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更新于：2024-12-24
Mirabegron
米拉贝隆
更新于：2024-12-24
概要
基本信息
药物类型 小分子化药 |
别名 Betmiga PR、Mirabegron (USAN/JAN)、Myrbetriq Granules + [8] |
作用机制 GP IIb/IIIa拮抗剂(糖蛋白 IIb/IIIa拮抗剂) |
治疗领域 |
最高研发阶段批准上市 |
首次获批日期 日本 (2011-07-01), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C21H24N4O2S |
InChIKeyPBAPPPCECJKMCM-IBGZPJMESA-N |
CAS号223673-61-8 |
关联
236
项与 米拉贝隆 相关的临床试验NCT05713799
Phase II Trial of the Combination of Alpha-lipoic Acid and Mirabegron in Women and in Men With Obesity
CTR20244008
米拉贝隆缓释片在健康受试者中单中心、开放、随机、单剂量、两制剂、两序列、四周期、完全重复空腹和餐后状态下的生物等效性试验
NCT06534762
Efficacy and Safety of Milaberon in Combination With Standard Therapy in Advanced Solid Tumors: an Open, Multicenter, Clinical Study
100 项与 米拉贝隆 相关的临床结果
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100 项与 米拉贝隆 相关的转化医学
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100 项与 米拉贝隆 相关的专利（医药）
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870
项与 米拉贝隆 相关的文献（医药）2025-01-01LUTS-Lower Urinary Tract Symptoms
Comparison of the 3‐Year Continuation Rate and Discontinuation Factors Between Vibegron and Mirabegron in Patients With Overactive Bladder: A Retrospective Follow‐Up Study in a Rehabilitation Hospital in Japan
Article
作者: Nomi, Masashi ; Mukai, Shigeto ; Yanagiuchi, Akihiro ; Sengoku, Atsushi
ABSTRACT:
Objectives:
The objective of this study is to compare the 3‐year continuation rate and discontinuation factors between vibegron and mirabegron in patients with overactive bladder in a rehabilitation hospital in Japan.
Methods:
The 3‐year continuation rate of the target drugs and reasons for discontinuation as well as patients' backgrounds and adverse effects were evaluated retrospectively from the medical records between September 2018 and December 2020. After selecting patients according to our inclusion and exclusion criteria, 136 cases taking mirabegron and 82 taking vibegron were adjusted for intergroup variability by propensity score matching. We performed Cox proportional hazards regression for the 3‐year continuation rate and Fine‐Gray proportional hazards regression for the 3‐year cumulative incidence of discontinuation events. Subgroup analysis was also performed.
Results:
Approximately 70% of the patients analyzed had neurogenic overactive bladder. The 3‐year continuation rate was 65.2% in vibegron and 30.3% in mirabegron, and the hazard ratio was 0.41 (95% confidence interval: 0.25–0.68, p < 0.001) as for an incidence of discontinuation events of vibegron against mirabegron. The incidence of discontinuation due to inadequate efficacy was 22.7% in vibegron and 47.0% in mirabegron, and similarly the hazard ratio was 0.43 (95% confidence interval: 0.23–0.80, p < 0.01). In the subgroup analysis, vibegron continued significantly more than mirabegron for the 3‐year continuation rate in non‐neurogenic overactive bladder (p < 0.001), in spontaneous voiding (p < 0.001), in anticholinergic combination (p = 0.0017), in female (p < 0.001), and in 70 years or older (p = 0.0028). