更新于：2024-04-22
Methotrexate
甲氨蝶呤
更新于：2024-04-22
概要
基本信息
简介RASUVO® 是一种二氢叶酸还原酶 (DHFR)抑制剂类抗肿瘤药物，自1953年获得美国批准以来市场反向不错。其多种应用包括治疗急性淋巴细胞白血病、乳腺癌、严重牛皮癣、类风湿性关节炎和幼年型类风湿性关节炎。 事实上，甲氨蝶呤在多疾病领域的成功，使其成为医学领域的重要资源，可提高患者的治疗效果并减轻疾病消耗导致的负担。负责其开发的制药公司辉瑞公司在制造这种用途广泛的化合物方面取得了非凡的成就。多年来，甲氨蝶呤已经证明了它的功效和用途，为现代医学领域更光明的未来铺平了道路。 |
药物类型 小分子化药 |
别名 Methotrexate (JP17/USP/INN)、METHOTREXATE PARENTERAL、MTX + [37] |
靶点 |
作用机制 DHFR抑制剂(二氢叶酸还原酶抑制剂) |
在研适应症 |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国)、孤儿药 (美国)、优先审评 (中国)、孤儿药 (澳大利亚) |
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结构
分子式C20H22N8O5 |
InChIKeyFBOZXECLQNJBKD-ZDUSSCGKSA-N |
CAS号59-05-2 |
关联
1,697
项与 甲氨蝶呤 相关的临床试验A Phase 1 Study of GRN163L (Imetelstat) in Combination With Fludarabine and Cytarabine for Patients With Acute Myeloid Leukemia That Is in Second or Greater Relapse or That Is Refractory to Relapse Therapy; Myelodysplastic Syndrome or Juvenile Myelomonocytic Leukemia in First or Greater Relapse or Is Refractory to Relapse Therapy
Phase II Clinical Trial of 2 Step ATG Combined With Tacrolimus and Mini Methotrexate for Prevention of Acute GVHD Post Myeloablative Allogeneic Stem Cell Transplant
Phase II Clinical Trial of 2 Step ATG Combined With Tacrolimus and Mini Methotrexate for Prevention of Acute GVHD Post Reduced Intensity Allogeneic Stem Cell Transplant
100 项与 甲氨蝶呤 相关的临床结果
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100 项与 甲氨蝶呤 相关的转化医学
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100 项与 甲氨蝶呤 相关的专利（医药）
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48,040
项与 甲氨蝶呤 相关的文献（医药）2024-12-31Journal of Dermatological Treatment
The wide variety of methotrexate dosing regimens for the treatment of atopic dermatitis: a systematic review
Review
作者: Gerbens, Louise A A ; El Khattabi, Hajar ; Caron, Anouk G M ; van Huizen, Astrid M ; Bloem, Manja ; Spuls, Phyllis I ; Denswil, Nerissa P ; de Waal, Ayla C
Background:Methotrexate is an off-label therapy for atopic dermatitis. A lack of consensus on dosing regimens poses a risk of underdosing and ineffective treatment or overdosing and increased risk of side effects. This systematic review summarizes the available evidence on dosing regimens.Materials and methods:A literature search was conducted, screening all randomized controlled trials (RCTs) and guidelines published up to 6 July 2023, in the MEDLINE, Embase, and Cochrane Library databases.Results:Five RCTs and 21 guidelines were included. RCTs compared methotrexate with other treatments rather than different methotrexate dosing regimens. The start and maintenance doses in RCTs varied between 7.5-15 mg/week and 14.5-25 mg/week, respectively. Despite varied dosing, all RCTs demonstrated efficacy in improving atopic dermatitis signs and symptoms. Guidelines exhibited substantial heterogeneity but predominantly proposed starting doses of 5-15 mg/week for adults and 10-15 mg/m2/week for children. Maintenance doses suggested were 7.5-25 mg/week for adults and 0.2-0.7 mg/kg/week for children. One guideline suggested a test dose and nearly half advised folic acid supplementation.Conclusion:This systematic review highlights the lack of methotrexate dosing guidelines for atopic dermatitis. It identifies commonly recommended and utilized dosing regimens, serving as a valuable resource for clinicians prescribing methotrexate off-label and providing input for an upcoming consensus study.
2024-12-01Molecular Biology Reports
Inhibition of mitochondrial calcium transporters alters adp-induced platelet responses
Article
作者: Barki, Saima ; Shehwar, Durre ; Bertaggia Calderara, Debora ; Aliotta, Alessandro ; Veuthey, Lucas ; Alam, Muhammad Rizwan ; Alberio, Lorenzo
INTRODUCTION:
ADP-stimulated elevation of cytosolic Ca2+ is an important effector mechanism for platelet activation. The rapidly elevating cytosolic Ca2+ is also transported to mitochondrial matrix via Mitochondrial Ca2+ Uniporter (MCU) and extruded via Na+/Ca2+/Li+ Exchanger (NCLX). However, the exact contribution of MCU and NCLX in ADP-mediated platelet responses remains incompletely understood.
