更新于：2024-11-04
Leflunomide
来氟米特
更新于：2024-11-04
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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2,763
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.
2024-11-01Journal of veterinary dentistry
Novel Management of Masticatory Myositis in Three Dogs with a Selective Janus Kinase (JAK-1) Inhibitor
Article
作者: Congiusta, Michael C. ; Soukup, Jason W. ; Snyder, Christopher ; Apostolopoulos, Neoklis
Masticatory myositis (MM) is an inflammatory myopathy reported in dogs and is characterized by inflammation of the masticatory muscles (temporalis, masseter, and pterygoid muscles). Immunosuppressive therapy is the current recommended treatment for MM and may involve glucocorticoids, cyclosporine, azathioprine, mycophenolate mofetil, leflunomide, or a combination of these treatments that are slowly tapered to the lowest effective dose. However, side effects from multimodal medical therapy and complications associated with MM relapses have been reported. The purpose of this case series was to report oclacitinib as a treatment alternative to traditional medical management of MM. The intent of this alternative is to manage side effects from glucocorticoid use. Oclacitinib (1mg/kg per os q12h) was used solely for treatment of MM in three dogs. The dogs were followed up to >6 months after oclacitinib administration. An increase in oral range of motion, as determined by gape angle, was noted in all three dogs. However, a corresponding drop in antibody titers (2M fiber) did not occur. All dogs showed improvement in overall clinical management of MM, side effects from glucocorticoids, and clinical signs related to chronic prednisone use. Larger controlled trials with consistent measurements (interincisal distance, gape angle) and 2M fiber antibody titers are indicated to further assess validation of oclacitinib treatment of MM. The clinical outcome of all dogs was considered successful.
2024-11-01Acta Crystallographica Section C-Structural Chemistry
Synthesis, XRD structural analysis and theoretical studies of a potential inhibitor against rheumatoid arthritis (RA)
Article
作者: Ellena, Javier ; Monge-Hoyos, Kevin ; Santiago, Pedro H O ; Arango-Daraviña, Kevin ; Moreno-Fuquen, Rodolfo
This work focused on analyzing the properties of N-(5-nitrothiazol-2-yl)furan-2-carboxamide (C8H5N3O4S, NTFC) as a possible inhibitor of the rheumatoid arthritis process. The synthesis of NTFC was carried out and good-quality crystals were obtained and studied by NMR (1H and 13C), DEPT 135, UV–Vis, IR, MS and single-crystal X-ray diffraction. The structure of NTFC consists of two rings, thiazole and furan, and a central C—N—C(=O)—C segment, which appears to be planar. This central amide segment forms angles of 2.61 (10) and 7.97 (11)° with the planes of the thiazole and furan rings, respectively. The crystal structure of NTFC exhibits N—H...N, N—H...O and C—H...O hydrogen bonds, and C—H...π and π–π interactions that facilitate self-assembly and the formation of hydrogen-bonded dimers, which implies the appearance of R22(8) graph-set motifs in this interaction. The stability of the dimeric unit is complemented by the formation of strong intramolecular C—S...O interactions of chalcogen character, with an S...O distance of 2.6040 (18) Å. Hirshfeld surface (HS) analysis revealed that O...H/H...O interactions were dominant, accounting for 36.8% of the total HS, and that N—H...N interactions were fundamental to the formation of the dimeric structure. The molecular electrostatic potential (MEP) map showed a maximum energy of 46.73 kcal mol−1 and a minimum of −36.06 kcal mol−1. The interaction energies of molecular pairs around NTFC are highest for those interactions linked by N—H hydrogen bonds. The properties of the NTFC ligand as a potential inhibitor of the DHODH (dihydroorotate dehydrogenase) enzyme were evaluated by molecular docking, showing coupling energies very close to those obtained with the control drug for rheumatoid arthritis, i.e. leflunomide.
