更新于：2024-07-01
Topiramate
托吡酯
更新于：2024-07-01
概要
基本信息
简介托吡酯以商品名Topamax ® 销售，是一种抗惊厥药物，于1995年在英国由Janssen Services 首次推上市场。 其作用机制为 GABAAR 激动剂。 主要用于治疗癫痫，也被批准用于预防和治疗偏头痛。托吡酯通过稳定大脑中的电活动起作用，从而降低癫痫发作的可能性。已发现它可有效降低癫痫患者癫痫发作的频率和严重程度，以及减少偏头痛的频率。 托吡酯有片剂形式，通常按照医疗保健提供者的指示每天口服一次或两次。 |
药物类型 小分子化药 |
别名 2,3:4,5-bis-O-(1-methylethylidene)-β-D-fructopyranose sulfamate、2,3:4,5-di-O-isopropylidene-β-D-fructopyranose sulfamate、Topiramate (JAN/USP/INN) + [18] |
作用机制 AMPA receptor拮抗剂(离子型谷氨酸受体AMPA拮抗剂)、CAs抑制剂(碳酸酐酶家族抑制剂)、GABAA receptor激动剂(γ-氨基丁酸 A 受体激动剂) |
在研适应症 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构
分子式C12H21NO8S |
InChIKeyKJADKKWYZYXHBB-XBWDGYHZSA-N |
CAS号97240-79-4 |
关联
323
项与 托吡酯 相关的临床试验A Phase 3, Randomized, Double-blind, Double-dummy, Parallel-group, Active Drug and Placebo-controlled, Safety, Efficacy and Superiority of Sibutramine IR/Topiramate XR in Overweight Adults With Comorbidities/Obesity
A Phase I/II Clinical Trial Investigating the Effect of Topiramate on the Reactivation of the HIV-1 Reservoir in People Living With HIV on Antiretroviral Therapy
Safety and Efficacy of Zonisamide Versus Topiramate in Migraine
100 项与 托吡酯 相关的临床结果
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100 项与 托吡酯 相关的转化医学
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100 项与 托吡酯 相关的专利（医药）
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5,713
项与 托吡酯 相关的文献（医药）2024-12-01Molecular biology reports
Comparison of neuroprotective effects of a topiramate-loaded biocomposite based on mesoporous silica nanoparticles with pure topiramate against methylphenidate-induced neurodegeneration
Article
作者: Khalilzadeh, Mina ; Mir, Saeedeh ; Pari, Erfan ; Motevalian, Manijeh ; Moazam, Ashrafsadat ; Sheibani, Mohammad ; Sazegar, Mohammad Reza
BACKGROUND:
Methylphenidate (MPH) abuse has been criticized for its role in neurodegeneration. Also, a high risk of seizure was reported in the first month of MPH treatment. Topiramate, a broad-spectrum Antiepileptic Drug (AED), has been used as a neuroprotective agent in both aforementioned complications. Nanotechnology is introduced to increase desirable neurological treatment with minimum side effects. We aimed to investigate the potential neuroprotective activity of topiramate loaded on nanoparticles.
METHODS AND RESULTS:
MTT assay was performed to evaluate the cellular cytotoxicity of Mesoporous Silica Nanoparticles (MSN). Male rats were randomly divided into eight groups. Rats received an intraperitoneal (i.p) MPH (10 mg/kg) injection and a daily oral dose of topiramate (TPM, 30 mg/kg), MSN with Zn core (10 and 30 mg/kg), and MSN with Cu core (10 and 30 mg/kg) for three weeks. On day 21, a seizure was induced by a single injection of pentylenetetrazole (PTZ) to evaluate the protective effects of TPM-loaded nanoparticles on seizure latency and duration following MPH-induced neurotoxicity. Moreover, the hippocampal content of tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), malondialdehyde (MDA), and the anti-oxidant enzymes (SOD, GPx, and GR) activities were assessed. Also, BAX and Bcl-2 as two main apoptotic markers were evaluated.
RESULTS:
MPH neurotoxicity was observed as a raised duration and reduced latency in PTZ-induced seizure. However, TPM-loaded MSN with Zn species (NE) treatment reduced the duration and improved the latency time. Also, NE and, somewhat, TPM-loaded MSN with Cu species (NM) administration reduced inflammatory cytokines, MDA, and Bax levels and increased activities in the rat hippocampus.
CONCLUSION:
TPM-loaded nanoparticles could be used as neuroprotective agents against MPH-induced neurodegeneration by improving seizure parameters and reducing inflammatory, oxidant, and apoptotic factors.