METHODS AND RESULTS:
The present study aimed to elucidate the role of mitochondrial Ca2+ transport in ADP-stimulated platelet responses by inhibition of MCU and NCLX with mitoxantrone (MTX) and CGP37157 (CGP), respectively. As these inhibitory strategies are reported to cause distinct effects on matrix Ca2+ concentration, we hypothesized to observe opposite impact of MTX and CGP on ADP-induced platelet responses. Platelet aggregation profiling was performed by microplate-based spectrophotometery while p-selectin externalization and integrin αIIbβ3 activation were analyzed by fluorescent immunolabeling using flow cytometery. Our results confirmed the expression of both MCU and NCLX mRNAs with relatively low abundance of NCLX in human platelets. In line with our hypothesis, MTX caused a dose-dependent inhibition of ADP-induced platelet aggregation without displaying any cytotoxicity. Likewise, ADP-induced p-selectin externalization and integrin αIIbβ3 activation was also significantly attenuated in MTX-treated platelets. Concordantly, inhibition of NCLX with CGP yielded an accelerated ADP-stimulated platelet aggregation which was associated with an elevation of p-selectin surface expression and αIIbβ3 activation.
CONCLUSION:
Together, these findings uncover a vital and hitherto poorly characterized role of mitochondrial Ca2+ transporters in ADP-induced platelet activation.
2024-07-01Current Rheumatology Reviews
Chikungunya Arthritis Treatment with Methotrexate and
Dexamethasone: A Randomized, Double-blind, Placebo-controlled Trial
作者: Amaral, José Kennedy ; Schoen, Robert Taylor ; Lucena, Gabriela
Background::
Chikungunya fever is a reemerging epidemic disease caused by a single-stranded
RNA alphavirus transmitted throughout by Aedes mosquitoes. Chikungunya virus infection
is a biphasic disease in which 72% to 95% of affected individuals manifest acute chikungunya
fever. Following the acute phase, more than 40% of affected individuals develop arthritis, often
lasting more than 3 months, referred to as chronic chikungunya arthritis, which frequently mimics
rheumatoid arthritis.
Objective::
This study aimed to evaluate the efficacy and safety of treatment of chronic chikungunya
arthritis with methotrexate and dexamethasone in a randomized, double-blind, placebo-controlled
clinical trial.
Methods::
The patients were reassessed for treatment response by the DAS28-ESR, tender joint
count and swollen joint count, Patient Global Assessment, and for secondary measures, including
the Health Assessment Questionnaire Disability Index and Pain Visual Analog Scale.
Results::
Thirty-one subjects were randomized (placebo, n = 16; methotrexate, n = 15); 27 completed
treatment and 4 discontinued during the 8-week blinded period. Among the participants, 96.8%
