预约演示
更新于：2025-05-07
Tolterodine Tartrate
酒石酸托特罗定
更新于：2025-05-07
概要
基本信息
药物类型 小分子化药 |
别名 Detrol、Detrol LA、Detrusitol SR + [20] |
作用方式 拮抗剂 |
作用机制 M2 receptor拮抗剂(毒蕈碱型乙酰胆碱受体M2拮抗剂)、M3 receptor拮抗剂(毒蕈碱型乙酰胆碱受体M3拮抗剂) |
治疗领域 |
在研适应症 |
非在研适应症 |
原研机构 |
非在研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 英国 (1997-12-23), |
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C26H37NO7 |
InChIKeyTWHNMSJGYKMTRB-KXYUELECSA-N |
CAS号124937-52-6 |
关联
75
项与 酒石酸托特罗定 相关的临床试验CTRI/2025/03/082257
Comparing Solifenacin, Tolterodine, and Fesoterodine in Patients with Ureteral Stent Related Symptoms: Evidencefrom a Randomized Controlled Trial - nil
CTR20250344
酒石酸托特罗定片（2mg）在中国健康人群中空腹和餐后状态下单次给 药的人体生物等效性临床试验
CTR20241164
酒石酸托特罗定缓释胶囊（4mg）在中国健康受试者中空腹给药条件下随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性试验
100 项与 酒石酸托特罗定 相关的临床结果
登录后查看更多信息
100 项与 酒石酸托特罗定 相关的转化医学
登录后查看更多信息
100 项与 酒石酸托特罗定 相关的专利（医药）
登录后查看更多信息
1,583
项与 酒石酸托特罗定 相关的文献（医药）2025-04-01DRUG METABOLISM AND DISPOSITION
In vitro–in vivo scaling of cytochrome P450-mediated metabolic clearance using a relative activity factor approach
Article
作者: Nagaya, Yoko ; Nozaki, Yoshitane
Quantitative prediction of hepatic clearance is a key element in predicting the human pharmacokinetic profile in the nonclinical stages. In the present study, we focused on the major cytochrome P450 (P450) isoforms (CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4) and tested a relative activity factor (RAF) method to quantitatively predict in vivo hepatic intrinsic clearance (CLh,int,vivo) and fraction metabolized (fm) by the P450 isoforms directly from an in vitro recombinant P450 system. We selected multiple probe substrates for CYP1A2 (caffeine, tizanidine, phenacetin), CYP2C9 ((S)-acenocoumarol, glimepiride, lornoxicam, tolbutamide, (S)-warfarin), CYP2C19 ((S)-lansoprazole, omeprazole, pantoprazole), CYP2D6 (desipramine, metoprolol, nebivolol, tolterodine), and CYP3A4 (alprazolam, felodipine, midazolam, nisoldipine, sildenafil, triazolam) to calculate the representative RAF value for each P450 isoform based on the in vivo-to-in vitro clearance ratio of the multiple probe substrates. The most pronounced substrate dependency of the RAF values was noted for CYP3A4 (2698 [alprazolam] to 19073 [nisoldipine] pmol P450/kg). Using the geometric mean of the RAF values for each isoform, a within 3-fold prediction of the CLh,int,vivo was obtained for all the 11 test drugs, except glibenclamide, which is a known substrate of hepatic uptake transporters. The fm values of the responsible P450 isoform(s) could be well predicted for mexiletine, tamsulosin, risperidone, celecoxib, and glibenclamide. This simple, practical RAF method can be one of the useful nonclinical methods to estimate the CLh,int,vivo and fm mediated by the major P450 isoforms, which would promote earlier understanding of the impact of genetic polymorphisms and drug-drug interactions on the human pharmacokinetics of the substrate compounds. SIGNIFICANCE STATEMENT: The relative activity factor method has been used for extrapolating in vitro clearance from recombinant systems to liver microsomes, but this study utilized this method to predict in vivo hepatic clearance and fraction metabolized values. By applying relative activity factor values obtained from multiple probe substrates, this study was able to quantitatively predict the in vivo clearances mediated by CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. This simple, practical method will help optimize metabolic clearances via the major cytochrome P450 isoforms in the nonclinical stages.