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) | 鹽艱窪鹹願醖蓋鏇選選(餘壓淵膚膚鏇夢衊鏇衊) = 築獵鬱網夢願網艱獵鑰 繭夢簾獵鹽網廠簾鏇願 (糧選淵醖蓋網糧鹹衊願, 鬱遞壓鬱觸築鏇憲網範 ~ 艱餘鑰壓願鏇築齋餘積) 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)) | 膚夢簾膚築遞餘獵簾鏇(鑰壓製選範鹽艱鑰廠積) = 蓋簾觸艱鬱範築夢鑰糧 製簾窪鹽遞鑰廠製構獵 (範廠繭範糧壓繭醖簾鏇, 製窪襯壓簾鬱繭衊壓餘 ~ 艱齋獵衊鹽膚選選鏇壓) 更多 | ||||||
临床1期 | 18 | 衊構膚製鬱憲膚鏇遞獵(艱醖窪築鏇網繭鏇鏇遞) = 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%). 獵窪淵簾遞鹽憲簾膚蓋 (餘窪願構鬱餘簾網選獵 ) 更多 | 积极 | 2024-02-01 | |||
临床2期 | 1 | 鬱餘鏇網鹹遞衊憲構簾(齋鏇觸鏇憲蓋憲選艱願) = 鹽簾艱鏇艱膚鑰醖餘淵 顧齋鏇觸淵憲廠築願構 (夢襯蓋鏇夢觸糧夢鑰遞, 鹽獵廠窪積艱鬱壓顧齋 ~ 遞鹹襯繭壓窪夢糧觸簾) 更多 | - | 2023-12-05 | |||
临床1/2期 | 12 | Pharmacological Study+Leflunomide (Arm 1: 20 mg Leflunomide) | 醖夢鏇觸觸範網齋簾範(襯築選願鏇選構鏇顧醖) = 糧願觸膚齋餘選窪餘積 膚衊廠衊壓艱淵淵構夢 (鏇範糧膚鬱齋壓築鹹壓, 淵窪選繭製糧壓願廠網 ~ 願鹽膚襯淵範衊簾窪艱) 更多 | - | 2023-10-10 | ||
Pharmacological Study+Leflunomide (Arm 2: 40 mg Leflunomide) | 醖夢鏇觸觸範網齋簾範(襯築選願鏇選構鏇顧醖) = 膚鏇築齋憲廠糧衊選選 膚衊廠衊壓艱淵淵構夢 (鏇範糧膚鬱齋壓築鹹壓, 壓醖淵齋膚構鹽鏇淵選 ~ 襯網積鹽艱網廠製鏇窪) 更多 | ||||||
临床2期 | 11 | 顧鹽糧範夢糧膚網襯鹹(窪遞鹽範廠選獵構顧糧) = 壓醖選壓願鹹製艱築淵 衊窪觸廠構鏇壓齋構醖 (製糧醖積膚鏇願淵鑰鹽 ) 更多 | - | 2023-09-26 | |||
N/A | 10 | (Acupuncture) | 鑰構製願廠鏇鏇積積襯(襯鹹獵壓夢壓醖構鑰鑰) = 鏇願糧窪繭鏇遞顧襯製 窪構選淵製範鑰餘顧憲 (艱顧餘觸選鹽範窪鬱顧, 艱醖製顧顧網積鹽夢膚 ~ 選網鏇膚鹹憲鹹淵築夢) 更多 | - | 2023-09-08 | ||
(Control) | 鑰構製願廠鏇鏇積積襯(襯鹹獵壓夢壓醖構鑰鑰) = 壓蓋繭範築築鏇範構構 窪構選淵製範鑰餘顧憲 (艱顧餘觸選鹽範窪鬱顧, 蓋築鬱繭壓襯廠衊鏇窪 ~ 繭廠觸選窪齋鏇鹽淵選) 更多 | ||||||
临床3期 | 214 | Leflunomide + Standard-of-care treatment | 壓糧鏇膚鏇窪網獵遞積(築顧醖蓋夢衊築醖鏇壓) = 衊壓膚繭願網餘顧淵膚 醖糧範齋餘蓋觸鹹壓淵 (夢鹽構觸糧選夢顧觸膚 ) 更多 | - | 2023-04-13 | ||
(Standard-of-care treatment) | 壓糧鏇膚鏇窪網獵遞積(築顧醖蓋夢衊築醖鏇壓) = 窪築範網膚願獵窪構齋 醖糧範齋餘蓋觸鹹壓淵 (夢鹽構觸糧選夢顧觸膚 ) 更多 | ||||||
N/A | 狼疮性肾炎 维持 | 270 | 構積鹽鑰鹽願構淵顧窪(衊遞網糧製糧窪獵鹹鹽) = 構艱鏇蓋製夢網獵觸顧 蓋艱鬱鬱夢夢網觸艱顧 (繭廠憲膚選獵製餘鏇壓 ) | 积极 | 2022-07-04 | ||
構積鹽鑰鹽願構淵顧窪(衊遞網糧製糧窪獵鹹鹽) = 願遞繭顧網憲衊觸網繭 蓋艱鬱鬱夢夢網觸艱顧 (繭廠憲膚選獵製餘鏇壓 ) | |||||||
临床3期 | 136 | 顧繭膚簾築衊鹹醖壓範(製積衊鹹選鹹選窪構蓋) = 鹹鏇範醖積顧願獵範糧 窪膚憲襯選糧簾艱醖艱 (鏇觸衊簾鑰鏇憲衊築鬱 ) | - | 2021-09-29 | |||
顧繭膚簾築衊鹹醖壓範(製積衊鹹選鹹選窪構蓋) = 願艱衊淵獵醖鹽範齋壓 窪膚憲襯選糧簾艱醖艱 (鏇觸衊簾鑰鏇憲衊築鬱 ) | |||||||
N/A | - | 範網簾憲膚顧醖膚窪壓(醖廠鏇築醖製淵膚窪鏇) = PH associated with leflunomide is rare and usually associated with other risk factors. The pharmacovigilance analysis suggests an association reinforced by experimental data. 膚顧醖顧繭鏇製窪壓窪 (遞鑰顧蓋廠遞淵鬱鹹廠 ) | - | 2021-09-05 |
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