更新于：2024-11-15
Leflunomide
来氟米特
更新于：2024-11-15
概要
基本信息
原研机构 |
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
分子式C12H9F3N2O2 |
InChIKeyVHOGYURTWQBHIL-UHFFFAOYSA-N |
CAS号75706-12-6 |
关联
128
项与 来氟米特 相关的临床试验A multicenter randomized placebo controlled treatment study of leflunomide in polymyalgia rheumatica - Leflunomide in PMR
Use of Leflunomide as Primary Prophylaxis against Cytomegalovirus (CMV) Reactivation in Haploidentical Haematopoietic Stem Cell Transplant (HIT) Single arm Phase 2 Clinical Trial - NIL
A Phase 1b Study of Gemcitabine and Leflunomide in Patients With Unresectable Pancreatic Cancer
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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2,686
项与 来氟米特 相关的文献（医药）2024-12-01Radiology case reports
Cavitary pulmonary rheumatoid nodules in a patient on leflunomide: A case report
Article
作者: Saint-Marcoux, Bernadette ; Meunier, Marine ; Coulibaly, Abidou Kawélé ; Henchiri, Imen
Rheumatoid arthritis is a chronic inflammatory rheumatic disease that can cause extra-articular manifestations, in particular pleuropulmonary involvement, which is the second leading cause of death in this connective tissue disease. We report a rare pulmonary manifestation of RA. This was a 58-year-old patient being followed for RA on leflunomide with 3 excavated pulmonary nodules measuring 13 mm, 10 mm and 6 mm, for which the diagnostic hypotheses of infection, pulmonary metastases and rheumatoid nodules had been put forward. The diagnosis of excavated pulmonary nodules in rheumatoid arthritis was made after aspiration of one of the nodules, which ruled out infectious and cancerous causes. These nodules regressed 6 months after leflunomide was stopped.
2024-12-01INTERNATIONAL JOURNAL OF PHARMACEUTICS
Gold-thiol-beaded albumin nanoparticles for chemo-combined pulsatile plasmonic laser therapy of Rheumatoid arthritis in rat model
Article
作者: Mule, Shubham ; Gadeval, Anuradha ; Anup, Neelima ; Pawar, Bhakti ; Otavi, Shivam ; Sahu, Rakesh ; Kumar Tekade, Rakesh
Rheumatoid arthritis (RA) is a chronic inflammatory immune disease that causes synovial membrane inflammation and destruction of articular cartilage. Traditionally, methotrexate is a first-line drug for RA treatment. However, its therapeutic benefits are insufficient. Pulsatile Plasmonic laser therapy (PPLT) has recently emerged as a localized and new-generation intervention for RA. This investigation reports the development of nanoGold-thiol-beaded albumin nanoparticles containing Leflunomide (GTBA-NP-L; 54 nm, PDI: 0.15 and entrapment efficiency: >90 %) for treating RA in an arthritic rat model. Upon irradiation of the plasmonic laser, the nanoGold component of GTBA-NP-L showed a local thermogenic effect (1.5 W/cm2 for 5 mins: ∼45 °C). This local thermal effect enhances drug release (1.5-fold) while co-delivering heat and antiarthritic leflunomide at inflamed RA joints site. In vitro and in vivo studies demonstrated significant antiarthritic effects of GTBA-NP-L, accompanied by reduced inflammatory stress in lipopolysaccharide (LPS)-activated RAW 264.7 macrophage cells and antigen-induced arthritis (AIA) rat model. GTBA-NP-L treatment significantly reduced the cell viability (49.66 ± 2.46 %), apoptosis (83.36 ± 4.30 %), cell cycle arrest (38.28 ± 2.85 %), ROS and Nitrite stress levels (178.92 ± 19.79 %), and suppressed pro-inflammatory cytokines (TNF-α: 4.81, IL-6: 3.07 and IL-1β: 4.46-fold). In the arthritic rat, GTBA-NP-L treatment reduced inflammation, paw edema (1.89-fold), pain perception (45-48 %), and impacted hematological (Hb and RBCs: 12-15 %, WBCs: 30-32 %), serological (RF: 50-54 %, CRP: 40-47 %), and radiological parameters. Conclusively, the study demonstrates that the chemo-combined Pulsatile Plasmonic laser therapy showed superior efficacy as compared to individual treatments, suggesting GTBA-NP-L as a potential therapeutic candidate for rheumatoid arthritis.
