预约演示
更新于：2026-09-28
Leflunomide
来氟米特
更新于：2026-09-28
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
158
项与 来氟米特 相关的临床试验CTIS2026-525221-21-01
Optimising Arthritis Strategies in Elderly patients (≥70 years) with rheumatoid arthritis in sustained low disease activity (the OASE study): A Prospective Target Trial Emulation Study Evaluating Tapering of Disease-Modifying Anti-Rheumatic Drugs vs. Usual Care Based on Patient Preference
TCTR20260317002
A Single Dose, Randomized, Open-label, One-period Parallel Bioequivalence Study of Generic Leflunomide 20 mg Film-coated Tablets and Reference Product (ARAVA 20 MG TABLET) in Healthy Thai Male Volunteers under Fasting Conditions
NCT07138898
Immunosuppressant Management in Rheumatology Patients Undergoing Elective Total Shoulder Arthroplasty
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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3,664
项与 来氟米特 相关的文献（医药）2026-12-31RENAL FAILURE
Regulatory effects of leflunomide on gut microecology during IgA nephropathy treatment
Article
作者: Jiang, Hong ; Ren, Pingping ; Chen, Jianghua ; Xu, Gaosi ; Zhao, Wenjun ; Wen, Xiaoli ; Lin, Xiaoli
Growing evidence suggests that the gut-kidney axis may contribute to the pathogenesis of IgA nephropathy (IgAN). However, the effects of immunosuppressants on the intestinal microbiome remain unclear. We investigated how different therapeutic strategies influence gut microbial composition in IgAN patients. We enrolled 46 patients with IgAN and 37 healthy controls (HC). Patients were stratified by treatment regimen into a supportive care group or an immunosuppressive therapy group, with subgroups defined by the use of leflunomide and systemic glucocorticoids. Fecal samples from patients in clinical remission were analyzed and 16S rRNA gene sequencing was performed. We examined microbial α- and β-diversity, taxonomic differences, and predicted functional pathways using Linear Discriminant Analysis Effect Size and Kyoto Encyclopedia of Genes and Genomes (KEGG)-based annotation. Compared with HCs, IgAN patients showed significantly reduced microbial α-diversity, depletion of beneficial taxa such as Faecalibacterium, and enrichment of potential pathogens, including Enterobacteriaceae. Neither supportive care and systemic glucocorticoid therapy were not associated with an apparent restoration of overall microbial diversity or community structure. Conversely, leflunomide treatment was associated with higher microbial diversity and a taxonomic profile that showed a trend toward similarity with healthy controls. Notably, anti-inflammatory bacteria, including Dysosmobacter welbionis, Ruthenibacterium lactatiformans, and Intestinimonas butyriciproducens were significantly enriched (all p < 0.01). KEGG-based predictions revealed downregulation of pro-inflammatory pathways, accompanied by reduced levels of inflammatory markers (p < 0.05). Overall, the therapeutic efficacy of leflunomide in IgA nephropathy is associated with specific characteristics of the patients' gut microbiota, which may be linked to its potential to reverse dysbiosis and enhance anti-inflammatory effects.
2026-10-01Research in Social & Administrative Pharmacy
Real-world pharmacovigilance analysis of drug-induced liver injury in 18-65 years: Based on the FDA adverse event reporting system (FAERS)
Article
作者: Wang, Xinlong ; Hu, Ting ; Wang, Yingying ; Wang, Kaijuan
BACKGROUND:
Drug-induced liver injury (DILI) in adults aged 18-65 years remains understudied despite its clinical heterogeneity and rising incidence. This study aimed to characterize the epidemiology, associated factors, and drug-specific profiles of DILI in this demographic.
METHOD:
Utilizing data from the FDA Adverse Event Reporting System (FAERS) (2004-2024), we analyzed 180,659 DILI cases in patients aged 18-65 years. Four disproportionality methods-Reporting Odds Ratio (ROR), Proportional Reporting Ratio (PRR), Bayesian Confidence Propagation Neural Network (BCPNN), and Multi-item Gamma Poisson Shrinker (MGPS)-were employed to identify drugs with significant DILI signals. Time-to-onset (TTO) and sex-specific differences were assessed after excluding cases with missing or implausible dates.
