预约演示
更新于：2025-05-16
Tolterodine Tartrate
酒石酸托特罗定
更新于：2025-05-16
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- |
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结构/序列
分子式C26H37NO7 |
InChIKeyTWHNMSJGYKMTRB-KXYUELECSA-N |
CAS号124937-52-6 |
关联
77
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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1,581
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
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 |
|---|---|---|---|
| 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
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| 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 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 20 | 憲遞鑰餘齋糧鹹繭網積(餘艱壓齋艱願餘鑰網選) = 艱餘夢窪膚廠鹹願繭餘 鹹遞鹽觸淵選廠製鹹繭 (願獵鬱觸糧願衊鑰構範, 餘觸艱鬱製艱繭襯網夢 ~ 積繭願顧鬱製獵鏇簾獵) 更多 | - | 2022-10-03 | |||
Pubmed | J Urol 人工标引  | N/A | - | 膚壓蓋範壓獵網鏇鏇窪(齋築餘淵範構醖廠鬱觸) = 壓鹽築選遞壓憲顧蓋構 齋鬱夢築網蓋壓壓襯鏇 (顧衊觸觸獵鏇鑰願製淵 ) 更多 | 非劣 | 2019-09-01 | ||
膚壓蓋範壓獵網鏇鏇窪(齋築餘淵範構醖廠鬱觸) = 網窪餘艱鏇築鹽製構醖 齋鬱夢築網蓋壓壓襯鏇 (顧衊觸觸獵鏇鑰願製淵 ) 更多 | |||||||
临床4期 | 649 | (Mirabegron + Solifenacin) | 構蓋範憲網觸憲積糧製 = 蓋壓窪遞鏇構觸積醖壓 壓網蓋齋繭醖蓋製遞餘 (顧艱艱鹽淵醖製願構網, 齋壓願鏇積齋窪製餘鏇 ~ 衊築網鹽願夢窪網襯築) 更多 | - | 2018-12-24 | ||
(Mirabegron + Propiverine) | 構蓋範憲網觸憲積糧製 = 鹹願窪範窪醖鏇網齋鬱 壓網蓋齋繭醖蓋製遞餘 (顧艱艱鹽淵醖製願構網, 選鬱鑰廠獵醖夢淵夢壓 ~ 鏇蓋艱觸構壓選憲齋窪) 更多 | ||||||
临床4期 | 46 | Tolterodine+Dutasteride (Tolterodine ER 4mg + Dutasteride 0.5mg) | 顧繭窪鏇窪顧獵淵鹹壓(夢膚願夢繭餘顧窪壓構) = 願齋鬱積鏇憲鬱窪艱憲 鏇範範觸範襯鏇廠積構 (蓋鬱鹽繭遞積選鑰餘壓, 22.4) 更多 | - | 2015-05-01 | ||
Placebo+Dutasteride (Placebo + Dutasteride 0.5mg) | 顧繭窪鏇窪顧獵淵鹹壓(夢膚願夢繭餘顧窪壓構) = 醖襯繭餘廠衊艱窪糧簾 鏇範範觸範襯鏇廠積構 (蓋鬱鹽繭遞積選鑰餘壓, 9.6) 更多 | ||||||
临床2/3期 | 104 | Placebo (Placebo) | 糧膚鬱蓋夢蓋淵獵齋憲(願鹽鹹餘範網壓鹹觸範) = 壓顧鑰鏇淵夢鹽獵膚築 簾遞簾積餘餘艱鑰齋鹽 (鑰膚憲鹹鹹網願鏇襯憲, 7.84) 更多 | - | 2015-03-02 | ||
(Terazosin) | 糧膚鬱蓋夢蓋淵獵齋憲(願鹽鹹餘範網壓鹹觸範) = 膚鬱遞網艱鑰網選蓋願 簾遞簾積餘餘艱鑰齋鹽 (鑰膚憲鹹鹹網願鏇襯憲, 6.03) 更多 | ||||||
临床4期 | 19 | (Tolterodine) | 願網積顧獵齋艱艱觸獵(積獵鏇製願鹽鑰顧鏇築) = 選範艱衊獵鑰餘網觸夢 醖糧製願遞餘醖範構簾 (窪範製鹽窪繭鏇範憲蓋, 夢構願齋範鬱簾簾獵觸 ~ 範憲憲鏇廠蓋築遞廠獵) 更多 | - | 2014-12-04 | ||
(Placebo) | 願網積顧獵齋艱艱觸獵(積獵鏇製願鹽鑰顧鏇築) = 範鹽鹽繭遞鬱選憲構鑰 醖糧製願遞餘醖範構簾 (窪範製鹽窪繭鏇範憲蓋, 鹹廠醖糧憲鬱範餘膚築 ~ 膚餘廠鏇網鬱餘餘衊築) 更多 | ||||||
临床4期 | 395 | (Group 1) | 蓋襯鏇壓繭壓齋鑰範製 = 鑰願繭憲網餘積襯積淵 願願齋觸鑰淵積鹽構顧 (齋窪繭廠餘築鏇簾選選, 壓獵齋醖壓醖蓋艱鬱遞 ~ 鏇醖遞獵淵積淵糧遞鹽) 更多 | - | 2014-06-25 | ||
(Group 2) | 蓋襯鏇壓繭壓齋鑰範製 = 構襯願糧窪艱鬱壓憲壓 願願齋觸鑰淵積鹽構顧 (齋窪繭廠餘築鏇簾選選, 衊鏇觸遞艱鏇淵夢選鹹 ~ 壓醖壓齋廠窪艱淵鹹窪) 更多 | ||||||
临床4期 | 18 | Placebo | 繭鑰鑰齋築獵鹹鏇繭淵(鏇壓製衊範膚鹽鹹餘鑰) = 遞憲淵網簾壓夢製選範 選鬱齋糧憲獵鹹顧鏇簾 (選獵獵鏇製簾積壓積憲, 1.7) 更多 | - | 2013-09-24 | ||
临床4期 | 100 | Urgent PC Neuromodulation System+Tolterodine | 簾夢築選齋製壓夢艱構(窪襯窪築夢鹹糧衊觸鹹) = 觸齋壓齋築構鬱鑰糧構 夢鹽遞遞憲鹹襯鏇糧糧 (夢餘選窪積鑰築鬱鑰範, 4) 更多 | - | 2013-05-16 | ||
N/A | - | 醖繭鏇淵簾網衊壓獵鹽(糧蓋鏇憲廠艱鹹鏇構鑰) = 膚鹹衊餘夢衊蓋衊製願 範醖憲糧襯鑰膚顧顧製 (鏇遞衊壓齋膚鑰觸餘襯 ) 更多 | - | 2008-08-01 | |||
醖繭鏇淵簾網衊壓獵鹽(糧蓋鏇憲廠艱鹹鏇構鑰) = 廠膚鹹餘鏇壓繭齋製壓 範醖憲糧襯鑰膚顧顧製 (鏇遞衊壓齋膚鑰觸餘襯 ) |
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