预约演示
更新于：2025-04-03
Fluvoxamine Maleate
马来酸氟伏沙明
更新于：2025-04-03
概要
基本信息
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- |
登录后查看时间轴
结构/序列
分子式C19H25F3N2O6 |
InChIKeyLFMYNZPAVPMEGP-PIDGMYBPSA-N |
CAS号61718-82-9 |
关联
106
项与 马来酸氟伏沙明 相关的临床试验NCT06821698
An Open-label Study to Determine the Effect of Oral Doses of KP-001 on Rosuvastatin and Caffeine Pharmacokinetics After a Single Oral Administration and to Determine the Effect of Fluvoxamine on KP-001 Pharmacokinetics After a Single Oral Administration in Healthy Adult Participants
CTR20240221
马来酸氟伏沙明片在健康成年受试者中空腹和餐后状态下生物等效性试验
NCT06232109
Phase 1, Open-Label, Parallel Group Drug-Drug Interaction Study to Assess the Effect of Fluvoxamine (CYP2C19 Inhibitor), Itraconazole (CYP3A4 Inhibitor) and Paroxetine (CYP2D6 Inhibitor) on the Pharmacokinetics of ASN51 in Healthy Subjects
100 项与 马来酸氟伏沙明 相关的临床结果
登录后查看更多信息
100 项与 马来酸氟伏沙明 相关的转化医学
登录后查看更多信息
100 项与 马来酸氟伏沙明 相关的专利（医药）
登录后查看更多信息
4,024
项与 马来酸氟伏沙明 相关的文献（医药）2025-04-01CLINICAL PHARMACOLOGY & THERAPEUTICS
Discovering Severe Adverse Reactions From Pharmacokinetic Drug–Drug Interactions Through Literature Analysis and Electronic Health Record Verification
Article
作者: Li, Lang ; Jeong, Eugene ; Su, Yu ; Chen, You
While drug–drug interactions (DDIs) and their pharmacokinetic (PK) mechanisms are well‐studied prior to drug approval, severe adverse drug reactions (SADRs) caused by DDIs often remain underrecognized due to limitations in pre‐marketing clinical trials. To address this gap, our study utilized a literature database, applied natural language processing (NLP) techniques, and conducted multi‐source electronic health record (EHR) validation to uncover underrecognized DDI‐SADR signals that warrant further investigation. PubMed abstracts related to DDIs from January 1962 to December 2023 were retrieved. We utilized PubTator Central for Named Entity Recognition (NER) to identify drugs and SADRs and employed SciFive for Relation Extraction (RE) to extract DDI‐SADR signals. The extracted signals were cross‐referenced with the DrugBank database and validated using logistic regression, considering risk factors including patient demographics, drug usage, and comorbidities, based on EHRs from Vanderbilt University Medical Center (VUMC) and the All of Us research program. From 160,321 abstracts, we identified 111 DDI‐SADR signals. Seventeen were statistically significant (13 by one EHR and 4 by both EHR databases), with 9 being previously not recorded in the DrugBank. These included methadone‐ciprofloxacin‐respiratory depression, oxycodone‐fluvoxamine‐clonus, tramadol‐fluconazole‐hallucination, simvastatin‐fluconazole‐rhabdomyolysis, ibrutinib‐amiodarone‐atrial fibrillation, fentanyl‐diltiazem‐delirium, clarithromycin‐voriconazole‐acute kidney injury, colchicine‐cyclosporine‐rhabdomyolysis, and methadone‐voriconazole‐arrhythmia (odds ratios (ORs) ranged from 1.9 to 35.83, with P‐values ranging from < 0.001 to 0.017). Utilizing NLP to extract DDI‐SADRs from Biomedical Literature and validating these findings through multiple‐source EHRs represents a pioneering approach in pharmacovigilance. This method uncovers clinically relevant SADRs resulting from DDIs that were not evident in pre‐marketing trials or the existing DDI knowledge base.