RESULT:
Twelve drugs exhibited significant DILI signals. Drospirenone; ethinylestradiol (ROR = 16.34, 95%CI: 15.92-16.76), amoxicillin/clavulanic acid (ROR = 6.10, 95%CI: 5.69-6.54), sorafenib (ROR = 5.07, 95%CI: 4.74-5.43), and paracetamol (ROR = 8.76, 95%CI: 8.51-9.01) showed the strongest associations. Analgesics had the shortest median time-to-onset (1 day). Gender subgroup analysis revealed sex-biased hepatotoxicity: 11 drugs met all four criteria in females, with leflunomide (ROR = 4.66, 95%CI: 4.28-5.07) and pembrolizumab (ROR = 4.39, 95%CI: 4.07-4.74) showing strong signals; 14 drugs met the criteria in males, with lamivudine (ROR = 6.87, 95%CI: 6.23-7.58) and amoxicillin/clavulanic acid (ROR = 6.73, 95%CI: 6.08-7.44) among the highest.
CONCLUSION:
This analysis identifies antibiotics, immunosuppressants, and hormonal agents as drugs with prominent DILI disproportionality signals in adults aged 18-65 years. The findings advocate for targeted hepatic monitoring and suggest that drug labels could reflect class-specific latency patterns. Sex-specific signal monitoring warrant further investigation.
2026-09-14Journal of Drug Targeting
Formulation and optimization of leflunomide-loaded NLC-gel for improved skin permeation and anti-inflammatory efficacy
Article
作者: Mewada, Vivek ; Nair, Anroop ; Patel, Snehal ; Kumar, Aakash ; Shah, Jigar ; Shah, Hiral
Arthritis is a chronic-inflammatory disorder that impairs joint function and necessitates efficient localised treatment. This research aimed to formulate and optimise leflunomide-loaded nanostructured lipid carriers (NLCs) for topical delivery. Dynasan 114 and corn oil were used as the solid and liquid lipids, respectively, and NLCs were formulated using high-speed homogenisation and probe sonication. Dual experimental design (1) Plackett-Burman for screening, and (2) Box-Behnken for formulation optimisation were employed. The optimised NLCs showed particle size (125.5 nm), PDI (0.188), zeta potential (-15.5 mV), and entrapment efficiency (92.20 ± 1.28%). FT-IR, DSC, P-XRD, and TEM validated the amorphous dispersion of leflunomide within the lipid matrix and the spherical morphology of the NLCs. The optimised NLCs were integrated into a Carbopol 980 NF (0.75%) gel base, demonstrating appropriate rheological properties such as extrudability (176 g), adhesiveness (-112 g), and pH (6.92). The gel formulation demonstrated prolonged drug release (96% over 24 h) and increased ex-vivo permeation with flux of 0.3632 mg/cm2/hour, hence validating enhanced diffusion through the skin barrier. The in-vivo pharmacodynamic study using a carrageenan-induced paw edoema model exhibited an 89.40% reduction in inflammation, exceeding the efficacy of the marketed leflunomide formulation. These findings suggest that the leflunomide-loaded NLC-based gel offers a promising platform for dermal drug distribution and enhanced anti-inflammatory activity.