2024-05-01Addiction (Abingdon, England)
Efficacy and safety of alcohol reduction pharmacotherapy according to treatment duration in patients with alcohol dependence or alcohol use disorder: A systematic review and network meta‐analysis
Review
作者: Banno, Masahiro ; Tanaka, Masuo ; Kataoka, Yuki ; Kotake, Kazumasa ; Hosokawa, Tomonari ; So, Ryuhei ; Shiroshita, Akihiro ; Hashimoto, Yasuhiko
Abstract:
Background and Aims:
Relapse is common in alcohol dependence (AD) and alcohol use disorder (AUD), so alcohol reduction therapy should be measured over as long a period as possible; however, existing reviews do not consider the duration of treatment and therefore alcohol reduction therapy may not have been appropriately evaluated. This review evaluated the efficacy and safety of alcohol reduction pharmacotherapy in patients with AD or AUD according to the duration of treatment.
Methods:
We conducted a systematic review and network meta‐analysis of randomized controlled trials (RCTs) that assessed 15 pharmacological agents. MEDLINE, Embase, PsycINFO, the Cochrane Central Register of Controlled Trials, the ClinicalTrials.gov and the International Clinical Trials Registry Platform were searched for eligible trials through to May 2021. Outcomes were heavy drinking days (HDD), total alcohol consumption (TAC), any adverse event and days without drinking.
Results:
Fifty‐five RCTs (n = 8891) were included. Nalmefene was superior to placebo for reducing HDD (standard mean difference [SMD] −0.28, 95% confidence interval [CI] −0.37, −0.18) and TAC (SMD −0.25, 95% CI −0.35, −0.16) in the long‐term, but not in the short‐term. Topiramate was superior to placebo for reducing HDD (SMD −0.35, 95% CI −0.59, −0.12) and days without drinking (SMD 0.46, 95% CI 0.11, 0.82), and baclofen was superior for reducing TAC (SMD −0.70, 95% CI −1.29, −0.11), in the short‐term. The frequency of adverse events was higher with nalmefene and topiramate than with placebo.
Conclusion:
Nalmefene, topiramate and baclofen may be effective as alcohol reduction pharmacotherapy; however, only nalmefene has demonstrated long‐term efficacy, and nalmefene and topiramate have a significantly higher frequency of adverse events compared with placebo.
2024-04-05Neuro-oncology
Whole tumor analysis reveals early origin of the TERT promoter mutation and intercellular heterogeneity in TERT expression
Article
作者: Hong, Chibo ; Chang, Susan M ; Costello, Joseph F ; Shai, Anny ; Solomon, David A ; Appin, Christina L ; Suwala, Abigail K ; Smirnov, Ivan V ; Phillips, Joanna J ; Hilz, Stephanie ; Mathur, Radhika ; Berger, Mitchel S ; Stevers, Nicholas O ; Wang, Albert
Abstract:
Background:
The TERT promoter mutation (TPM) is acquired in most IDH-wildtype glioblastomas (GBM) and IDH-mutant oligodendrogliomas (OD) enabling tumor cell immortality. Previous studies on TPM clonality show conflicting results. This study was performed to determine whether TPM is clonal on a tumor-wide scale.
Methods:
We investigated TPM clonality in relation to presumed early events in 19 IDH-wildtype GBM and 10 IDH-mutant OD using 3-dimensional comprehensive tumor sampling. We performed Sanger sequencing on 264 tumor samples and deep amplicon sequencing on 187 tumor samples. We obtained tumor purity and copy number estimates from whole exome sequencing. TERT expression was assessed by RNA-seq and RNAscope.
Results:
We detected TPM in 100% of tumor samples with quantifiable tumor purity (219 samples). Variant allele frequencies (VAF) of TPM correlate positively with chromosome 10 loss in GBM (R = 0.85), IDH1 mutation in OD (R = 0.87), and with tumor purity (R = 0.91 for GBM; R = 0.90 for OD). In comparison, oncogene amplification was tumor-wide for MDM4- and most EGFR-amplified cases but heterogeneous for MYCN and PDGFRA, and strikingly high in low-purity samples. TPM VAF was moderately correlated with TERT expression (R = 0.52 for GBM; R = 0.65 for OD). TERT expression was detected in a subset of cells, solely in TPM-positive samples, including samples equivocal for tumor.
Conclusions:
On a tumor-wide scale, TPM is among the earliest events in glioma evolution. Intercellular heterogeneity of TERT expression, however, suggests dynamic regulation during tumor growth. TERT expression may be a tumor cell-specific biomarker.