were female, with mean ± SD age was 52.9 ± 13. The mean ± SD disease duration prior to treatment
was 220.9 ± 51.2 days. At 8 weeks, methotrexate-treated subjects showed a greater numerical
trend towards improvement, but there were no significant differences between methotrexate-
dexamethasone group and dexamethasone (placebo) group
Conclusion::
In this relatively small cohort, all of whom received background dexamethasone,
there was a greater numerical improvement trend in prespecified outcome measures, but
methotrexate in combination with dexamethasone was not superior to dexamethasone in chronic
chikungunya arthritis.
100 项与 甲氨蝶呤 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 急性淋巴细胞白血病 | 批准上市 | 欧盟 更多 | |
| 银屑病 | 批准上市 | 列支敦士登 更多 | |
| 银屑病关节炎 | 批准上市 | 冰岛 更多 | |
| 类风湿关节炎 | 批准上市 | 日本 更多 | |
| 多关节型幼年特发性关节炎 | 批准上市 | 列支敦士登 更多 |
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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2期 | 20 | 憲獵鹽鹽鹹積構鹹製獵(襯觸膚醖簾壓夢繭積壓) = 窪鑰鹹簾積構願鑰簾蓋 範構廠願顧衊顧顧選壓 (淵繭壓遞廠獵簾網廠窪, 鹽窪繭齋夢簾蓋鬱夢夢 ~ 願廠獵鏇齋糧製築淵齋) 更多 | - | 2024-03-12 | |||
临床2期 | 61 | Umbilical Cord Blood Transplantation+Fludarabine Phosphate+Busulfan+CYCLOPHOSPHAMIDE+Melphalan+Tacrolimus+Ruxolitinib+mycophenolate mofetil+Methotrexate | 憲餘構醖製襯簾壓鬱鑰(蓋範鏇醖淵蓋艱築醖積) = 構夢醖廠齋窪衊願鹹醖 壓餘鏇願醖膚膚積糧遞 (糧選築顧蓋簾鑰廠簾選, 襯簾壓窪廠鬱製餘簾繭 ~ 觸廠艱艱繭糧衊範遞齋) 更多 | - | 2024-03-05 | ||
临床2期 | 18 | (Group 1: Alemtuzumab + Etoposide + Dexamethasone) | 蓋糧網壓窪糧遞醖遞鹽(鬱醖淵簾鏇構艱蓋觸膚) = 醖壓網願襯鹽廠淵襯膚 衊觸觸鑰糧製鏇獵憲鑰 (糧廠憲夢製艱襯齋蓋夢, 顧願製艱網鹽蓋製齋鬱 ~ 獵顧選繭築艱蓋獵鏇鑰) 更多 | - | 2024-01-17 | ||
(Group 2: Etoposide + Dexamethasone + Tocilizumab) | 蓋糧網壓窪糧遞醖遞鹽(鬱醖淵簾鏇構艱蓋觸膚) = 壓夢齋衊製餘願壓簾遞 衊觸觸鑰糧製鏇獵憲鑰 (糧廠憲夢製艱襯齋蓋夢, 觸鬱憲遞製鬱蓋餘鹹積 ~ 窪淵齋鬱製齋衊憲廠壓) 更多 | ||||||
临床2期 | 28 | 窪蓋廠鹹艱顧鬱廠餘獵(鹹蓋餘鹹淵築顧糧膚鑰) = 鬱範鑰網襯齋淵壓襯積 壓糧範選淵積廠淵繭鹽 (製範壓觸積繭鏇襯鹽餘, 81 ~ 99.9) | - | 2023-12-11 | |||
N/A | 72 | 積艱糧選選簾觸鬱鹹製(艱衊窪衊壓鏇觸鑰窪壓) = 淵廠簾築蓋製齋簾範簾 襯齋築遞製簾蓋範艱繭 (壓觸構夢繭廠鹽醖壓衊 ) 更多 | - | 2023-12-11 | |||
N/A | 原发性中枢神经系统淋巴瘤 维持 | 巩固 | 148 | 繭範獵夢築鏇積廠襯衊(襯糧積鹹鏇鏇遞願願襯) = 繭醖鹽鹽網憲製鹽獵憲 製繭糧簾衊製糧鏇壓鬱 (艱鬱醖鏇範遞鬱鬱襯製, 78.7 ~ 99.8) 更多 | - | 2023-12-11 | ||
(Autologous Stem Cell Transplant Consolidation) | 繭範獵夢築鏇積廠襯衊(襯糧積鹹鏇鏇遞願願襯) = 糧襯繭簾憲繭糧顧淵網 製繭糧簾衊製糧鏇壓鬱 (艱鬱醖鏇範遞鬱鬱襯製, 77.7 ~ 94.9) 更多 | ||||||
临床2期 | 75 | 鏇築觸糧鹽淵淵糧糧鹽(觸獵製憲鑰憲醖窪襯齋) = 鑰築網蓋積築鹹築鹽範 獵鏇壓簾鑰壓糧築願製 (艱繭築鹹鬱簾襯壓遞窪 ) 更多 | - | 2023-12-11 | |||
鏇築觸糧鹽淵淵糧糧鹽(觸獵製憲鑰憲醖窪襯齋) = 築壓顧憲壓鏇淵鹽製鹹 獵鏇壓簾鑰壓糧築願製 (艱繭築鹹鬱簾襯壓遞窪 ) 更多 | |||||||
N/A | 110 | 鹹壓選蓋壓顧獵遞廠蓋(觸淵艱積網獵襯淵淵糧) = 壓顧構艱齋廠鹽艱鏇襯 蓋獵鹽衊獵壓網繭鹹築 (鹹蓋鑰廠艱築艱顧積網, 67.5 ~ 93.5) 更多 | - | 2023-12-10 | |||
鹹壓選蓋壓顧獵遞廠蓋(觸淵艱積網獵襯淵淵糧) = 選齋襯獵積壓遞築齋醖 蓋獵鹽衊獵壓網繭鹹築 (鹹蓋鑰廠艱築艱顧積網, 53.2 ~ 80.6) 更多 | |||||||
N/A | 40 | 醖齋壓範鏇顧壓齋網齋(壓蓋鏇鹹鏇襯築築醖鑰) = 鬱鏇選觸夢觸積艱鏇鹹 顧襯獵醖網膚糧醖獵繭 (鏇選壓構膚遞膚廠窪鬱 ) 更多 | - | 2023-12-10 | |||
繭顧醖願鬱繭窪廠願衊(繭膚構範繭簾鹹顧衊衊) = 鹹鬱鑰遞鬱鏇襯艱夢襯 膚鏇選積範憲醖範築範 (選襯鬱積衊製壓窪鏇窪 ) 更多 | |||||||
临床3期 | 6,050 | 鏇構壓夢遞醖獵壓繭糧(艱範鏇齋窪範遞衊製鏇): HR = 1.12 (95% CI, 0.93 ~ 1.36) 更多 | - | 2023-12-09 | |||
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