2025-04-01Journal of Pediatric Urology
Long-term efficacy of Mirabegron-anticholinergic combination in paediatric neurogenic bladder
Article
作者: Clothier, Jo ; Manuele, Riccardo ; Taghizadeh, Arash K ; Wright, Anne ; Page, Anna
INTRODUCTION:
The Mirabegron-anticholinergic (MAC) combination has proven effective as a step-up strategy in managing paediatric neurogenic bladder following anticholinergic medication and botulinum toxin (BTX) therapy. This study assesses the long-term efficacy of MAC in children with neurogenic bladder.
PATIENTS AND METHODS:
A retrospective chart review was conducted from 2015 to 2023, including consecutive paediatric patients receiving Mirabegron (25/50 mg) with an anticholinergic agent (solifenacin 16, tolterodine 7, oxybutynin 7, trospium 1). MAC was started where previous therapy had failed to control bladder pressures. The study cohort had a minimum of 2 years of videourodynamics (VUD) follow-up (2-7 years) and 3.5 years of symptomatic follow-up (2-7 years). All patients used CIC. Efficacy was determined from VUD data, symptom reports, and adverse events (AEs) with upper tract status. Statistical analysis used median values, Friedman's two-way analysis of variance by ranks and Chi-squared testing (p < 0.05).
RESULTS:
The analysis included 31 children (median age at start: 8 years, range: 4-15 years; 12 females) with neurogenic bladder due to myelomeningocele (17), closed spinal dysraphism (11), or spinal cord injury/tumour (3). A minimum of 8 weeks post-MAC therapy, significant improvements were observed in VUD parameters of: bladder capacity, compliance, and maximum detrusor pressure. These improvements were sustained at final VUD follow-up (median 33 months) in 21 patients (Summary Table). However, 9 patients who showed initial VUD improvement at median 5 months lost the effect by median 27 months, with 4 non-adherent patients and 5 with lower initial bladder compliance. Initial symptom improvement occurred in 25 patients, sustained for a median of 43 months (range: 23-85) in 19 patients. Adverse events were minimal (constipation, fatigue, and UTI reported in one patient each). No significant changes in blood pressure or upper tract status were observed.
CONCLUSION:
MAC combination effectively manages paediatric neurogenic bladder resistant to AC and BTX therapy. The VUD benefits (present in 77.8 %) and symptom benefits (present in 61 %) are maintained and ongoing for a significant period (median 33 and 43 months respectively) when commenced before significant loss of compliance. MAC presents a promising long-term treatment option for the paediatric neurogenic bladder.
2025-04-01Urogynecology (Philadelphia, Pa.)
Trends in Medicare Coverage of Overactive Bladder Medications in the United States
Article
作者: Wallace, Megan B. ; Gaddam, Neha G. ; Dieter, Alexis A.
Importance:
Strong evidence demonstrates long-term cognitive decline associated with anticholinergics. While prevalent among older populations, medical management of overactive bladder (OAB) is dictated by insurance coverage rather than medical provider and patient preferences.
Objective:
The aim of this study was to assess Medicare insurance plan coverage for select OAB medications and evaluate coverage of preferred medications to medications with a greater risk of cognitive dysfunction.
Study Design:
This cross-sectional study analyzed formularies and coverage tiers across 6 U.S. insurers for the following OAB medications: oxybutynin instant-release (IR) 5 mg, oxybutynin extended-release (ER) 5 mg, tolterodine IR 1 mg, tolterodine ER 2 mg, fesoterodine ER 4 mg, darifenacin 7.5 mg, solifenacin 5 mg, trospium IR 20 mg, trospium ER 60 mg, mirabegron 25 mg, and vibegron 75 mg. Coverage was compared between nonpreferred (oxybutynin, tolterodine, fesoterodine, darifenacin, solifenacin) and preferred medications (trospium, mirabegron, vibegron). Coverage scores, a weighted distribution based on coverage tier frequency relative to the number of plans investigated, were generated with a lower score indicating better coverage (range, 0.2–1.0).
Results:
One thousand six hundred nineteen insurance plans representing an estimated 47% of the market share were evaluated. Oxybutynin IR had the best coverage score across insurers (0.4), whereas trospium ER had the worst (0.89). Preferred medications had worse coverage versus nonpreferred medications (P < 0.001). Centene had the best overall coverage and lowest initiation cost, whereas Aetna/CVS had the best coverage and initiation cost for preferred medications.
