预约演示
更新于：2025-03-31
Imidafenacin
咪达那新
更新于：2025-03-31
概要
基本信息
药物类型 小分子化药 |
别名 Imidafenacin (JAN/INN)、KRP 197、KRP-197 + [9] |
作用方式 拮抗剂 |
作用机制 M1 receptor拮抗剂(毒蕈碱型乙酰胆碱受体M1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 |
非在研适应症- |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 日本 (2007-04-18), |
最高研发阶段(中国)临床1期 |
特殊审评- |
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结构/序列
分子式C20H21N3O |
InChIKeySQKXYSGRELMAAU-UHFFFAOYSA-N |
CAS号170105-16-5 |
关联
48
项与 咪达那新 相关的临床试验CTR20242398
咪达那新片在中国健康受试者中的单中心、随机、开放、双周期、双交叉空腹及餐后状态下的生物等效性试验
ChiCTR2300070562
A randomized, open-label, two-formulation, two-period, crossover study of the bioequivalence of a single oral dose of Imidafenacin tablets in fasted and fed healthy Chinese subjects
CTR20202404
咪达那新片（0.1mg）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
100 项与 咪达那新 相关的临床结果
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100 项与 咪达那新 相关的转化医学
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100 项与 咪达那新 相关的专利（医药）
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158
项与 咪达那新 相关的文献（医药）2024-06-01Journal of Inclusion Phenomena and Molecular Recognition in Chemistry
Predictors for symptom improvement in overactive bladder patients treated with imidafenacin
作者: Jang, Kyoungha ; Lee, Jeong Zoo ; Park, Yangkyu ; Seong, Wooseop ; Kim, Seunghyeon ; Shin, Dong Gil ; Kim, Hyeon Woo ; Kim, Tae Nam
The objective of this investigation is to ascertain the determinants associated with the amelioration of symptoms in female patients suffering from overactive bladder (OAB) following treatment with 0.2 mg of imidafenacin.The study included 66 female OAB patients who had been prescribed a daily dose of 0.2 mg imidafenacin for a min. of 3 mo, spanning from March 2018 to June 2020.Various clin. parameters including age, coexistence of addnl. voiding symptoms, prior history of urol. surgeries, and responses to the Overactive Bladder Symptom Score questionnaire (OABSS), both pre- and post-initiation of imidafenacin therapy, were evaluated.The mean total OABSS scores recorded before and 3 mo subsequent to imidafenacin therapy were 8.36 ± 3.65 and 5.15 ± 3.22, resp.Following the 3-mo course of imidafenacin treatment, there was a statistically significant improvement in both the total OABSS score and the severity of OAB symptoms (p < 0.001 for both).Prior to treatment initiation, Group B (n = 38) exhibited significantly higher total OABSS scores and subscores compared to Group A (n = 28) (p < 0.05).Multivariable anal. identified the OABSS subscores for items 1 and 3 prior to treatment as significant predictors for the improvement of OAB severity subsequent to imidafenacin therapy (p = 0.046, OR 3.10, 95% CI 1.019-9.440 and p < 0.001, OR 2.77, 95% CI 1.671-4.587, resp.).Consequently, imidafenacin emerges as an efficacious therapeutic agent for alleviating OAB severity in female patients, with the OABSS subscores for items 1 and 3 prior to treatment initiation holding potential utility in predicting the efficacy of imidafenacin in managing OAB.
2024-06-01Drug metabolism and pharmacokinetics
Predicting muscarinic receptor occupancy in human bladder mucosa from urinary concentrations of antimuscarinic agents for overactive bladder
Article
作者: Yamada, Shizuo ; Tanaka, Shimako ; Akashita, Gaku ; Nakatani, Eriko ; Shiho, Mizuki ; Okura, Takashi
To assess the pharmacologically relevant and selective muscarinic receptor occupancy in the bladder mucosa, we considered not only plasma drug concentrations but also urinary drug concentrations. The purpose of this study was to predict muscarinic receptor occupancy in the human bladder mucosa based on urinary concentrations in response to clinical dosages of antimuscarinic agents used to treat overactive bladder. The calculated mean plasma or serum unbound steady state concentrations were 0.06-11 nM in clinical dosages of five antimuscarinic agents. Urinary concentrations calculated from the mean plasma or serum and renal clearance ranged between 19 nM and 2 μM, which were >10-fold higher than the Ki values for bladder muscarinic receptors excluding propiverine. Bladder mucosal muscarinic receptor occupancy estimated from the urinary concentrations and the Ki values was >90 % at a steady state in clinical dosages of five antimuscarinic agents. The bladder muscarinic receptor occupancy was higher than that in the parotid gland calculated based on the mean plasma or serum unbound concentrations and Ki values for muscarinic receptors in the parotid gland. These results suggest that sufficient and selective muscarinic receptor occupancy by antimuscarinic agents, to exert pharmacological effects, in the bladder mucosa can be predicted using urinary concentrations.
