Fesoterodine
(Synonyms: 弗斯特罗定) 目录号 : GC39379
A muscarinic acetylcholine receptor antagonist
Cas No.:286930-02-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fesoterodine is an antagonist of muscarinic acetylcholine receptors (Kis = 15.8, 11.2, 12.6, 22.4, and 25.1 nM for human M1-5, respectively).1 In vivo, fesoterodine (0.01 mg/kg, i.v.) reduces micturition pressure and increases bladder capacity and intercontraction interval (ICI) in conscious female rats. Fesoterodine also reduces intermicturition pressure and prevents bladder overactivity in a rat model of spinal cord injury-induced overactive bladder.2
1.Ney, P., Pandita, R.K., Newgreen, D.T., et al.Pharmacological characterization of a novel investigational antimuscarinic drug, fesoterodine, in vitro and in vivoBJU Int.101(8)1036-1042(2008) 2.Biardeau, X., Przydacz, M., Aharony, S., et al.Early fesoterodine fumarate administration prevents neurogenic detrusor overactivity in a spinal cord transected rat modelPLoS One12(1)e0169694(2017)
| Cas No. | 286930-02-7 | SDF | |
| 别名 | 弗斯特罗定 | ||
| Canonical SMILES | O=C(C(C)C)OC1=CC=C(CO)C=C1[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C | ||
| 分子式 | C26H37NO3 | 分子量 | 411.58 |
| 溶解度 | Ethanol: 100 mg/mL (242.97 mM) | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4297 mL | 12.1483 mL | 24.2966 mL |
| 5 mM | 0.4859 mL | 2.4297 mL | 4.8593 mL |
| 10 mM | 0.243 mL | 1.2148 mL | 2.4297 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Fesoterodine
Drugs 2009;69(6):731-8.PMID:19405552DOI:10.2165/00003495-200969060-00006.
black triangle Fesoterodine is a muscarinic receptor antagonist that is rapidly and extensively converted to the active and more potent metabolite 5-hydroxymethyltolterodine. The drug is approved for once-daily oral administration in patients with overactive bladder syndrome (OAB). black triangle In two large, 12-week, randomized, double-blind, multicentre, phase III trials, oral Fesoterodine 4 or 8 mg once daily improved the symptoms of OAB (frequency of micturition, urgency and urge incontinence) significantly more than placebo. black triangle Furthermore, significantly more patients receiving Fesoterodine 4 or 8 mg once daily had a positive response to therapy than those receiving placebo, as determined by a treatment questionnaire. black triangle Health-related quality of life was improved to a significantly greater extent in patients with OAB who received Fesoterodine 4 or 8 mg once daily than in those who received placebo in a post hoc analysis of pooled data from the phase III trials. black triangle Fesoterodine 4 or 8 mg once daily was generally well tolerated in patients with OAB; the most frequent adverse event was dry mouth, which was generally mild to moderate in severity.
Fesoterodine: Pharmacological properties and clinical implications
Eur J Pharmacol 2018 Aug 15;833:155-157.PMID:29803689DOI:10.1016/j.ejphar.2018.05.036.
Fesoterodine (as one of three drugs: dutasteride, finasteride and Fesoterodine) was classified B (beneficial) by LUTS-FORTA 2014, indicating that it is a medicinal product with proven or obvious efficacy in the elderly, with limited side effects and/or safety concerns. A systematic literature review was undertaken in January 2018 using the PubMed and Google Scholar databases with the following individual and combined keywords: "Fesoterodine", "pharmacology", "overactive bladder" and "antimuscarinics". The aim of the review was to determine which of Fesoterodine's pharmacological properties explains its clinical benefits in general patient populations with OAB and the elderly in particular. The articles in the results were then selected by publication language (English and French only), methodology (off-topic studies, reported cases and literature reviews were excluded), relevance to the subject matter and publication date prior to 31 January 2018. A total of 205 articles was initially obtained, with 115 read and 45 selected. It appears that the association of four pharmacological properties specific to Fesoterodine can explain that this drug has a good balance between efficacy and tolerability. These properties are namely the drug's high and nearly equal affinity for both the M2 and M3 muscarinic receptors, poor penetration of the blood-brain barrier, lack of hepatic first-pass activation -fesoterodine being rapidly and extensively converted to its active metabolite, 5-hydroxymethyl tolterodine, by ubiquitous esterases-, and its extended-release formulation. Fesoterodine's pharmacological profile is optimal for the treatment of overactive bladder. It is now recognized as one of the leading first-line treatment for this indication.