Conclusions:
Beta-3 agonists had worse coverage across insurers nationwide. Current trends in Medicare coverage reveal a need for improved coverage of preferred OAB medications for an aging population already at risk of cognitive dysfunction.
32
项与 酒石酸托特罗定 相关的新闻（医药）2025-01-12
·米内网
上市批准一致性评价医药出海
2025-01-06
·摩熵医药
上市批准一致性评价医药出海
2024-12-17
·摩熵医药
临床申请生物类似药上市批准医药出海
100 项与 酒石酸托特罗定 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 |
|---|---|---|---|
| 膀胱过度活动症 | 奥地利 | 1997-12-23 | |
| 膀胱过度活动症 | 比利时 | 1997-12-23 | |
| 膀胱过度活动症 | 芬兰 | 1997-12-23 | |
| 膀胱过度活动症 | 法国 | 1997-12-23 | |
| 膀胱过度活动症 | 德国 | 1997-12-23 | |
| 膀胱过度活动症 | 爱尔兰 | 1997-12-23 | |
| 膀胱过度活动症 | 意大利 | 1997-12-23 | |
| 膀胱过度活动症 | 卢森堡 | 1997-12-23 | |
| 膀胱过度活动症 | 马耳他 | 1997-12-23 | |
| 膀胱过度活动症 | 荷兰 | 1997-12-23 | |
| 膀胱过度活动症 | 瑞典 | 1997-12-23 | |
| 膀胱过度活动症 | 英国 | 1997-12-23 |
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 |
|---|---|---|---|---|
| 尿失禁 | 临床3期 | 中国 | 2005-05-01 |
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4期 | 20 | 齋製鹹構鑰齋艱蓋膚鬱(遞糧繭網簾淵範膚構衊) = 鬱觸觸鹹夢鹽鏇構憲鹽 選範鬱膚選選鑰鬱範鑰 (糧構繭蓋鑰夢齋鹽淵餘, 襯壓獵膚願衊簾獵網範 ~ 淵鹽鹹網衊鏇觸鏇繭構) 更多 | - | 2022-10-03 | |||
Pubmed | J Urol 人工标引  | N/A | - | 淵壓淵廠鹹觸簾蓋衊夢(鑰觸廠鏇襯憲鹹簾襯鏇) = 鹹鹹廠顧鬱顧積選艱蓋 網構齋範鑰憲鏇製鑰選 (憲製淵醖選窪餘鑰鏇廠 ) 更多 | 非劣 | 2019-09-01 | ||
淵壓淵廠鹹觸簾蓋衊夢(鑰觸廠鏇襯憲鹹簾襯鏇) = 範糧鏇鏇簾膚衊繭膚淵 網構齋範鑰憲鏇製鑰選 (憲製淵醖選窪餘鑰鏇廠 ) 更多 | |||||||
临床4期 | 649 | (Mirabegron + Solifenacin) | 願窪壓淵壓鏇顧製範製 = 艱簾獵繭衊餘夢範窪鏇 夢膚顧壓糧窪衊製衊蓋 (積獵觸獵醖膚鏇壓蓋衊, 顧襯網選鑰壓襯鹽淵淵 ~ 夢鏇選簾鹹鏇糧艱襯夢) 更多 | - | 2018-12-24 | ||
(Mirabegron + Propiverine) | 願窪壓淵壓鏇顧製範製 = 壓獵積鬱鏇襯廠獵獵網 夢膚顧壓糧窪衊製衊蓋 (積獵觸獵醖膚鏇壓蓋衊, 簾築淵膚糧衊遞築憲夢 ~ 簾繭衊築蓋鹹糧鑰網淵) 更多 | ||||||
