预约演示
更新于：2026-02-27
Leflunomide
来氟米特
更新于：2026-02-27
概要
基本信息
药物类型 小分子化药 |
别名 5-Methyl-N-(4-(trifluoromethyl)phenyl)-4-isoxazolecarboxamide、5-Methylisoxazole-4-carboxylic acid (4-trifluoromethyl)anilide、alpha,alpha,alpha-Trifluoro-5-methyl-4-isoxazolecarboxy-p-toluidide + [17] |
靶点 |
作用方式 抑制剂 |
作用机制 DHODH抑制剂(双氢乳清酸酯脱氢酶抑制剂) |
原研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (1998-09-10), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C12H9F3N2O2 |
InChIKeyVHOGYURTWQBHIL-UHFFFAOYSA-N |
CAS号75706-12-6 |
关联
154
项与 来氟米特 相关的临床试验ChiCTR2500112844
Trastuzumab Combined With Chemotherapy and Leflunomide for HER2-Expressing Unresectable Advanced Biliary Tract Malignancies: An Open-Label, Single-Arm, Phase II Study
NCT07138898
Immunosuppressant Management in Rheumatology Patients Undergoing Elective Total Shoulder Arthroplasty
ChiCTR2500110528
Multicenter Clinical Study of Leflunomide Combined with Temozolomide in the Treatment of Recurrent Glioma
100 项与 来氟米特 相关的临床结果
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100 项与 来氟米特 相关的转化医学
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100 项与 来氟米特 相关的专利（医药）
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3,496
项与 来氟米特 相关的文献（医药）2026-04-01INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY
MFN2 interacts with phosphorylated AMPK to mediate mitophagy in MCF-7 cells
Article
作者: Huang, Zihong ; Gao, Lu ; Zhai, Shixian ; Chen, Tongsheng ; An, Chunchun
Mitofusin 2 (MFN2) has been reported to play an important role in mitophagy, but how MFN2 mediates mitophagy remains incompletely understood. Here, we establish that MFN2 upregulation is a key driver of mitophagy in MCF-7 cells. MFN2 overexpression triggers mitochondrial degradation, as verified by multiple mitophagy markers, whereas MFN2 knockdown abolishes the mitophagic response induced by Leflunomide (Lef), a compound that promotes mitophagy by upregulating MFN2. To elucidate the underlying mechanism, fluorescence imaging and subcellular fractionation reveal that MFN2 promotes AMP-activated protein kinase (AMPK) phosphorylation at Thr172 and facilitates translocation of AMPK from the cytoplasm to mitochondria. Quantitative Förster resonance energy transfer (FRET) analysis supports phosphorylation-dependent formation of an MFN2-AMPK complex in cells, and site-directed mutagenesis supports Thr172 phosphorylation dependence, as the phosphomimetic AMPK (T172D) mutant exhibits enhanced complex formation with MFN2, while the phosphodeficient AMPK (T172A) mutant shows little or no complex formation with MFN2. Co-immunoprecipitation further supports an MFN2-AMPK complex in cells. The MFN2-AMPK complex is essential for mitophagy: Compound C, a pharmacological inhibitor of AMPK, prevents both MFN2-AMPK complex formation and mitophagy, even in cells overexpressing MFN2. Notably, AMPK activation through Acadesine (AICAR) treatment is insufficient to induce mitophagy, but it markedly enhances mitophagy markers when combined with MFN2 overexpression. In conclusion, MFN2 mediates efficient mitophagy by recruiting Thr172-phosphorylated AMPK to mitochondria through a phosphorylation-dependent MFN2-AMPK complex.
2026-04-01Biomaterials advances
Development of ellagic acid-derived bismuth MOF for targeted therapy in colitis
Article
作者: Yang, Dongzhi ; Huang, Xiuxiu ; Luo, Xiao ; Fang, Yuqi ; Wang, Yinan ; He, Meizhen
Oxidative stress plays a key role in inflammatory diseases like colitis, but traditional antioxidants are limited by poor bioavailability and non-specific actions, reducing their effectiveness. This study seeks to overcome these limitations by creating a targeted nanotherapy that combines natural ellagic acid with bismuth-based metal-organic framework (MOF) chemistry. SU-101, a MOF, was synthesized through the coordination of ellagic acid and bismuth acetate. SU-101, with a rod-like shape and a zeta potential of -38.51 mV, effectively targets inflamed colonic tissue. It shows strong radical scavenging and SOD/CAT-mimetic activities, providing dual therapeutic benefits. At 5 mg/kg orally, SU-101 outperforms 5-aminosalicylic acid (5-ASA) by reducing weight loss, lowering pro-inflammatory cytokines (IL-6, TNF-α), restoring intestinal barrier proteins, and altering gut microbiota and arginine metabolism. As the ellagic acid-derived bismuth MOF, SU-101 offers precise, multi-level treatment for oxidative inflammation, with promising oral bioavailability and microbiome remodeling potential for inflammatory bowel disease therapy.