2024-04-19ACS chemical biology
Characterization of Chemical Interactions between Clinical Drugs and the Oral Bacterium, Corynebacterium matruchotii, via Bioactivity-HiTES
Article
作者: Kim, Chung Sub ; Kim, Ki Hyun ; Kim, Jonghwan ; Lee, Seoung Rak ; Song, Jeongwon ; Lee, Gyu Sung ; Park, Sehwan ; Lee, Bum Soo ; Lee, Da Yeong
In the field of natural product research, the rediscovery of already-known compounds is one of the significant issues hindering new drug development. Recently, an innovative approach called bioactivity-HiTES has been developed to overcome this limitation, and several new bioactive metabolites have been successfully characterized by this method. In this study, we applied bioactivity-HiTES to Corynebacterium matruchotii, the human oral bacterium, with 3120 clinical drugs as potential elicitors. As a result, we identified two cryptic metabolites, methylindole-3-acetate (MIAA) and indole-3-acetic acid (IAA), elicited by imidafenacin, a urinary antispasmodic drug approved by the Japanese Pharmaceuticals and Medical Devices Agency (PMDA). MIAA showed weak antibacterial activity against a pulmonary disease-causing Mycobacterium conceptionense with an IC50 value of 185.7 μM. Unexpectedly, we also found that C. matruchotii metabolized fludarabine phosphate, a USFDA-approved anticancer drug, to 2-fluoroadenine which displayed moderate antibacterial activity against both Bacillus subtilis and Escherichia coli, with IC50 values of 8.9 and 20.1 μM, respectively. Finally, acelarin, a prodrug of the anticancer drug gemcitabine, was found to exhibit unreported antibacterial activity against B. subtilis with an IC50 value of 33.6 μM through the bioactivity-HiTES method as well. These results indicate that bioactivity-HiTES can also be applied to discover biotransformed products in addition to finding cryptic metabolites in microbes.
1
项与 咪达那新 相关的新闻（医药）2024-01-15
·信狐药迅
100 项与 咪达那新 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 | 日本 | 2007-04-18 | |
| 膀胱过度活动症 | 日本 | 2007-04-18 |
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 |
|---|---|---|---|---|
| 尿频 | 申请上市 | 俄罗斯 | 2022-01-30 | |
| 急迫性尿失禁 | 临床1期 | 中国 | 2015-06-17 |
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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3期 | 300 | 顧範積顧遞構鏇憲積夢(壓願積衊選構膚壓鬱鬱) = 鏇壓窪鹽繭顧齋壓艱簾 範鏇夢艱蓋窪艱觸膚糧 (範膚壓襯襯襯鹹構襯鏇, 2.2) 更多 | 非劣 | 2019-06-01 | |||
顧範積顧遞構鏇憲積夢(壓願積衊選構膚壓鬱鬱) = 構鹽製艱糧積願憲膚繭 範鏇夢艱蓋窪艱觸膚糧 (範膚壓襯襯襯鹹構襯鏇, 1.8) 更多 | |||||||
临床3期 | 300 | (Uritos®) | 積壓鹽獵繭顧選餘簾獵(糧簾積顧膚憲製鹹鬱憲) = 淵觸範簾願鏇鏇餘獵鹹 鹽膚觸壓襯築鑰齋壓鑰 (廠淵網觸餘製廠夢憲構, 3.5) 更多 | - | 2019-05-21 | ||
(Urotol®) | 積壓鹽獵繭顧選餘簾獵(糧簾積顧膚憲製鹹鬱憲) = 觸積觸顧鹽構衊顧蓋齋 鹽膚觸壓襯築鑰齋壓鑰 (廠淵網觸餘製廠夢憲構, 2.7) 更多 | ||||||
临床4期 | 649 | (Mirabegron + Solifenacin) | 齋鑰膚蓋醖醖繭遞壓鹹 = 蓋廠選獵鑰簾鑰簾糧積 艱遞觸簾淵壓蓋淵積齋 (獵網廠選願簾鏇製鏇鏇, 鹹淵鬱壓鏇艱範艱觸艱 ~ 築鹽顧鹽鏇遞網餘範製) 更多 | - | 2018-12-24 | ||
(Mirabegron + Propiverine) | 齋鑰膚蓋醖醖繭遞壓鹹 = 願鏇遞膚願壓鹽壓繭淵 艱遞觸簾淵壓蓋淵積齋 (獵網廠選願簾鏇製鏇鏇, 餘鑰積選艱鑰艱夢繭選 ~ 繭鏇遞顧齋鏇願衊遞鏇) 更多 | ||||||
N/A | 308 | 壓獵淵夢齋鹹遞窪遞鹽(鬱觸鏇襯簾鹹艱築選積) = 積艱窪醖糧鑰齋艱艱網 觸蓋壓膚鬱廠壓蓋窪鹹 (範顧顧鑰鬱壓網遞獵廠, 1.47 ~ 2.74) 更多 | 积极 | 2013-10-01 |
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