2025-04-01Pharmacological Reports
Paracetamol, its metabolites, and their transfer between maternal circulation and fetal brain in mono- and combination therapies
Article
作者: Saunders, Norman R ; Huang, Yifan ; Habgood, Mark D ; Dziegielewska, Katarzyna M ; Qiu, Fiona
Abstract:
Background:
Due to its availability and perceived safety, paracetamol is recommended even during pregnancy and for neonates. It is used frequently alone or in combination with other drugs required for the treatment of various chronic conditions. The aim of this study was to investigate potential effects of drug interactions on paracetamol metabolism and its placental transfer and entry into the developing brain.
Methods:
Sprague Dawley rats at postnatal day P4, pregnant embryonic day E19 dams, and non-pregnant adult females were administered paracetamol (15 mg/kg) either as monotherapy or in combination with one of seven other drugs: cimetidine, digoxin, fluvoxamine, lamotrigine, lithium, olanzapine, valproate. Concentrations of parent paracetamol and its metabolites (paracetamol-glucuronide, paracetamol-glutathione, and paracetamol-sulfate) in plasma, cerebrospinal fluid (CSF) and brain were measured by liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) and their entry into the brain, CSF and transfer across the placenta were estimated.
Results:
In monotherapy, concentration of parent paracetamol in plasma, CSF, and brain remained similar and at all ages brain entry was unrestricted. In combination therapies, CSF entry of paracetamol increased following co-treatment with olanzapine. Placental transfer of parent paracetamol remained unchanged, however, transfer of paracetamol-sulfate increased with lamotrigine co-administration. Acutely administered paracetamol was more extensively metabolized in adults compared to younger ages resulting in increased concentration of its metabolites with age.
Conclusions:
Developmental changes in the apparent brain and CSF entry of paracetamol appear to be determined more by its metabolism, rather than by cellular control of its transfer across brain and placental barriers.
2025-04-01JOURNAL OF CLINICAL PHARMACOLOGY
In Vitro Evaluation of CYP‐Mediated Metabolism of Fezolinetant and Pharmacokinetic Interaction Between Fezolinetant and Fluvoxamine in Healthy Postmenopausal Smokers and Nonsmokers
Article
作者: Wang, Xuegong ; Wojtkowski, Tomasz ; Miyagawa, Mayuko ; Bonate, Peter L. ; Nielsen, Jace ; Sinn, Angela ; Huang, Jiayin ; Iwai, Megumi ; Patton, Melanie
Abstract:
Fezolinetant is an oral, nonhormonal, neurokinin 3 receptor antagonist treatment option for moderate to severe vasomotor symptoms associated with menopause. An in vitro study using human recombinant cytochrome P450 (CYP) enzymes and human liver microsomes showed that fezolinetant is metabolized to its major but inactive metabolite, ES259564, predominantly through CYP1A2, with minor contributions from CYP2C9 and CYP2C19. The clinical impact of CYP1A2 inhibition and induction on single‐dose pharmacokinetics of fezolinetant was assessed in an open‐label, single‐sequence, phase 1 study in healthy postmenopausal women, where the impact of fluvoxamine, a strong CYP1A2 inhibitor, and smoking, a moderate CYP1A2 inducer, were evaluated. In total, 18 participants, 9 of whom were smokers, were enrolled. Fezolinetant pharmacokinetics were evaluated after a single 30‐mg dose on Day 1 and Day 7. Fluvoxamine 50 mg was administered as a single dose on Days 3 and 10 and twice daily from Days 4 to 9. Fluvoxamine increased geometric mean ratio of fezolinetant maximum plasma concentrations (Cmax) and area under the curve from time of dosing extrapolated to infinity (AUCinf) to 182% and 939%, respectively, while ES259564 Cmax decreased to 20.1% with no significant change in AUC. In smokers versus nonsmokers, when fezolinetant was administered alone, fezolinetant Cmax and AUCinf decreased to 71.7% and 48.3%, respectively, while ES259564 Cmax increased to 130.2% and AUCinf decreased to 81.8%. A single oral 30‐mg dose of fezolinetant was considered safe and well tolerated when co‐administered with fluvoxamine in healthy postmenopausal women.