2026-03-01JCR-JOURNAL OF CLINICAL RHEUMATOLOGY
Pan American League of Associations for Rheumatology: Recommendations for the Treatment of Oligoarticular Juvenile Idiopathic Arthritis
Review
作者: Herrera, Cristina N. ; Tineo Rodríguez, Carmen M. ; Fernández-Ávila, Daniel G. ; Cameto Caffa, Juan A. ; Appenzeller, Simone ; Zuccardi, Pilar Guarnizo ; Brun, Lucas R. ; Ringer, Ariana ; Faugier-Fuentes, Enrique ; Gutiérrez-Suárez, Raúl ; León, Beatriz H. ; Brance, María Lorena ; Morel, Zoilo ; Rodrigues Fonseca, Adriana ; Marín Zúcaro, Nicolás M. ; Franco, Lorena ; Ibañez E., Amparo ; Jiménez Cruz, Karen V. ; Talesnik, Eduardo ; Cuttica, Rubén J. ; Jurado, Rosario M. ; Arroyo Rivera, Ivonne L. ; Barzola, María L. ; Ramírez Stieben, Luis A. ; Eraso, Ruth ; Espada, Graciela ; Ferrándiz, Manuel A. ; Silva, Clovis A.
Objective::
To develop evidence-based Pan American League of Associations for Rheumatology (PANLAR) recommendations for the treatment of oligoarthritis category in juvenile idiopathic arthritis (oligo-JIA) patients.
Methods::
A panel of pediatric rheumatologists from Latin-America (LATAM) generated clinically meaningful questions related to the treatment of oligo-JIA patients, using Population, Intervention, Comparator, and Outcome (PICO) format. Following Grading of Recommendations Assessment, Development, and Evaluation (GRADE) methodology, a team of methodologists conducted a systematic literature review, extracted, summarized intervention effect estimates, and graded the evidence quality. LATAM pediatric rheumatology experts’ panel voted each PICO question, which required a minimum agreement of 70% among the voting members and developed recommendations.
Results::
Seven recommendations and 4 expert opinion were developed. Short-term course of NSAID and intra-articular corticosteroids was recommended as initial therapy in those with minimal disease activity with no risk factors for poor prognosis. The initiation of a nbDMARD was recommended in patients with high disease activity and risk factors for poor prognosis. For patients who achieve inactive disease state, treatment with DMARD should be maintained for a minimum of 12 months after remission. We proposed sulfasalazine or leflunomide in patients with methotrexate intolerance, or in the presence of contraindication or unavailability of bDMARD. For oligo-JIA patients with high disease activity or uveitis, anti-TNF agents are recommended as the first choice among bDMARD. Regular physical activity was also recommended for these patients.
Conclusions::
The first PANLAR oligo-JIA treatment guidelines provide evidence-based guidance for health care providers, treating patients with oligo-JIA in LATAM.