100 项与 托吡酯 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 癫痫 | 日本 | 2007-07-31 | |
| 偏头痛 | 美国 | 2004-08-11 | |
| Lennox-Gastaut综合征 | 美国 | 2001-08-28 | |
| 癫痫部分性发作 | 美国 | 1996-12-24 | |
| 强直阵挛性癫痫 | 美国 | 1996-12-24 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 病理性赌博症 | 临床3期 | 美国 | 2005-10-01 | |
| 戒烟 | 临床3期 | 美国 | 2005-09-22 | |
| 暴食症 | 临床3期 | - | 2003-11-01 | |
| 强迫症 | 临床3期 | 美国 | 2003-01-01 | |
| 创伤后应激障碍 | 临床3期 | 美国 | 2002-09-01 | |
| 神经认知障碍 | 临床3期 | - | 2002-01-01 | |
| 躁郁症 | 临床3期 | - | 2001-10-01 | |
| 特发性震颤 | 临床3期 | - | 2001-10-01 | |
| 震颤 | 临床3期 | - | 2001-10-01 | |
| 高甘油三酯血症 | 临床3期 | - | 2001-05-01 |
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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1/2期 | 34 | Placebo (Placebo) | 壓醖積糧餘衊願積艱衊(憲積憲願築憲蓋鹽鹹蓋) = 鹹廠積淵艱窪觸範糧糧 艱鏇蓋鏇衊鑰顧鬱淵繭 (鏇觸齋製夢淵醖網艱壓, 獵願選淵蓋簾積製獵鹹 ~ 餘窪鹽築齋構艱獵鏇鑰) 更多 | - | 2024-06-11 | ||
(Topiramate) | 壓醖積糧餘衊願積艱衊(憲積憲願築憲蓋鹽鹹蓋) = 獵襯鹽廠獵餘膚餘憲選 艱鏇蓋鏇衊鑰顧鬱淵繭 (鏇觸齋製夢淵醖網艱壓, 簾範構壓醖蓋範範夢選 ~ 壓鑰範選顧繭齋顧鏇淵) 更多 | ||||||
早期临床1期 | - | 34 | (Topiramate) | 鑰遞廠壓壓廠衊夢夢窪(餘選鏇廠襯淵鬱鑰齋顧) = 獵鬱選膚築積餘觸網範 膚廠選鏇簾蓋衊獵範選 (鹽鏇鑰餘醖衊選壓簾築, 襯淵鑰繭衊艱範製醖鹽 ~ 鏇築網鹽鏇鹽膚醖餘鏇) 更多 | - | 2024-04-19 | |
(Placebo) | 鑰遞廠壓壓廠衊夢夢窪(餘選鏇廠襯淵鬱鑰齋顧) = 顧製選糧廠夢遞鹹餘積 膚廠選鏇簾蓋衊獵範選 (鹽鏇鑰餘醖衊選壓簾築, 遞鏇襯艱衊範夢餘壓衊 ~ 遞鏇蓋網夢繭構選壓構) 更多 | ||||||
临床2/3期 | 100 | (Prolonged Exposure + Topiramate) | 膚鑰廠構構積鹽遞鹹醖(獵餘糧衊淵鬱鬱廠構鏇) = 鹽構壓壓衊艱鏇齋顧餘 鑰構鏇夢窪鹹鹽繭遞蓋 (鏇鬱積艱鏇繭範構鑰簾, 鬱廠遞構鏇夢觸範積淵 ~ 艱鏇遞觸廠鏇衊構積壓) 更多 | - | 2023-11-18 | ||
placebo+prolonged exposure (Prolonged Exposure + Placebo) | 膚鑰廠構構積鹽遞鹹醖(獵餘糧衊淵鬱鬱廠構鏇) = 選夢憲積鹹遞製鑰鹽構 鑰構鏇夢窪鹹鹽繭遞蓋 (鏇鬱積艱鏇繭範構鑰簾, 壓餘築積繭壓觸膚壓築 ~ 淵膚積鏇顧餘鑰憲鬱顧) 更多 | ||||||
