预约演示
更新于：2025-05-23
Acotiamide Hydrochloride Hydrate
盐酸阿考替胺
更新于：2025-05-23
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 日本 (2013-03-25), |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C21H37ClN4O8S |
InChIKeyNPTDXIXCQCFGKC-UHFFFAOYSA-N |
CAS号773092-05-0 |
关联
49
项与 盐酸阿考替胺 相关的临床试验TCTR20250319014
Comparative Efficacy and Safety of Acotiamide versus Domperidone in the Treatment of Functional Dyspepsia: A Randomized Controlled Trial
JPRN-UMIN000053000
A Randomized, Placebo-Controlled, Double-Blind, Crossover Comparative Study of the Effect of Acotiamide on Gastrointestinal Symptoms in Patients with Myasthenia Gravis - ACTMG
CTR20241669
盐酸阿考替胺片在中国健康人群中单次给药的人体生物等效性临床试验
100 项与 盐酸阿考替胺 相关的临床结果
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100 项与 盐酸阿考替胺 相关的转化医学
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100 项与 盐酸阿考替胺 相关的专利（医药）
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169
项与 盐酸阿考替胺 相关的文献（医药）2025-03-31International Neurourology Journal
Effect of Acotiamide on Detrusor Underactivity Induced Through Bilateral Pelvic Nerve Crush Injury in Rats
Article
作者: Fujimura, Tetsuya ; Takaoka, Ei-Ichiro ; Yoshimura, Naoki ; Kamei, Jun ; Sugihara, Toru ; Nagahama, Kenji ; Ando, Satoshi
Purpose: To investigate the effectiveness of acotiamide on lower urinary tract dysfunction by using a rat model of neurogenic underactive bladder induced through pelvic nerve crush (PNC) injury.Methods: Bilateral PNC injuries were performed on 8-week-old female Sprague-Dawley rats (PNC group); the sham surgery group was used as control (control group). Two weeks after surgery, awake cystometrography (CMG) was performed, and acotiamide (10 or 100 mg/kg) was subcutaneously administered to the control and PNC groups. Subsequently, CMG parameter values obtained before and after treatment were compared.Results: In baseline CMG, compared to control group, PNC group revealed statistically significant elevations in the intercontraction intervals (ICIs), number of nonvoiding contractions, baseline pressure, threshold pressure, bladder capacity, voided volumes, and postvoid residual. However, contraction amplitudes and voiding efficiency were significantly decreased. In the control group, compared with the baseline values, 10-mg/kg acotiamide resulted in statistically significant elevations in contraction amplitudes. Treatment with 100-mg/kg acotiamide led to statistically significant elevations in contraction amplitudes and decreases in ICI and bladder volume. In the PNC group, there were no statistically significant changes noted in CMG parameters after treatment with 10-mg/kg acotiamide (n=6). Compared with the baseline values, the administration of 100-mg/kg acotiamide significantly decreased ICI (1,025±186 seconds vs. 578±161 seconds; P=0.012), bladder capacity (1,841±323 µL vs. 871±174 µL, respectively; P=0.0059) and postvoid residual (223±46 µL vs. 44±22 µL, respectively; P=0.023), and increased contraction amplitudes (22.09±1.76 cm H2O vs. 43.84±6.87 cm H2O, respectively; P=0.012) and voiding efficiency (0.87±0.02 vs. 0.94±0.03, respectively; P=0.029).Conclusions: Acotiamide showed effectiveness in the treatment of underactive bladder, possibly through activation of bladder afferent and detrusor activities.
2025-03-01NEUROUROLOGY AND URODYNAMICS
Is It Possible to Regenerate the Underactive Detrusor? Part 1. Molecular and Stem Cell Therapies Targeting the Urinary Bladder and Neural Axis ‐ ICI‐RS 2024
Review
作者: Tarcan, Tufan ; Przydacz, Mikolaj ; Sinha, Sanjay ; Wein, Alan ; Cuenca, Esther Martinez ; Gajewski, Jerzy B. ; Lazar, Jason M. ; Kanai, Anthony J. ; Tyagi, Pradeep ; Cruz, Francisco ; Van Huele, Andries ; Weiss, Jeffrey P. ; Kheir, George Bou ; Abrams, Paul
ABSTRACT:
Introduction:
Detrusor muscle weakness is commonly noted on urodynamics in patients with refractory voiding difficulty. No approved therapies have been proven to augment the strength of a detrusor voiding contraction.
Methods:
This subject was discussed by a think‐tank at the International Consultation on Incontinence‐ Research Society (ICI‐RS) meeting held in Bristol, June 2024. The discussions of the think‐tank are being published in two parts. This first part discusses molecular and stem cell therapies targeting the urinary bladder and the neural axis.
Results:
Senescence of the urothelium and extracellular ATP acting through P2X3 receptors might be important in detrusor underactivity. Several molecules such as parasympathomimetics, acotiamide, ASP8302, neurokinin‐2 agonists have been explored but none has shown unequivocal clinical benefit. Different stem cell therapy approaches have been used, chiefly in neurogenic dysfunction, with some studies showing benefit. Molecular targets for the neural axis have included TRPV‐4, Bombesin, and serotoninergic receptors and TAC‐302 which induces neurite growth.
Conclusions:
Several options are currently being pursued in the search for an elusive molecular or stem cell option for enhancing the power of the detrusor muscle. These encompass a wide range of approaches that target each aspect of the contraction mechanism including the urothelium of bladder and urethra, myocyte, and neural pathways. While none of these have shown unequivocal clinical utility, some appear promising. Lessons from other fields of medicine might prove instructive.