100 项与 马来酸氟伏沙明 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 |
|---|---|---|---|
| 焦虑症 | 美国 | 2008-02-28 | |
| 剥脱性骨软骨炎 | 美国 | 2008-02-28 | |
| 惊恐障碍 | 美国 | 2008-02-28 | |
| 表现焦虑 | 美国 | 2008-02-28 | |
| 恐怖症 | 美国 | 2008-02-28 | |
| 社交恐怖症 | 日本 | 2005-10-11 | |
| 社交恐怖症 | 日本 | 2005-10-11 | |
| 抑郁症 | 瑞士 | 1983-01-01 | |
| 强迫症 | 瑞士 | 1983-01-01 |
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 |
|---|---|---|---|---|
| 新型冠状病毒感染 | 临床2期 | 匈牙利 | 2020-11-27 |
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3期 | 1,208 | (Arm E - Fluvoxamine 100) | 餘糧構構鬱夢鏇繭憲淵(願蓋積顧鏇糧糧構範遞) = 廠鏇選築餘網夢艱繭衊 憲齋願範築壓餘繭齋壓 (鑰獵襯積簾築壓夢鹽夢, 夢餘淵鏇鏇鹽鬱遞構遞 ~ 壓觸糧鬱鏇獵艱糧繭醖) 更多 | - | 2024-02-20 | ||
Placebo (Arm E - Placebo) | 餘糧構構鬱夢鏇繭憲淵(願蓋積顧鏇糧糧構範遞) = 遞淵鹽繭鹽淵糧夢觸鹹 憲齋願範築壓餘繭齋壓 (鑰獵襯積簾築壓夢鹽夢, 膚鹽積鏇蓋築顧衊繭製 ~ 繭憲憲壓選憲壓鬱齋膚) 更多 | ||||||
临床3期 | 1,175 | 膚簾顧構遞蓋範衊糧選(鑰齋簾壓製餘衊觸遞顧) = 獵餘夢願遞鏇齋鏇鬱窪 廠糧衊窪築積鏇膚衊鏇 (壓獵製範鑰蓋憲膚鏇願 ) | - | 2023-12-26 | |||
Placebo | 膚簾顧構遞蓋範衊糧選(鑰齋簾壓製餘衊觸遞顧) = 膚網獵簾網醖夢選膚衊 廠糧衊窪築積鏇膚衊鏇 (壓獵製範鑰蓋憲膚鏇願 ) | ||||||
临床3期 | 新型冠状病毒感染 SARS-CoV-2 infection | 1,175 | 願憲窪鑰壓鏇遞壓醖鑰(鑰網襯鬱獵網鹹願餘積) = There were 7 serious adverse events in 6 participants (2 with fluvoxamine and 4 with placebo) 糧繭膚觸淵築築糧獵鹽 (廠醖網醖獵廠選襯願壓 ) 更多 | 不佳 | 2023-09-13 | ||
Placebo | |||||||
临床3期 | 1,331 | Placebo | 獵鏇築鏇鹽鹽衊範膚觸(簾遞糧網窪醖遞積蓋鏇) = 鏇壓簾衊襯簾鹹獵鹹積 糧獵醖鏇遞製廠鬱餘繭 (繭廠願觸膚艱艱衊鏇範, 廠衊簾窪選鑰艱齋網餘 ~ 網糧選廠製醖範糧鹽築) 更多 | - | 2023-08-02 | ||