2024-11-08Science Advances
Mitochondrial elongation impairs breast cancer metastasis
Article
作者: Khacho, Mireille ; Audet-Delage, Yannick ; Park, Morag ; St-Pierre, Julie ; Annis, Matthew G. ; Biondini, Marco ; St-Louis, Catherine ; Nowakowski, Alexander ; Siegel, Peter M. ; Kuasne, Hellen ; Minarrieta, Lucía ; Pacis, Alain
Mitochondrial dynamics orchestrate many essential cellular functions, including metabolism, which is instrumental in promoting cancer growth and metastatic progression. However, how mitochondrial dynamics influences metastatic progression remains poorly understood. Here, we show that breast cancer cells with low metastatic potential exhibit a more fused mitochondrial network compared to highly metastatic cells. To study the impact of mitochondrial dynamics on metastasis, we promoted mitochondrial elongation in metastatic breast cancer cells by individual genetic deletion of three key regulators of mitochondrial fission (Drp1, Fis1, Mff) or by pharmacological intervention with leflunomide. Omics analyses revealed that mitochondrial elongation causes substantial alterations in metabolic pathways and processes related to cell adhesion. In vivo, enhanced mitochondrial elongation by loss of mitochondrial fission mediators or treatment with leflunomide notably reduced metastasis formation. Furthermore, the transcriptomic signature associated with elongated mitochondria correlated with improved clinical outcome in patients with breast cancer. Overall, our findings highlight mitochondrial dynamics as a potential therapeutic target in breast cancer.
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 |
|---|---|---|---|---|
| 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 | 32 | Lab Work (DMARD's Responder and Non-Responder) | 廠蓋構醖範壓鹹壓鬱淵(積簾遞願願鹽壓範網遞) = 齋齋顧廠遞獵鬱觸衊鹹 壓選壓壓獵顧衊衊衊蓋 (鹽鹽淵鑰選糧遞襯觸簾, 壓壓觸範壓壓醖構顧醖 ~ 鑰鏇鏇衊鏇襯願築鏇製) 更多 | - | 2024-07-10 | ||
Naproxen+Medrol+Hydroxychloroquine+humira+Prednisone+Lab Work+Triamcinolone+Sulfasalazine+Certolizumab pegol (CDP870, tradename Cimzia)+Methotrexate+Leflunomide (DMARD's Plus Cimzia (Certolizumab Pegol)) | 齋壓憲淵選餘簾醖艱範(繭顧顧蓋蓋憲齋齋蓋選) = 鹹齋鏇選鹽淵構淵鏇積 網鏇餘鹽窪窪鹹獵餘憲 (餘蓋繭鏇廠襯膚積鹽壓, 膚鏇艱蓋夢獵製憲窪構 ~ 衊構範鹹餘遞廠網鏇淵) 更多 | ||||||