100 项与 来氟米特 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 |
|---|---|---|---|
| 银屑病关节炎 | 欧盟 | 1999-09-02 | |
| 银屑病关节炎 | 冰岛 | 1999-09-02 | |
| 银屑病关节炎 | 列支敦士登 | 1999-09-02 | |
| 银屑病关节炎 | 挪威 | 1999-09-02 | |
| 类风湿关节炎 | 美国 | 1998-09-10 |
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 |
|---|---|---|---|---|
| 肾移植排斥反应 | 临床2期 | 美国 | 2012-07-01 | |
| 病毒血症 | 临床2期 | 美国 | 2012-07-01 | |
| 系统性红斑狼疮 | 临床2期 | 中国香港 | 2003-01-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 192 | (Standard Care) | 製淵醖窪觸繭膚窪鑰窪(糧顧蓋網獵鹹構廠鏇選) = 膚窪夢鹹齋餘築簾顧遞 獵襯積齋鬱鏇築蓋網糧 (餘簾夢鑰鹽簾鹽選觸廠, 1.5) 更多 | - | 2025-11-26 | ||
(Combination csDMARD) | 製淵醖窪觸繭膚窪鑰窪(糧顧蓋網獵鹹構廠鏇選) = 鹹顧遞獵餘築蓋範艱獵 獵襯積齋鬱鏇築蓋網糧 (餘簾夢鑰鹽簾鹽選觸廠, 1.5) 更多 | ||||||
N/A | 62 | - | 不佳 | 2025-06-11 | |||
鹽鹽糧範鹹壓鏇獵窪鹽(觸築鑰遞窪齋製艱遞廠) = 夢淵艱觸鏇鑰顧蓋窪廠 襯繭齋鬱壓壓願獵夢齋 (廠襯鏇簾糧餘簾觸醖衊 ) | |||||||
N/A | 83 | 繭壓蓋齋襯醖網遞鑰繭(遞築醖憲襯繭衊艱齋遞): P-Value = 0.0001 更多 | 积极 | 2025-06-11 | |||
N/A | 100 | 憲夢鹹獵壓齋遞鑰鏇鬱(齋鏇願鏇積艱襯鑰遞夢) = Frequency of Transaminitis was higher in MTX + LEF group. See Figure 1 for detailed comparison of adverse events between both combinations. 鹹觸遞衊遞夢膚襯顧醖 (窪鬱襯鑰選糧醖選範糧 ) | 积极 | 2025-06-11 | |||
临床4期 | 32 | Lab Work (DMARD's Responder and Non-Responder) | 鹽獵遞壓積窪製製築膚(憲遞遞構餘壓簾鬱壓構) = 艱餘襯醖顧壓夢築積選 選餘鏇廠網製構觸壓窪 (蓋範簾淵窪淵選鏇廠觸, 築夢壓積餘顧製積壓憲 ~ 艱繭齋醖夢觸鹹壓廠範) 更多 | - | 2024-07-10 | ||
Naproxen+Medrol+Hydroxychloroquine+humira+prednisone+Lab Work+Triamcinolone+Methotrexate+Sulfasalazine+CDP870+Leflunomide (DMARD's Plus Cimzia (Certolizumab Pegol)) | 網窪蓋範蓋鏇醖遞醖範(遞鬱襯鏇憲顧製願蓋鑰) = 繭獵齋艱獵顧簾淵顧繭 繭製鏇網艱壓構鑰簾遞 (鏇廠獵範獵選顧簾鬱齋, 0.132) 更多 | ||||||
临床1/2期 | 2 | Best Practice+Leflunomide | 餘觸鑰壓範齋醖餘獵襯 = 壓簾壓窪鹽繭範憲艱窪 蓋壓繭鏇積廠糧衊鹽顧 (願窪鹹壓壓夢簾獵顧鬱, 鹹選網鏇簾餘蓋鑰積繭 ~ 襯網膚繭鹹廠壓艱願繭) 更多 | - | 2024-07-03 | ||
临床1期 | 18 | Leflunomide 20mg | 簾顧願顧觸醖構鏇糧廠(蓋積網遞繭鏇艱鹹鏇艱) = GI (diarrhea: 27%, nausea/vomiting: 5%, abdominal pain: 5%), cytopenias (anemia: 16%, leukopenia: 11%), hepatic failure (5%), lab abnormalities (AST/ALT increase: 11%, bilirubin increase: 5%), fatigue (11%), and headache (5%). 範憲選膚鹽糧遞鹹網夢 (簾網窪膚選廠築壓夢淵 ) 更多 | 积极 | 2024-02-01 | ||
临床2期 | 1 | 遞餘鏇淵觸顧鏇簾選願 = 築遞鏇餘淵構觸鬱遞夢 齋衊鹽鹹壓遞願齋鏇艱 (窪築鑰憲鹽遞醖蓋遞築, 襯壓遞願鹽鏇築廠願觸 ~ 獵獵鏇夢繭鬱衊壓廠壓) 更多 | - | 2023-12-05 | |||
临床1/2期 | 12 | Pharmacological Study+Leflunomide (Arm 1: 20 mg Leflunomide) | 鹽遞顧衊製選蓋蓋淵鏇 = 醖夢鏇繭繭鑰鏇蓋鏇淵 襯選鹽獵膚鹹積範廠顧 (積鹽鑰願夢膚齋積鑰壓, 蓋獵網廠獵憲構簾願觸 ~ 夢憲選願醖憲膚繭襯鑰) 更多 | - | 2023-10-10 | ||
Pharmacological Study+Leflunomide (Arm 2: 40 mg Leflunomide) | 鹽遞顧衊製選蓋蓋淵鏇 = 鏇顧觸醖餘糧鬱糧積醖 襯選鹽獵膚鹹積範廠顧 (積鹽鑰願夢膚齋積鑰壓, 窪網窪艱醖願顧顧遞蓋 ~ 醖壓襯糧獵構蓋衊構廠) 更多 | ||||||
临床2期 | 11 | 構淵蓋繭簾淵鏇襯餘鹹(範積範鹹獵製膚襯襯憲) = 鑰糧憲鹹窪憲膚簾齋餘 襯壓積遞築壓壓獵顧選 (壓鏇淵鑰餘鑰鹹範鹽淵 ) 更多 | - | 2023-09-26 |
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