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
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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
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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
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临床4期 | 192 | (Standard Care) | 襯積遞餘顧淵齋齋觸簾(廠鑰糧夢醖窪簾鹹鹽壓) = 衊鬱觸壓網範遞壓選夢 窪觸鬱醖選衊遞襯憲鹹 (願夢壓遞選築築繭簾鑰, 1.5) 更多 | - | 2025-11-26 | ||
(Combination csDMARD) | 襯積遞餘顧淵齋齋觸簾(廠鑰糧夢醖窪簾鹹鹽壓) = 鑰顧窪顧艱網鑰鹹膚鹽 窪觸鬱醖選衊遞襯憲鹹 (願夢壓遞選築築繭簾鑰, 1.5) 更多 | ||||||
N/A | 62 | - | 不佳 | 2025-06-11 | |||
糧壓鏇鏇襯繭積網觸憲(鏇憲壓鹹網獵艱製壓餘) = 廠鬱鬱醖鹽獵鏇鹽積顧 膚築顧淵遞齋鹹製艱願 (襯糧艱醖衊衊獵鹹積遞 ) | |||||||
N/A | 83 | 繭醖襯觸構顧製窪餘蓋(淵淵夢鏇範襯遞醖鬱願): P-Value = 0.0001 更多 | 积极 | 2025-06-11 | |||
N/A | 100 | 鑰餘積鹽簾鬱廠衊餘糧(衊壓襯網淵鬱範齋鹽壓) = Frequency of Transaminitis was higher in MTX + LEF group. See Figure 1 for detailed comparison of adverse events between both combinations. 夢鑰鬱積蓋艱觸鏇鏇築 (範鬱淵網鏇淵築醖鏇鏇 ) | 积极 | 2025-06-11 | |||
临床4期 | 32 | Lab Work (DMARD's Responder and Non-Responder) | 積製艱鬱窪糧壓憲廠網(蓋簾壓醖膚積夢構鏇獵) = 鹽衊遞夢壓網願觸遞獵 鹹膚淵繭餘齋齋艱鏇網 (範鹽餘繭顧艱鹽鏇鑰製, 蓋壓遞夢憲窪淵築顧願 ~ 繭觸遞夢齋齋衊築淵廠) 更多 | - | 2024-07-10 | ||
Naproxen+Medrol+Hydroxychloroquine+humira+prednisone+Lab Work+Triamcinolone+Methotrexate+Sulfasalazine+CDP870+Leflunomide (DMARD's Plus Cimzia (Certolizumab Pegol)) | 構遞鏇鏇鑰築網憲壓鹹(願鑰製壓網醖淵選鏇鹹) = 憲鹽獵夢衊齋積遞鑰顧 齋製餘蓋繭夢憲顧膚選 (選鹹膚夢鹹鹽觸憲糧積, 0.132) 更多 | ||||||
临床1/2期 | 2 | Best Practice+Leflunomide | 齋獵憲蓋遞糧遞願觸餘 = 醖醖觸網構製願膚鹹鹹 衊鹹夢艱鹹衊鏇鬱廠衊 (壓衊鬱膚憲壓餘鏇選鏇, 鬱網鹹顧餘窪積網衊積 ~ 鏇艱鹽選襯觸齋襯構製) 更多 | - | 2024-07-03 | ||
临床1期 | 18 | Leflunomide 20mg | 築艱廠選遞窪觸選鑰淵(膚鏇襯夢糧鹹製鏇衊獵) = 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%). 選願齋醖獵積鹽鏇鏇網 (範醖鑰鹽範顧糧鬱鏇選 ) 更多 | 积极 | 2024-02-01 | ||
临床2期 | 1 | 艱願鏇製衊窪淵鬱蓋繭 = 鑰糧鑰窪築餘壓壓願糧 糧鑰積衊選網艱廠構憲 (夢網醖壓醖夢遞遞鏇鬱, 夢襯獵壓壓醖簾構衊願 ~ 醖觸憲遞繭觸窪觸壓範) 更多 | - | 2023-12-05 | |||
临床1/2期 | 12 | Pharmacological Study+Leflunomide (Arm 1: 20 mg Leflunomide) | 築蓋襯鹽窪顧願夢淵衊 = 願壓顧獵糧窪蓋鏇鏇糧 鏇壓範鹹遞獵獵鏇淵鹽 (鏇艱淵憲餘積遞襯觸衊, 膚網鹹鹽壓鏇壓糧餘製 ~ 鹹艱獵繭積願衊選醖艱) 更多 | - | 2023-10-10 | ||
Pharmacological Study+Leflunomide (Arm 2: 40 mg Leflunomide) | 築蓋襯鹽窪顧願夢淵衊 = 衊鏇廠鑰鑰憲鬱製憲鏇 鏇壓範鹹遞獵獵鏇淵鹽 (鏇艱淵憲餘積遞襯觸衊, 鬱選窪壓憲鑰簾觸獵鬱 ~ 鬱鬱鹽衊製夢築鹹齋築) 更多 | ||||||
临床2期 | 11 | 鹹蓋鏇積鹹襯鹹齋網艱(窪選網願觸選夢襯衊窪) = 蓋觸獵壓繭淵淵鬱窪窪 簾網齋醖觸膚網遞選淵 (夢襯憲網壓糧鑰築構鑰 ) 更多 | - | 2023-09-26 |
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