Safety and Tolerability of Fesoterodine in Older Adult Patients with Overactive Bladder
Can Geriatr J 2022 Mar 2;25(1):72-78.PMID:35310472DOI:10.5770/cgj.25.530.
Background: Older patients (> 65 yr) suffering from overactive bladder (OAB) are more likely to have functional impairment and comorbidity than those without OAB. This article reviews available published studies and discusses how Fesoterodine might meet the specific needs of the older OAB patient. Methods: A comprehensive literature search was undertaken in order to evaluate Fesoterodine safety in older OAB patients. Results: Fesoterodine offers flexible dosing, allowing the clinician to balance risk and benefits according to the symptoms and preferences of the patient. Its balanced affinity for M2 and M3 muscarinic receptors may lead to its benefit on OAB symptoms. Its active metabolite is a P-gp substrate that is actively transported from the central nervous system (CNS), potentially avoiding adverse CNS effects. Fesoterodine can be used in mild or moderate hepatic or renal insufficiency and no dose adjustment is routinely required. Fesoterodine's benefit has been demonstrated in multiple clinical trials in older and medically vulnerable patients. Fesoterodine was rated as "beneficial" in the LUTS-FORTA classification due to its efficiency and tolerability in older patients. Conclusion: Here, the use of Fesoterodine in older and vulnerable patients is summarized given the need to approach pharmacotherapy for OAB differently in older adults.
Fesoterodine for the treatment of overactive bladder
Ann Pharmacother 2009 Dec;43(12):1992-2000.PMID:19920160DOI:10.1345/aph.1M308.
Objective: To review pharmacologic, pharmacokinetic, efficacy, and safety data for Fesoterodine and determine its role in the treatment of overactive bladder. Data sources: A MEDLINE search (1966-July 2009) was conducted using the key words Fesoterodine, tolterodine, muscarinic receptor antagonist, anticholinergic, overactive bladder, urge incontinence, efficacy, safety, adverse effect, pharmacology, pharmacokinetic, and receptor binding. Study selection and data extraction: All articles written in English that were identified from the data sources were evaluated, prioritizing randomized, controlled trials with human data. The references of published articles that we identified were examined for any additional studies appropriate for the review. Data synthesis: Fesoterodine, a competitive muscarinic receptor antagonist, is converted to its active metabolite, 5-hydroxymethyltolterodine, by nonspecific esterases, bypassing the cytochrome P450 system. Two randomized controlled Phase 3 trials examined the safety and efficacy of Fesoterodine in the treatment of overactive bladder. Fesoterodine was found to produce significant improvements in the treatment of overactive bladder symptoms compared with placebo. Post hoc analysis of these trials demonstrated significant improvements in health-related quality of life in patients with overactive bladder. Only one study included tolterodine, and direct comparisons between Fesoterodine and tolterodine were not conducted. The most common treatment-emergent adverse effects associated with Fesoterodine included dry mouth, constipation, urinary tract infection, and headache. Conclusions: Fesoterodine appears to be effective and generally safe for the treatment of overactive bladder. The efficacy and safety of Fesoterodine in overactive bladder treatment seem to be at least similar to that of tolterodine. Although additional comparative trials are needed, based on available data, it does not appear that Fesoterodine provides a substantial advantage over extended-release tolterodine in either efficacy or safety.
Review of Fesoterodine
Expert Opin Drug Saf 2011 Sep;10(5):805-8.PMID:21639817DOI:10.1517/14740338.2011.591377.
Introduction: Overactive bladder syndrome is a common condition that adversely affects the quality of life. It is mainly treated with a combination of bladder retraining and antimuscarinics. In a quest to reduce the side effect profile of these drugs, whilst improving their efficacy, more bladder-selective antimuscarinics were developed. One of the more recent of these antimuscarinics which has come to the market is Fesoterodine. This review examines the evidence of the safety and efficacy of this drug. Areas covered: A literature search performed identified two main multi-center trials which highlight the safety, efficacy and tolerability of Fesoterodine. These together with the pharmacologic properties of the drug are discussed at length throughout the review. An expert opinion is then formulated based on the current evidence available and on comparison with other antimuscarinics. Expert opinion: It is concluded that Fesoterodine has the added advantage of flexible dosing over some other antimuscarinics. It does, however, have a similar tolerability and side effect profile to other antimuscarinics and is, therefore, unlikely to revolutionize the treatment of the overactive bladder.