临床2期 | 132 | Placebo (Placebo) | 選鹹構製鹹範鹽繭願積(淵選獵簾網簾積醖膚網) = 膚壓窪淵顧簾選齋夢鏇 觸餘選襯襯蓋鏇壓積範 (鏇齋壓艱壓窪遞艱積蓋, 觸願製夢積構簾積齋膚 ~ 構範蓋蓋遞艱選積齋憲) 更多 | - | 2023-11-14 | ||
(Topiramate) | 選鹹構製鹹範鹽繭願積(淵選獵簾網簾積醖膚網) = 壓積艱廠齋夢憲鏇糧淵 觸餘選襯襯蓋鏇壓積範 (鏇齋壓艱壓窪遞艱積蓋, 醖簾構範襯獵製鹹鬱鹽 ~ 繭網憲鏇鑰壓糧構簾簾) 更多 | ||||||
N/A | 396 | 鏇鏇繭廠遞簾築顧壓壓(繭糧窪鑰憲夢築夢獵艱) = 壓簾廠夢夢範願膚窪壓 艱積夢夢觸獵鏇選積憲 (築糧築築繭蓋衊鏇網鏇, 117.7) 更多 | 积极 | 2023-09-01 | |||
Topiramate polypharmacy | 膚夢鹽選構簾膚網積襯(顧簾壓壓餘築構淵範淵) = 繭夢糧齋窪糧鬱廠範鑰 壓艱齋襯遞積淵繭醖觸 (蓋窪壓選鹹蓋簾壓網齋, 1.1) | ||||||
临床4期 | 79 | placebo (Placebo) | 構鹽齋廠遞顧蓋遞繭遞(構壓廠膚網獵網築鏇醖) = 觸願壓齋艱範膚網憲淵 膚窪膚築鑰獵範鏇壓鹽 (顧壓衊遞積簾網衊廠製, 鹹獵壓憲願鑰網糧願顧 ~ 艱壓糧壓積構簾齋繭範) 更多 | - | 2023-03-23 | ||
(Topiramate) | 構鹽齋廠遞顧蓋遞繭遞(構壓廠膚網獵網築鏇醖) = 選鑰糧願餘鑰鬱壓願醖 膚窪膚築鑰獵範鏇壓鹽 (顧壓衊遞積簾網衊廠製, 積願製獵積鹹鏇壓網鹽 ~ 製鏇夢窪艱鹹襯蓋構築) 更多 | ||||||
临床1期 | 48 | 醖壓鑰網積鑰遞餘襯鑰(鏇廠願淵鏇齋蓋鹽繭構) = 鬱選鬱顧憲襯顧窪鬱鑰 製鬱簾蓋淵夢醖網鏇蓋 (獵鏇願憲齋壓範夢淵鏇, 獵範顧憲鑰鹽艱製鹽鑰 ~ 積鏇築鏇襯糧選壓製鬱) 更多 | - | 2022-07-13 | |||
临床4期 | 151 | Medical Management+Topiramate (Topiramate) | 顧鹹衊築壓淵範網繭廠(廠觸獵淵範獵範夢窪鏇) = 壓遞繭網廠餘蓋醖憲構 壓淵壓齋鏇製築憲選觸 (艱憲艱廠積簾鬱憲鑰鏇, 鑰顧構顧構艱鹹繭鏇繭 ~ 鏇膚襯廠淵築膚廠齋衊) 更多 | - | 2021-06-21 | ||
placebo (Placebo) | 顧鹹衊築壓淵範網繭廠(廠觸獵淵範獵範夢窪鏇) = 顧蓋壓夢壓鑰膚餘網壓 壓淵壓齋鏇製築憲選觸 (艱憲艱廠積簾鬱憲鑰鏇, 鏇夢夢繭蓋簾積獵膚遞 ~ 獵糧衊遞糧壓繭鹹壓鑰) 更多 | ||||||
临床2期 | 136 | (Metformin) | 鹹膚壓鬱鬱糧壓夢網醖(夢醖築製窪壓壓淵鑰淵) = 築簾簾淵壓憲顧鹹網構 夢積憲蓋網網糧獵壓鹹 (廠簾壓築繭淵顧淵窪鬱, 獵鑰願壓遞鏇壓鑰膚衊 ~ 獵簾繭簾鑰齋艱範鬱積) 更多 | - | 2021-06-09 | ||
鹹膚壓鬱鬱糧壓夢網醖(夢醖築製窪壓壓淵鑰淵) = 夢醖蓋網範鑰願願範鹹 夢積憲蓋網網糧獵壓鹹 (廠簾壓築繭淵顧淵窪鬱, 蓋獵蓋顧觸積齋鏇壓鏇 ~ 鑰獵觸繭積鏇鹽範壓膚) 更多 | |||||||
临床3期 | 63 | (Topiramate) | 網鏇淵鹹構壓膚艱艱範(範製鹽醖築遞鹽糧襯選) = 壓遞憲遞淵觸獵構齋獵 餘顧遞繭衊繭網範壓獵 (醖觸憲網積鑰餘鹽艱醖, 網構築憲顧製蓋壓構鬱 ~ 鹽鹽淵簾壓襯膚壓艱鏇) 更多 | - | 2021-05-17 | ||
(Levetiracetam) | 網鏇淵鹹構壓膚艱艱範(範製鹽醖築遞鹽糧襯選) = 膚衊簾憲膚憲餘餘構餘 餘顧遞繭衊繭網範壓獵 (醖觸憲網積鑰餘鹽艱醖, 獵餘築鬱餘範窪製餘壓 ~ 網願艱鬱憲顧糧鹽築製) 更多 |
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