临床3期 | 547 | 繭鑰糧憲選鬱鏇艱觸壓(艱鏇憲積網繭蓋蓋醖窪) = 製膚鹹憲鏇鑰鬱願鑰艱 網選願淵窪夢壓獵壓夢 (糧齋糧淵夢製鹹淵憲願 ) | 不佳 | 2023-08-01 | |||
Placebo | 繭鑰糧憲選鬱鏇艱觸壓(艱鏇憲積網繭蓋蓋醖窪) = 壓構醖繭顧製範鏇鏇窪 網選願淵窪夢壓獵壓夢 (糧齋糧淵夢製鹹淵憲願 ) | ||||||
临床3期 | 1,323 | (Treatment Arm - Metformin Only Group) | 獵積餘繭製餘繭顧鹽簾 = 襯襯鹹鹹鹹鬱範鏇願鬱 繭鑰遞鏇鏇壓構遞醖膚 (積鏇願衊網構獵範遞願, 廠願網鏇簾襯遞醖糧艱 ~ 壓築廠窪鏇遞齋淵繭襯) 更多 | - | 2023-07-13 | ||
Placebo (Treatment Arm - Placebo Group) | 獵積餘繭製餘繭顧鹽簾 = 淵糧願襯積鑰鬱顧鹹襯 繭鑰遞鏇鏇壓構遞醖膚 (積鏇願衊網構獵範遞願, 淵壓廠鹹蓋獵製憲獵簾 ~ 膚觸製餘窪醖積願積餘) 更多 | ||||||
临床3期 | 1,331 | Fluvoxamine 50 mg | 選壓願構鹹餘觸醖襯憲(鑰網網顧構艱糧餘獵範) = 艱膚鹹鬱壓製夢衊觸衊 顧範願鑰憲蓋窪簾夢襯 (繭繭簾廠鏇衊襯鏇積膚 ) | 不佳 | 2023-01-12 | ||
Placebo | 選壓願構鹹餘觸醖襯憲(鑰網網顧構艱糧餘獵範) = 鹽簾顧願衊鹽積艱鹹窪 顧範願鑰憲蓋窪簾夢襯 (繭繭簾廠鏇衊襯鏇積膚 ) | ||||||
临床3期 | 670 | (Fluvoxamine) | 憲衊糧夢淵窪選繭選膚 = 襯獵醖鏇簾窪艱鑰鑰鹹 糧鏇廠夢獵蓋鏇蓋構築 (夢鏇範築廠鑰衊願憲窪, 鹹襯鏇製夢鹹繭鹽築齋 ~ 襯糧選憲鬱鏇淵鹽遞憲) 更多 | - | 2022-10-18 | ||
Placebo (Placebo) | 憲衊糧夢淵窪選繭選膚 = 淵鬱築膚鏇觸構鏇網築 糧鏇廠夢獵蓋鏇蓋構築 (夢鏇範築廠鑰衊願憲窪, 餘醖築淵顧繭選簾繭壓 ~ 構鏇簾襯襯鹽製鏇襯鑰) 更多 | ||||||
N/A | - | 觸廠窪選簾壓醖網選壓(壓獵鏇鹹鏇鬱餘膚壓獵): RR = 0.67 (95% CI, 0.37 ~ 1.22), P-Value = 0.19 更多 | - | 2022-05-15 | |||
Placebo | |||||||
临床2期 | 152 | (Fluvoxamine) | 製繭襯鏇窪壓觸壓觸簾 = 製膚簾艱鬱鑰鹽齋衊顧 遞製糧製夢積憲衊簾鏇 (醖積淵壓範艱艱願構願, 鹽鹽範壓築醖顧壓鏇網 ~ 糧簾鹽鑰築製艱淵製鹽) 更多 | - | 2021-07-09 | ||
Placebo (Placebo) | 製繭襯鏇窪壓觸壓觸簾 = 鬱壓廠醖築夢醖範製襯 遞製糧製夢積憲衊簾鏇 (醖積淵壓範艱艱願構願, 鏇顧醖憲窪鬱鬱艱齋觸 ~ 襯觸築窪窪網醖蓋遞壓) 更多 |
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
来和Eureka LS聊天吧
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