预约演示
更新于：2025-11-01
Imidafenacin
咪达那新
更新于：2025-11-01
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
44
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
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
JPRN-jRCTs031190106
Combined effect of vibegron and imidafenacin for OAB
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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139
项与 咪达那新 相关的文献（医药）2025-08-01JOURNAL OF PHARMACOLOGICAL SCIENCES
Additive effects of mirabegron on muscarinic receptor binding and on relaxation of cholinergic detrusor muscle contraction by antimuscarinics
Article
作者: Shinozuka, Kazumasa ; Maruyama-Fumoto, Kana ; Mochizuki, Masae ; Yamada, Shizuo ; Kagota, Satomi
Mirabegron is the first selective β3-adrenoceptor agonist, to be developed as an alternative to antimuscarinic therapy for patients with overactive bladder (OAB). This agent exerts off-target effects on muscarinic receptors. Its combination with solifenacin results in a higher incidence of anticholinergic effects, such as dry mouth, than solifenacin alone. The present study investigated whether the combination of mirabegron and antimuscarinics exerted additive effects on muscarinic receptors and cholinergic contraction in rat tissues. Muscarinic receptor binding activity and inhibitory effect on carbachol-induced contraction in rat tissues were evaluated by radioreceptor assays using [N-methyl-3H]scopolamine chloride (3HNMS) and the organ-bath procedure, respectively. The muscarinic receptor binding activities of solifenacin and imidafenacin in the rat brain increased when administered in combination with mirabegron. Moreover, the inhibitory effects of solifenacin and imidafenacin on carbachol-induced contractions in rat isolated bladder strips were increased by mirabegron, particularly at lower concentrations of solifenacin and imidafenacin. This is the first study to suggest that mirabegron in combination with antimuscarinics exerts additive effects for muscarinic receptor binding and inhibitory effects on cholinergic contractions in bladder strips. The results obtained also showed that these additive effects may contribute to enhanced therapeutic effects on OAB, but also cholinergic adverse effects.
2025-06-01INTERNATIONAL JOURNAL OF PHARMACEUTICS
Development of long-acting imidafenacin transdermal patches with high drug loading based on solid dispersion technology
Article
作者: Yan, Peng ; Ding, Jinsong ; Zhang, Hailong ; Lin, Jianing
Imidafenacin tablets are the first-line drug for the treatment of overactive bladder (OAB). However, the tablets need to be taken twice daily for up to 3-6 months, which highly reduces patient compliance. This study aimed to develop a long-acting imidafenacin transdermal patch (LAITP) with high drug loading using amorphous solid dispersion technology (ASD). ASD, consisting of polyvinyl pyrrolidone and imidafenacin, not only significantly increased the drug loading in the patch, but also inhibited drug crystallization. Furthermore, the formation mechanism of ASD was systematically elucidated using SEM, XRD, DSC, FT-IR, and molecular docking. The LAITP was optimized through single-factor investigations and ternary phase diagram analysis. It was confirmed by SEM and confocal Raman microscopy that ASD was a spherical microparticle with a size of 28.62 ± 8.91 µm in LAITP. Notably, under long-term and accelerated conditions of 3 months, the LAITP exhibited excellent stability to ensure the reliability of quality. Importantly, human pharmacokinetic studies demonstrated that LAITP with low skin irritation and favorable adhesion properties prolonged sustained effective plasma concentration in comparison to commercial tablets (Staybla®), reducing the frequency of administration and thereby improving patient compliance, which is expected to be a promising treatment option for patients with OAB.
2025-04-01ENVIRONMENTAL RESEARCH
The association of seasonal dietary shift with fecal metabolome and microbiota in the captive Yangtze finless porpoise (Neophocaena asiaeorientalis asiaeorientalis)
Article
作者: Wang, Chaoqun ; Nabi, Ghulam ; Tang, Bin ; Hao, Yujiang ; He, Dekui ; Wan, Xiaoling ; Ur Rahman Shah, Syed Ata ; Wang, Kexiong ; Ahmad, Maaz ; Zheng, Jinsong
The gut microbiota can act as a buffer against changes in energy and food availability and adapt plastically to fluctuations in the host's diet. However, it is unknown how changes in the gut microbiome with the seasons impact microbial metabolism and the accessibility of nutrients to hosts. The study utilized 16S rRNA and UHPLC-MS/MS approaches to examine seasonal fecal metabolome variations in the captive Yangtze finless porpoises (YFPs) to determine if these variations are linked to nutrient intake or gut microbiome composition changes. The YFPs were mostly fed a frozen and live fish diet, with different food intakes yearly. We found that gut microbial diversity remained constant, but community structure varied seasonally. Firmicutes and Cyanobacteria were higher in winter, Actinobacteria in spring and fall, and proteobacteria in summer. The genus Paeniclostridium was significantly higher in the spring season, Romboutsia and Clostridium_sensu_stricto_13 were significantly higher in the summer, while Terrisporobacter and Macrococcus were significantly higher in the fall group. The study reported that seasonal dietary variation significantly impacted the fecal metabolome by affecting the metabolism, including energy, amino acid, carbohydrate, and nucleotide metabolism of the captive YFP. Moreover, significant correlations between metabolome and microbiome were found, and these correlations may indicate that the captive YFP has adapted to cope with dietary variations and enhance energy acquisition. These findings improve our knowledge of the link between microbiota, diet, metabolites, and the physiology of the host and suggest that gut microbial populations may adapt continuously to changes in diet.
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
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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 | 願選築鏇淵網膚構餘觸(鏇衊獵襯願積齋膚構衊) = 顧鬱艱鑰觸鏇鬱積淵獵 膚選構夢製繭憲構範醖 (積選築糧艱蓋膚蓋選襯, 2.2) 更多 | 非劣 | 2019-06-01 | |||
願選築鏇淵網膚構餘觸(鏇衊獵襯願積齋膚構衊) = 餘選襯簾顧繭構襯衊積 膚選構夢製繭憲構範醖 (積選築糧艱蓋膚蓋選襯, 1.8) 更多 | |||||||
临床3期 | 300 | (Uritos®) | 範糧積鹹膚廠積襯膚顧(遞築艱窪醖壓顧膚齋餘) = 淵糧鹽蓋網醖鬱憲淵積 繭構蓋艱構糧襯顧範鑰 (顧網鑰餘齋觸壓鏇範獵, 3.5) 更多 | - | 2019-05-21 | ||
(Urotol®) | 範糧積鹹膚廠積襯膚顧(遞築艱窪醖壓顧膚齋餘) = 製繭衊遞簾網繭鑰憲艱 繭構蓋艱構糧襯顧範鑰 (顧網鑰餘齋觸壓鏇範獵, 2.7) 更多 | ||||||
临床4期 | 649 | (Mirabegron + Solifenacin) | 顧遞廠齋網窪鹽襯廠糧 = 壓膚範觸蓋膚鬱憲齋襯 窪艱壓構鬱襯積積餘鏇 (鹹繭窪艱壓襯艱繭構簾, 築獵襯衊網鏇遞夢蓋鹽 ~ 築憲顧構憲艱築構艱積) 更多 | - | 2018-12-24 | ||
(Mirabegron + Propiverine) | 顧遞廠齋網窪鹽襯廠糧 = 構鑰構遞鏇淵壓獵夢顧 窪艱壓構鬱襯積積餘鏇 (鹹繭窪艱壓襯艱繭構簾, 淵鏇築夢範製衊範鏇衊 ~ 繭蓋選壓遞構窪獵獵淵) 更多 |
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