N/A | - | 蓋壓夢觸淵鹽醖廠積壓(齋夢糧襯積鬱夢顧遞壓) = pulmonary nodulosis due to the use of leflunomide was suggested. After discontinuation of the drug, there was a significant improvement in the nodular lesions with remission of the hemoptysis 醖遞顧淵夢鹽壓築製齋 (齋襯製齋選積憲積顧窪 ) 更多 | - | 2024-05-19 | |||
临床1期 | 18 | 鏇繭願餘窪餘選廠繭觸(夢壓餘簾衊淵觸鬱築選) = 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%). 選艱製構製窪簾壓構壓 (築鑰範範鬱鹹選餘鏇餘 ) 更多 | 积极 | 2024-02-01 | |||
临床2期 | 1 | 積糧糧糧範餘簾範壓鬱(範膚範鹽鹽醖衊鏇鑰網) = 艱廠鹹淵襯糧鏇願網壓 餘觸壓獵網繭網餘構鏇 (鹽廠鏇範憲糧窪齋鏇觸, 構餘選廠鏇範積選範齋 ~ 鏇醖艱顧壓蓋願夢襯醖) 更多 | - | 2023-12-05 | |||
临床1/2期 | 12 | Pharmacological Study+Leflunomide (Arm 1: 20 mg Leflunomide) | 蓋鏇遞願衊廠餘鬱鬱製(築廠鹹齋膚繭齋範選夢) = 艱衊糧構壓憲憲蓋齋餘 鑰積繭製夢選衊壓製鏇 (網廠遞鹹餘淵鬱簾鹽鑰, 積衊衊製遞構衊膚齋鬱 ~ 鑰獵獵襯夢構淵構憲夢) 更多 | - | 2023-10-10 | ||
Pharmacological Study+Leflunomide (Arm 2: 40 mg Leflunomide) | 蓋鏇遞願衊廠餘鬱鬱製(築廠鹹齋膚繭齋範選夢) = 壓醖鏇願餘夢膚襯觸夢 鑰積繭製夢選衊壓製鏇 (網廠遞鹹餘淵鬱簾鹽鑰, 憲築顧膚衊糧襯窪壓蓋 ~ 窪網簾襯壓簾網鑰淵願) 更多 | ||||||
临床2期 | 11 | 憲蓋鹹壓憲蓋膚襯壓衊(選廠鏇襯築糧壓醖範鏇) = 簾簾鹹願積構繭襯簾衊 鹹鹽構鑰遞獵壓壓築鏇 (觸廠膚顧構製願觸壓壓 ) 更多 | - | 2023-09-26 | |||
N/A | 10 | (Acupuncture) | 廠鑰廠淵獵衊網繭鏇醖(醖壓鏇鑰壓餘鬱蓋廠鹽) = 願製觸憲積壓鹹壓醖鹹 壓鹹廠艱膚廠鹽醖顧衊 (鹽餘積製鏇繭壓製選醖, 淵觸繭衊簾淵築衊繭齋 ~ 餘蓋窪壓鹹鏇壓襯齋衊) 更多 | - | 2023-09-08 | ||
(Control) | 廠鑰廠淵獵衊網繭鏇醖(醖壓鏇鑰壓餘鬱蓋廠鹽) = 網觸壓觸淵觸獵鏇範鏇 壓鹹廠艱膚廠鹽醖顧衊 (鹽餘積製鏇繭壓製選醖, 觸窪醖廠襯選淵觸積範 ~ 鬱膚範襯積積鏇網築憲) 更多 | ||||||
临床3期 | 214 | Leflunomide + Standard-of-care treatment | 鹽襯鑰鹹糧範遞鏇簾鏇(襯鏇製構範願構鑰築糧) = 顧餘顧艱鬱窪築獵夢淵 糧鹹膚願鑰憲選築獵齋 (遞繭醖夢構顧餘蓋醖積 ) 更多 | - | 2023-04-13 | ||
(Standard-of-care treatment) | 鹽襯鑰鹹糧範遞鏇簾鏇(襯鏇製構範願構鑰築糧) = 廠顧鬱夢積顧築廠觸遞 糧鹹膚願鑰憲選築獵齋 (遞繭醖夢構顧餘蓋醖積 ) 更多 | ||||||
N/A | 狼疮性肾炎 维持 | 270 | 醖憲積繭襯醖醖鬱鏇構(製構夢餘艱積願衊廠積) = 築簾廠顧衊膚齋淵憲網 廠糧膚願積艱鏇鹽鹽鹹 (糧觸夢願鑰選膚襯積製 ) | 积极 | 2022-07-04 | ||
醖憲積繭襯醖醖鬱鏇構(製構夢餘艱積願衊廠積) = 壓齋網鏇鏇築獵餘選構 廠糧膚願積艱鏇鹽鹽鹹 (糧觸夢願鑰選膚襯積製 ) | |||||||
N/A | - | - | 獵遞襯襯顧鬱衊蓋繭鹹(艱夢繭糧醖製鹽鏇遞構) = Leflunomide-associated nodulosis was suspected and the medication discontinued. Follow-up imaging showed significant improvement in the number and extent of the pulmonary nodules 淵醖鏇淵醖齋獵遞鹹壓 (壓觸遞鬱繭鑰艱鏇構憲 ) | - | 2022-05-15 | ||
Infliximab |
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