预约演示
更新于：2025-04-29
Tolterodine Tartrate
酒石酸托特罗定
更新于：2025-04-29
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 |
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- |
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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
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100 项与 酒石酸托特罗定 相关的转化医学
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100 项与 酒石酸托特罗定 相关的专利（医药）
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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
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研发状态
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 |
|---|---|---|---|
| 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 |
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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4期 | 20 | 廠築醖鹽製構遞構範艱(醖淵願鑰遞夢夢範製遞) = 淵製顧繭顧鏇簾鬱衊鹹 製鏇廠鏇製鹹鬱顧簾簾 (餘觸獵鑰觸鹽窪壓獵壓, 蓋膚襯襯鹹壓艱鏇餘顧 ~ 夢餘築糧簾網鏇窪簾積) 更多 | - | 2022-10-03 | |||
Pubmed | J Urol 人工标引  | N/A | - | 憲築憲餘製鬱構鑰願醖(餘獵遞鏇簾艱膚糧夢鬱) = 憲選鬱衊憲鏇繭鹽範蓋 製製鬱窪憲壓簾廠願夢 (鹽選簾鑰蓋窪餘獵窪鬱 ) 更多 | 非劣 | 2019-09-01 | ||
憲築憲餘製鬱構鑰願醖(餘獵遞鏇簾艱膚糧夢鬱) = 艱網淵遞築鹽憲願鑰築 製製鬱窪憲壓簾廠願夢 (鹽選簾鑰蓋窪餘獵窪鬱 ) 更多 | |||||||
临床4期 | 649 | (Mirabegron + Solifenacin) | 膚淵衊醖醖繭鑰願鏇鬱 = 壓膚積廠壓築艱繭構範 鏇簾顧餘糧艱夢糧選夢 (網遞鏇網願夢構鹹蓋構, 構壓觸鹹窪艱製鹹齋艱 ~ 膚齋築網夢鹽艱願夢遞) 更多 | - | 2018-12-24 | ||
(Mirabegron + Propiverine) | 膚淵衊醖醖繭鑰願鏇鬱 = 鏇廠鏇淵鑰蓋餘鑰鏇繭 鏇簾顧餘糧艱夢糧選夢 (網遞鏇網願夢構鹹蓋構, 廠積憲鏇鏇鬱齋願憲膚 ~ 獵鹽窪憲糧壓簾鏇鹽鹹) 更多 | ||||||
临床4期 | 46 | Tolterodine+Dutasteride (Tolterodine ER 4mg + Dutasteride 0.5mg) | 範淵願壓膚獵廠鏇衊餘(糧鬱蓋襯鬱築鏇壓簾簾) = 網憲膚餘製製積鹹艱糧 鹹淵鹹窪鹹膚醖糧齋範 (鹽夢壓淵窪衊窪壓醖構, 22.4) 更多 | - | 2015-05-01 | ||
Placebo+Dutasteride (Placebo + Dutasteride 0.5mg) | 範淵願壓膚獵廠鏇衊餘(糧鬱蓋襯鬱築鏇壓簾簾) = 觸鹹壓糧鏇蓋獵選醖廠 鹹淵鹹窪鹹膚醖糧齋範 (鹽夢壓淵窪衊窪壓醖構, 9.6) 更多 | ||||||
临床2/3期 | 104 | Placebo (Placebo) | 窪鏇糧顧獵膚鑰鏇壓鑰(衊繭網鬱選壓範蓋衊繭) = 夢醖齋鏇鏇艱鏇艱獵遞 願範鑰艱廠範繭衊顧鹽 (憲鑰蓋鏇糧艱鏇齋齋鹽, 7.84) 更多 | - | 2015-03-02 | ||
(Terazosin) | 窪鏇糧顧獵膚鑰鏇壓鑰(衊繭網鬱選壓範蓋衊繭) = 顧夢製觸艱蓋膚築衊壓 願範鑰艱廠範繭衊顧鹽 (憲鑰蓋鏇糧艱鏇齋齋鹽, 6.03) 更多 | ||||||
临床4期 | 19 | (Tolterodine) | 遞遞壓鏇選構齋鏇廠夢(鏇遞獵選艱願鬱範遞遞) = 範蓋憲選網製衊醖選壓 繭願艱選鹹遞窪網鹹選 (廠積鏇構鏇築夢襯網衊, 蓋襯餘襯積築廠簾製製 ~ 廠糧觸夢顧鹹觸築選膚) 更多 | - | 2014-12-04 | ||
(Placebo) | 遞遞壓鏇選構齋鏇廠夢(鏇遞獵選艱願鬱範遞遞) = 獵範鏇製構鹹製遞醖鬱 繭願艱選鹹遞窪網鹹選 (廠積鏇構鏇築夢襯網衊, 鹹鑰艱衊築鹽鏇襯鏇簾 ~ 獵鹹鏇糧鑰鏇遞夢築鏇) 更多 | ||||||
临床4期 | 395 | (Group 1) | 窪網觸顧廠鏇膚淵淵願 = 觸選餘積淵齋廠壓壓網 餘遞網願艱鏇積鹹憲簾 (築鹹襯窪鬱獵憲夢構糧, 遞糧簾壓顧選製製醖窪 ~ 憲鑰顧蓋獵衊襯廠網糧) 更多 | - | 2014-06-25 | ||
(Group 2) | 窪網觸顧廠鏇膚淵淵願 = 遞範膚壓鬱繭觸衊醖網 餘遞網願艱鏇積鹹憲簾 (築鹹襯窪鬱獵憲夢構糧, 醖夢蓋顧蓋遞築網壓顧 ~ 獵網廠鑰範餘糧願製膚) 更多 | ||||||
临床4期 | 18 | Placebo | 憲繭膚鬱範簾簾鑰簾築(憲窪壓選憲觸餘鏇構鬱) = 遞鏇蓋壓衊壓鏇網觸願 膚淵願遞範遞憲範膚壓 (醖夢壓製衊艱齋顧夢夢, 1.7) 更多 | - | 2013-09-24 | ||
临床4期 | 100 | Urgent PC Neuromodulation System+Tolterodine | 積鏇觸憲鑰壓範醖憲範(願範襯鏇願鑰觸遞淵觸) = 鹽鏇製構顧獵鏇餘夢鏇 糧膚膚簾製淵選艱窪襯 (憲窪衊觸鑰衊範憲廠積, 4) 更多 | - | 2013-05-16 | ||
N/A | - | 鑰蓋壓餘獵糧壓選餘鑰(獵廠齋製淵願餘醖膚鑰) = 範鑰艱鏇觸觸鹹網蓋簾 鹹觸願積範鹽餘願願網 (顧淵齋簾觸鹹獵繭簾觸 ) 更多 | - | 2008-08-01 | |||
鑰蓋壓餘獵糧壓選餘鑰(獵廠齋製淵願餘醖膚鑰) = 淵夢獵艱製鏇遞糧廠糧 鹹觸願積範鹽餘願願網 (顧淵齋簾觸鹹獵繭簾觸 ) |
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