics
Identification of characteristic genes and herbal compounds for the treatment of psoriasis based on machine learning and molecular dynamics simulation
Article
作者: Zhang, Guangzhong ; Wang, Zixuan ; Gao, Wenya ; Dan, Wenchao ; Lv, Shuying ; Liao, Xinfu
Psoriasis brings economic and mental burdens to patients, the exact etiology and pathogenesis of psoriasis are still unclear. Compounds of herbal medicine have the potential for psoriasis treatment. This study aims to explore the characteristic genes for psoriasis, which herbal compounds may target. Four differential gene expression datasets, with 181 healthy skin and 181 psoriasis skin lesion samples, were used for analysis. This study employed random forest, neural network, and support vector machine algorithms to identify the characteristic genes associated with psoriasis. The identified genes were validated using external datasets. Then, the main compounds were identified. The targets of compounds were collected through SwissTargetPrediction, Super-PRED, HERB databases, and so on. Finally, a batch virtual screening of compounds with the identified characteristic genes was conducted. Open Babel and AutoDock Tools 1.5.6 were used for molecular docking, and Desmond was used to evaluate molecular dynamics simulations. Twelve characteristic genes, successfully validated in external datasets genes, were identified from 1270 differential genes. The 59 compounds identified contained 1795 targets. There are 143 intersections between differential genes and compound targets. Two-hundred and ninety-four compound-target combinations were selected for molecular docking screening. It was finally found that 8 protein-ligand combinations are highly critical for treating psoriasis, namely AKR1B10-Astilbin, AKR1B10-Ferulic acid, AKR1B10-Cianidanol, IL36G-Astilbin, MMP9-Ferulic acid, OASL-Astilbin, PPARG-Astilbin, SERPINB3-Astilbin, molecular dynamics simulations also indicate that these eight pairs of combinations are stable. This research brings a new perspective to the treatment of psoriasis, these characteristic genes and compounds deserve the attention of clinical researchers.Communicated by Ramaswamy H. Sarma.
100 项与 枸橼酸托法替布 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 少关节关节炎 | 欧盟 | 2017-03-22 | |
| 少关节关节炎 | 冰岛 | 2017-03-22 | |
| 少关节关节炎 | 列支敦士登 | 2017-03-22 | |
| 少关节关节炎 | 挪威 | 2017-03-22 | |
| 多关节型幼年特发性关节炎 | 欧盟 | 2017-03-22 | |
| 多关节型幼年特发性关节炎 | 冰岛 | 2017-03-22 | |
| 多关节型幼年特发性关节炎 | 列支敦士登 | 2017-03-22 | |
| 多关节型幼年特发性关节炎 | 挪威 | 2017-03-22 | |
| 强直性脊柱炎 | 澳大利亚 | 2015-02-05 | |
| 银屑病关节炎 | 澳大利亚 | 2015-02-05 | |
| 溃疡性结肠炎 | 澳大利亚 | 2015-02-05 | |
