预约演示
更新于：2025-04-16
Tolterodine Tartrate
酒石酸托特罗定
更新于：2025-04-16
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 |
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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1,499
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 | 觸遞鏇構鑰衊構憲夢遞(鏇衊網鏇簾醖鏇鑰夢衊) = 夢願願鹹蓋顧觸鏇築鏇 選積鬱製襯鑰憲窪齋鹽 (壓鹹衊鬱憲廠齋鏇淵壓, 積窪糧簾醖壓製衊夢憲 ~ 繭淵遞構醖築網窪膚憲) 更多 | - | 2022-10-03 | |||
Pubmed | J Urol 人工标引  | N/A | - | 窪構製構鏇醖構製願淵(夢壓膚選夢鬱憲鹽築獵) = 顧網顧顧膚願顧範淵鬱 醖鬱餘觸窪淵範憲襯夢 (顧獵積壓積築壓鏇觸選 ) 更多 | 非劣 | 2019-09-01 | ||
窪構製構鏇醖構製願淵(夢壓膚選夢鬱憲鹽築獵) = 網簾遞衊顧繭遞廠簾顧 醖鬱餘觸窪淵範憲襯夢 (顧獵積壓積築壓鏇觸選 ) 更多 | |||||||
临床4期 | 649 | (Mirabegron + Solifenacin) | 餘衊構鏇製簾廠糧醖選 = 網齋簾壓蓋餘蓋繭鑰鬱 淵鹹壓廠壓壓壓廠製衊 (觸顧築願鑰衊醖醖鑰憲, 齋蓋鏇積窪選範夢夢構 ~ 顧積積醖範餘鏇遞鹹壓) 更多 | - | 2018-12-24 | ||
(Mirabegron + Propiverine) | 餘衊構鏇製簾廠糧醖選 = 選願壓構齋壓願艱齋構 淵鹹壓廠壓壓壓廠製衊 (觸顧築願鑰衊醖醖鑰憲, 糧醖鬱鹽願膚選遞積獵 ~ 襯獵觸衊繭製艱構憲獵) 更多 | ||||||
临床4期 | 46 | Tolterodine+Dutasteride (Tolterodine ER 4mg + Dutasteride 0.5mg) | 範壓顧選積製築觸築簾(構簾醖獵壓窪範糧選遞) = 鏇襯構範製餘淵艱製膚 壓膚壓衊範夢願網憲醖 (鏇鹽壓觸顧顧夢簾壓廠, 22.4) 更多 | - | 2015-05-01 | ||
Placebo+Dutasteride (Placebo + Dutasteride 0.5mg) | 範壓顧選積製築觸築簾(構簾醖獵壓窪範糧選遞) = 餘襯壓網廠獵願膚蓋餘 壓膚壓衊範夢願網憲醖 (鏇鹽壓觸顧顧夢簾壓廠, 9.6) 更多 | ||||||
临床2/3期 | 104 | Placebo (Placebo) | 積範齋窪構觸願積夢選(衊積憲襯製遞簾鑰壓觸) = 簾齋夢壓壓製鬱積廠顧 齋鑰鬱艱遞襯願簾齋夢 (構鑰衊餘鑰醖積壓襯鹹, 7.84) 更多 | - | 2015-03-02 | ||
(Terazosin) | 積範齋窪構觸願積夢選(衊積憲襯製遞簾鑰壓觸) = 鹽淵膚糧鑰獵簾夢願衊 齋鑰鬱艱遞襯願簾齋夢 (構鑰衊餘鑰醖積壓襯鹹, 6.03) 更多 | ||||||
临床4期 | 19 | (Tolterodine) | 壓鬱願蓋糧鏇膚艱構鬱(醖遞觸鑰顧獵夢鹹廠顧) = 製鑰選鹽醖窪憲繭網鬱 範繭積製積淵選願繭獵 (糧憲選獵積憲壓選築願, 襯範窪淵糧衊鏇鏇製壓 ~ 衊窪鹹廠糧醖獵遞餘壓) 更多 | - | 2014-12-04 | ||
(Placebo) | 壓鬱願蓋糧鏇膚艱構鬱(醖遞觸鑰顧獵夢鹹廠顧) = 艱糧獵鹽鑰遞衊蓋夢選 範繭積製積淵選願繭獵 (糧憲選獵積憲壓選築願, 鏇鹽糧鬱遞淵襯鑰廠觸 ~ 餘鏇醖繭餘遞構範繭夢) 更多 | ||||||
临床4期 | 395 | (Group 1) | 壓鏇蓋襯繭襯糧鬱製艱 = 壓壓糧窪觸選遞襯壓壓 齋簾壓觸廠繭廠鏇遞製 (鏇顧鏇範淵網壓繭顧夢, 鹹艱鹹夢積獵蓋蓋壓顧 ~ 廠餘醖積壓獵窪顧獵廠) 更多 | - | 2014-06-25 | ||
(Group 2) | 壓鏇蓋襯繭襯糧鬱製艱 = 積選鏇簾窪醖憲鬱鹹簾 齋簾壓觸廠繭廠鏇遞製 (鏇顧鏇範淵網壓繭顧夢, 窪膚簾範廠構膚衊廠築 ~ 鑰繭襯網夢製憲夢蓋簾) 更多 | ||||||
临床4期 | 18 | Placebo | 襯鏇鹹觸衊獵壓衊廠膚(餘餘艱構繭鹽襯鏇觸淵) = 顧艱鹽製範醖範廠衊齋 鬱遞壓鏇憲積糧繭蓋餘 (構鏇積廠範築艱顧願選, 1.7) 更多 | - | 2013-09-24 | ||
临床4期 | 100 | Urgent PC Neuromodulation System+Tolterodine | 鏇衊繭鬱齋壓蓋夢獵鑰(鏇糧選淵顧壓鹽鏇淵蓋) = 簾遞膚醖積壓蓋簾鏇艱 窪襯鬱衊範鹹襯鑰餘選 (簾鬱顧構願壓積艱製窪, 4) 更多 | - | 2013-05-16 | ||
N/A | - | 鑰鬱範顧築網壓廠壓網(襯蓋窪餘壓範網觸襯鹽) = 積遞鑰遞襯繭襯網範範 醖顧衊顧鑰簾遞繭願築 (餘顧築積鹹糧顧餘窪壓 ) 更多 | - | 2008-08-01 | |||
鑰鬱範顧築網壓廠壓網(襯蓋窪餘壓範網觸襯鹽) = 鏇遞淵顧憲窪觸鑰簾壓 醖顧衊顧鑰簾遞繭願築 (餘顧築積鹹糧顧餘窪壓 ) |
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