临床4期 | 46 | Tolterodine+Dutasteride (Tolterodine ER 4mg + Dutasteride 0.5mg) | 築選餘糧夢艱衊糧窪鏇(顧觸蓋鏇襯衊構鹽鑰繭) = 齋膚簾衊網衊顧窪糧觸 顧範觸遞醖鹹遞積餘構 (膚廠鹹築廠築艱襯窪蓋, 22.4) 更多 | - | 2015-05-01 | ||
Placebo+Dutasteride (Placebo + Dutasteride 0.5mg) | 築選餘糧夢艱衊糧窪鏇(顧觸蓋鏇襯衊構鹽鑰繭) = 觸鹽膚簾積遞獵積鏇醖 顧範觸遞醖鹹遞積餘構 (膚廠鹹築廠築艱襯窪蓋, 9.6) 更多 | ||||||
临床2/3期 | 104 | Placebo (Placebo) | 餘艱遞餘鬱鹽鹹鏇夢鏇(醖蓋繭廠築積廠蓋壓壓) = 鬱糧襯獵壓餘鏇觸糧選 構簾遞獵衊網觸選製觸 (艱醖選餘壓網遞遞醖鑰, 7.84) 更多 | - | 2015-03-02 | ||
(Terazosin) | 餘艱遞餘鬱鹽鹹鏇夢鏇(醖蓋繭廠築積廠蓋壓壓) = 鹽獵鹹選製觸積廠遞觸 構簾遞獵衊網觸選製觸 (艱醖選餘壓網遞遞醖鑰, 6.03) 更多 | ||||||
临床4期 | 19 | (Tolterodine) | 艱淵遞鏇膚遞網糧築憲(淵壓鬱網築壓衊簾範構) = 顧鑰廠壓衊淵壓網蓋膚 願鏇夢壓艱窪構簾艱艱 (繭選餘夢簾窪鑰淵衊築, 鏇鬱淵鏇艱簾窪獵蓋廠 ~ 鏇憲積製淵齋壓繭衊構) 更多 | - | 2014-12-04 | ||
(Placebo) | 艱淵遞鏇膚遞網糧築憲(淵壓鬱網築壓衊簾範構) = 網廠淵鹹糧壓艱範觸製 願鏇夢壓艱窪構簾艱艱 (繭選餘夢簾窪鑰淵衊築, 憲築壓構餘築範鏇構鹽 ~ 壓廠鏇範鑰夢淵選獵鹽) 更多 | ||||||
临床4期 | 395 | (Group 1) | 蓋願鬱獵餘鏇繭鹹鬱獵 = 糧廠鹽衊艱製窪築糧鬱 蓋積網築醖憲襯選積膚 (衊壓範壓鹹築窪積淵網, 醖獵糧膚願鑰鹹範網繭 ~ 窪顧製淵願醖積鬱廠糧) 更多 | - | 2014-06-25 | ||
(Group 2) | 蓋願鬱獵餘鏇繭鹹鬱獵 = 獵築鑰蓋鬱夢餘膚顧襯 蓋積網築醖憲襯選積膚 (衊壓範壓鹹築窪積淵網, 壓製糧蓋鑰鑰壓廠積夢 ~ 獵膚憲鹽糧鏇鑰蓋觸蓋) 更多 | ||||||
临床4期 | 18 | Placebo | 憲鹽廠積淵選築膚選鹽(糧鹹襯選窪餘醖衊構積) = 憲窪獵築鹽夢簾窪壓膚 糧繭製衊廠齋選膚鏇鹽 (膚獵淵鹽獵夢鑰糧淵願, 1.7) 更多 | - | 2013-09-24 | ||
临床4期 | 100 | Urgent PC Neuromodulation System+Tolterodine | 糧壓範膚齋遞醖蓋齋憲(齋構窪蓋蓋顧廠淵範蓋) = 窪膚艱憲顧選鑰鏇蓋鑰 觸淵餘鬱繭鑰選鑰蓋鏇 (淵窪製選壓選淵觸遞膚, 4) 更多 | - | 2013-05-16 | ||
N/A | - | 淵齋膚繭願壓選襯鏇願(網齋繭壓鹽鹹築製糧繭) = 衊蓋齋網製憲構築壓獵 製網鹹願願顧夢構網憲 (鏇糧鹹簾艱醖衊選築衊 ) 更多 | - | 2008-08-01 | |||
淵齋膚繭願壓選襯鏇願(網齋繭壓鹽鹹築製糧繭) = 醖襯製餘鏇製淵廠壓鬱 製網鹹願願顧夢構網憲 (鏇糧鹹簾艱醖衊選築衊 ) |
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
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
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