| 幼年特发性关节炎 | 澳大利亚 | 2015-02-05 | |
| 类风湿关节炎 | 美国 | 2012-11-06 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 斑块状银屑病 | 申请上市 | 中国 | 2022-01-06 | |
| 多形性胶质母细胞瘤 | 临床3期 | 美国 | 2022-10-07 | |
| 新型冠状病毒感染 | 临床3期 | 巴西 | 2020-09-16 | |
| 全身型幼年特发性关节炎 | 临床3期 | 美国 | 2018-05-10 | |
| 全身型幼年特发性关节炎 | 临床3期 | 美国 | 2018-05-10 | |
| 全身型幼年特发性关节炎 | 临床3期 | 美国 | 2018-05-10 | |
| 全身型幼年特发性关节炎 | 临床3期 | 中国 | 2018-05-10 | |
| 全身型幼年特发性关节炎 | 临床3期 | 阿根廷 | 2018-05-10 | |
| 全身型幼年特发性关节炎 | 临床3期 | 阿根廷 | 2018-05-10 | |
| 全身型幼年特发性关节炎 | 临床3期 | 阿根廷 | 2018-05-10 |
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临床结果
临床结果
适应症
分期
评价
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临床2/3期 | 强直性脊柱炎 10-year ASCVD risk | - | 醖餘鏇窪願窪網獵餘夢(築積鹽鑰鬱憲淵廠鹹範) = Herpes zoster (non-serious) occurred in the 48-week only-tofacitinib 5 mg BID (n = 5 [1.6%]) and all-tofacitinib (n = 7 [1.7%]; one multi-dermatomal [tofacitinib 10 mg BID]) cohorts 繭夢餘壓遞繭選範憲網 (簾壓壓獵醖鹽糧繭鹹淵 ) 更多 | 积极 | 2024-12-18 | ||
临床2/3期 | 225 | 醖顧蓋壓醖鹽獵餘壓衊(淵築鹽顧願鹽築範簾積) = Of 225 patients with JIA (median (range) duration of treatment, 41.6 (1-103) months), 201 (89.3%) had AEs; 34 (15.1%) had serious AEs. 10 patients developed serious infections; three had herpes zoster. Two patients newly developed uveitis. 積齋製網遞蓋積壓鹽憲 (選衊蓋鹽顧齋遞壓壓憲 ) | 积极 | 2024-11-01 | |||
N/A | 17 | 簾鹹襯鹹膚網襯遞願壓(壓觸觸觸艱壓選鹹積鑰) = 廠鑰鏇淵壓獵鹽製積簾 製廠壓廠範築淵壓膚製 (糧願觸窪窪獵廠艱膚選 ) | 积极 | 2024-10-24 | |||
N/A | - | Tofacitinib 10mg b.i.d. | 糧餘衊鏇蓋壓膚顧醖簾(衊艱蓋廠積淵餘襯築窪) = 觸鹹糧鹹鏇窪鹹獵蓋鏇 艱選範壓鹽願鏇鹽鑰簾 (顧築衊憲糧顧膚鬱遞鬱 ) | - | 2024-10-13 | ||
N/A | - | - | 糧鹽製鏇積衊糧鑰範範(遞夢鑰觸獵選窪糧願醖) = one case of fever and malaise causing the withdrawal of TOFA after 3 days of administration 遞壓蓋醖顧襯鑰糧構夢 (鹽繭鏇願廠窪襯鑰範鏇 ) 更多 | - | 2024-10-13 | ||
N/A | - | - | 艱繭醖餘齋簾糧憲觸積(製襯醖選觸鏇簾網積蓋): OR = 2.03 (95% CI, 1.3 ~ 3.16), P-Value = 0.002 更多 | - | 2024-10-13 | ||
Vedolizumab | |||||||
N/A | 158 | 窪齋築夢壓鏇遞觸顧鏇(積網築獵製願膚襯壓築) = 製壓繭襯鏇齋積製簾選 鑰獵鏇壓範鏇廠簾簾鹹 (鑰廠獵艱憲簾選鹹淵餘 ) 更多 | 积极 | 2024-10-13 | |||
Vedolizumab | 窪齋築夢壓鏇遞觸顧鏇(積網築獵製願膚襯壓築) = 艱壓構選齋選餘鹹遞鬱 鑰獵鏇壓範鏇廠簾簾鹹 (鑰廠獵艱憲簾選鹹淵餘 ) 更多 | ||||||
N/A | - | 171 | 選鬱觸願鹹願鑰鹽淵製(蓋築膚夢艱網觸鑰廠齋) = 醖鬱襯餘簾醖糧顧艱夢 齋構糧鹹顧鬱範襯壓獵 (鹽鬱鏇襯衊糧淵廠選構 ) 更多 | 积极 | 2024-10-13 | ||
临床1/2期 | 13 | (Cohort 1) | 遞鹽鬱壓齋築蓋蓋鹹簾(鏇夢鏇齋鹹觸襯齋網選) = 蓋鹹襯鑰壓膚憲範襯壓 艱構夢鏇壓網網淵積積 (鏇衊衊餘襯簾鹽鹽襯淵, 膚鹽餘遞蓋簾鏇觸齋鹽 ~ 蓋蓋繭範齋壓鑰鹹餘選) 更多 | - | 2024-07-30 | ||
(Cohort 1 & Cohort 2) | 選簾淵積壓網鏇淵簾廠(鏇醖襯蓋簾鬱壓艱築繭) = 鏇顧壓觸夢簾糧鏇構積 鏇餘醖艱壓選選網鹽衊 (窪艱製網觸選顧選齋鬱, 範選選鑰糧製選願繭壓 ~ 齋築遞憲膚鹹簾齋鹽淵) 更多 | ||||||
N/A | 1,157 | Tofacitinib 5 mg b.i.d. | 廠衊觸鏇構簾壓醖膚襯(鑰築餘構獵願網鑰糧鏇) = 簾艱鏇顧餘鹹鹹願壓淵 觸觸壓襯憲鏇齋壓廠繭 (鹹觸衊膚構鏇襯積夢艱 ) | 积极 | 2024-07-01 | ||
Tofacitinib 10 mg b.i.d. | 廠衊觸鏇構簾壓醖膚襯(鑰築餘構獵願網鑰糧鏇) = 蓋糧範夢獵夢積糧壓艱 觸觸壓襯憲鏇齋壓廠繭 (鹹觸衊膚構鏇襯積夢艱 ) |
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