Clinical Trial Registration:
Not necessary. Not a clinical trial.
2025-03-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Repurposing FDA-approved drugs to target G-quadruplexes in breast cancer
Article
作者: Moraca, Federica ; Napolitano, Fabiana ; D'Aria, Federica ; Pagano, Bruno ; Amato, Jussara ; Landolfi, Laura ; Catalanotti, Bruno ; Di Porzio, Anna ; Castellano, Giuliano ; Malfitano, Anna Maria ; Arciuolo, Valentina ; Marzano, Simona ; Randazzo, Antonio
Breast cancer, a leading cause of cancer-related mortality in women, is characterized by genomic instability and aberrant gene expression, often influenced by noncanonical nucleic acid structures such as G-quadruplexes (G4s). These structures, commonly found in the promoter regions and 5'-untranslated RNA sequences of several oncogenes, play crucial roles in regulating transcription and translation. Stabilizing these G4 structures offers a promising therapeutic strategy for targeting key oncogenic pathways. In this study, we employed a drug repurposing approach to identify FDA-approved drugs capable of binding and stabilizing G4s in breast cancer-related genes. Using ligand-based virtual screening and biophysical methods, we identified several promising compounds, such as azelastine, belotecan, and irinotecan, as effective G4 binders, with significant antiproliferative effects in breast cancer cell lines. Notably, belotecan and irinotecan exhibited a synergistic mechanism, combining G4 stabilization with their established topoisomerase I inhibition activity to enhance cytotoxicity in cancer cells. Our findings support the therapeutic potential of G4 stabilization in breast cancer, validate drug repurposing as an efficient strategy to identify G4-targeting drugs, and highlight how combining G4 stabilization with other established drug activities may improve anticancer efficacy.
13
项与 盐酸阿考替胺 相关的新闻（医药）2024-10-27
·信狐药迅
100 项与 盐酸阿考替胺 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 |
|---|---|---|---|
| 消化不良 | 日本 | 2013-03-25 |
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 |
|---|---|---|---|---|
| 餐后窘迫综合征 | 临床3期 | 比利时 | 2014-03-01 | |
| 餐后窘迫综合征 | 临床3期 | 保加利亚 | 2014-03-01 | |
| 餐后窘迫综合征 | 临床3期 | 拉脱维亚 | 2014-03-01 | |
| 餐后窘迫综合征 | 临床3期 | 立陶宛 | 2014-03-01 | |
| 餐后窘迫综合征 | 临床3期 | 罗马尼亚 | 2014-03-01 | |
| 餐后窘迫综合征 | 临床3期 | 俄罗斯 | 2014-03-01 | |
| 餐后窘迫综合征 | 临床3期 | 斯洛伐克 | 2014-03-01 | |
| 餐后窘迫综合征 | 临床3期 | 瑞典 | 2014-03-01 | |
| 餐后窘迫综合征 | 临床3期 | 乌克兰 | 2014-03-01 | |
| 餐后窘迫综合征 | 临床3期 | 英国 | 2014-03-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | (Patients with EGJOO) | 鏇鑰顧鏇選夢蓋簾遞淵(餘網獵獵艱窪鬱遞艱淵) = Acotiamide was administered to address severe symptoms in six out of 13 patients with EGJOO. Acotiamide normalized impaired receptive LES relaxation and substantially improved symptoms. 醖範獵網壓積簾製願繭 (鏇構鏇廠遞壓齋衊顧壓 ) | - | 2016-10-01 | ||
(Normal subjects) | |||||||
N/A | - | Acotiamide 10 mg thrice daily | 壓積艱襯夢窪齋繭憲鹽(鏇範膚積簾襯鏇製網構) = 範蓋齋遞獵範鹹艱願艱 齋糧窪製衊選顧襯鏇構 (鏇襯艱鹽齋簾齋憲顧夢 ) | - | 2016-10-01 | ||
Placebo | 壓積艱襯夢窪齋繭憲鹽(鏇範膚積簾襯鏇製網構) = 鏇襯窪範獵鬱觸遞醖簾 齋糧窪製衊選顧襯鏇構 (鏇襯艱鹽齋簾齋憲顧夢 ) | ||||||
N/A | 50 | 簾繭壓鏇範積範遞衊膚(淵鬱襯蓋鹽廠鑰築顧膚) = 顧簾壓築簾鏇廠鏇選艱 蓋獵艱築願網膚夢獵遞 (醖鹽積壓齋製鏇鬱衊廠 ) 更多 | 积极 | 2016-10-01 | |||
Placebo | 簾繭壓鏇範積範遞衊膚(淵鬱襯蓋鹽廠鑰築顧膚) = 鹹憲衊醖鹹餘廠遞願鬱 蓋獵艱築願網膚夢獵遞 (醖鹽積壓齋製鏇鬱衊廠 ) 更多 | ||||||
临床3期 | - | 範繭繭糧觸網鹽壓遞鹽(簾繭淵鏇觸壓遞製構憲) = 鏇願齋築鹹壓選壓醖範 鏇鹽網構願簾膚鹽鏇襯 (衊觸鹹淵齋網醖網積窪 ) | 积极 | 2012-06-01 | |||
Placebo | 範繭繭糧觸網鹽壓遞鹽(簾繭淵鏇觸壓遞製構憲) = 範醖膚艱顧願顧築鹹築 鏇鹽網構願簾膚鹽鏇襯 (衊觸鹹淵齋網醖網積窪 ) |
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