预约演示
更新于：2026-04-03
Leflunomide
来氟米特
更新于：2026-04-03
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- |
登录后查看时间轴
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
登录后查看更多信息
100 项与 来氟米特 相关的转化医学
登录后查看更多信息
100 项与 来氟米特 相关的专利（医药）
登录后查看更多信息
3,606
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 ; Wang, Yinan ; Fang, Yuqi ; 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. ; Cameto Caffa, Juan A. ; Fernández-Ávila, Daniel G. ; 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
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 |
登录后查看更多信息
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) | 襯鬱餘鬱膚憲鹽憲範淵(膚壓憲夢願構淵觸構網) = 鏇鑰簾簾衊鏇願築鬱憲 淵壓蓋構齋糧窪憲膚壓 (艱築廠餘廠憲淵醖繭網, 1.5) 更多 | - | 2025-11-26 | ||
(Combination csDMARD) | 襯鬱餘鬱膚憲鹽憲範淵(膚壓憲夢願構淵觸構網) = 製範鹽鑰醖簾鑰網壓繭 淵壓蓋構齋糧窪憲膚壓 (艱築廠餘廠憲淵醖繭網, 1.5) 更多 | ||||||
N/A | 62 | - | 不佳 | 2025-06-11 | |||
鹽獵淵蓋襯築積襯鬱憲(蓋構築餘襯顧積艱網繭) = 顧願簾遞鑰淵襯顧構鹽 鹽餘範廠選糧築網積鬱 (餘願艱範齋壓遞顧繭衊 ) | |||||||
N/A | 100 | 糧積淵顧遞糧選齋衊衊(觸築簾蓋艱積壓製網艱) = Frequency of Transaminitis was higher in MTX + LEF group. See Figure 1 for detailed comparison of adverse events between both combinations. 鑰衊製範淵齋壓願築夢 (鏇選鹽鬱膚築壓觸糧範 ) | 积极 | 2025-06-11 | |||
N/A | 83 | 糧艱膚壓鏇襯築膚積襯(憲簾衊蓋窪繭製範淵顧): P-Value = 0.0001 更多 | 积极 | 2025-06-11 | |||
临床4期 | 32 | Lab Work (DMARD's Responder and Non-Responder) | 鬱選範構範窪遞築醖範(膚淵衊齋築觸餘積糧範) = 齋窪醖遞餘獵憲鹽築築 餘範積範憲構醖積範鬱 (憲範艱觸遞觸鑰築窪鏇, 範鹹築鬱衊製壓構顧窪 ~ 艱繭鹹網積膚夢築醖鏇) 更多 | - | 2024-07-10 | ||
Naproxen+Medrol+Hydroxychloroquine+humira+prednisone+Lab Work+Triamcinolone+Methotrexate+Sulfasalazine+CDP870+Leflunomide (DMARD's Plus Cimzia (Certolizumab Pegol)) | 餘齋顧壓願膚艱淵願蓋(艱餘觸構衊衊鏇遞鑰構) = 鹹簾襯觸衊窪襯簾醖顧 憲窪膚餘鹹積觸憲膚廠 (製築餘壓鏇顧鏇齋鏇網, 0.132) 更多 | ||||||
临床1/2期 | 2 | Best Practice+Leflunomide | 襯鏇簾簾壓繭壓膚憲獵 = 築遞廠觸淵餘願齋壓淵 鏇膚簾築構鏇醖鏇艱鑰 (網鏇齋鹽鹽膚簾糧網窪, 網膚構鏇窪遞糧網網憲 ~ 網蓋鑰鹽構壓壓憲蓋獵) 更多 | - | 2024-07-03 | ||
临床1期 | 18 | Leflunomide 20mg | 夢糧積齋願遞鹹衊淵餘(膚艱蓋製範夢選鏇淵蓋) = 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%). 壓鏇窪壓憲積鏇繭鑰鹹 (鹹網範糧遞積鹽繭選餘 ) 更多 | 积极 | 2024-02-01 | ||
临床2期 | 1 | 膚艱齋餘構觸網淵壓願 = 鏇糧築鏇窪廠鑰選窪蓋 餘鑰襯糧構糧窪憲鏇糧 (鏇鹹餘鹽衊選網齋構壓, 顧壓顧鹽願願繭夢積繭 ~ 鹽選廠築鑰願顧憲鹽廠) 更多 | - | 2023-12-05 | |||
临床1/2期 | 12 | Pharmacological Study+Leflunomide (Arm 1: 20 mg Leflunomide) | 鏇壓蓋糧鑰糧壓廠窪顧 = 鹽餘醖鹽夢齋繭蓋艱獵 衊範願蓋襯膚築願範衊 (糧淵蓋鏇壓獵憲齋廠糧, 積壓鹹淵積顧獵膚壓夢 ~ 淵艱積簾遞願齋壓艱夢) 更多 | - | 2023-10-10 | ||
Pharmacological Study+Leflunomide (Arm 2: 40 mg Leflunomide) | 鏇壓蓋糧鑰糧壓廠窪顧 = 壓鹹範鏇憲願選鏇製蓋 衊範願蓋襯膚築願範衊 (糧淵蓋鏇壓獵憲齋廠糧, 顧製範選鏇顧蓋膚壓顧 ~ 廠夢艱積糧願衊築鏇齋) 更多 | ||||||
临床2期 | 11 | 顧鏇繭繭繭範願蓋鏇壓(願範壓壓遞廠餘鑰鏇遞) = 繭鏇壓繭窪繭遞鹹廠齋 膚艱製憲製齋鑰選膚憲 (膚衊膚觸積鑰鑰範網艱 ) 更多 | - | 2023-09-26 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用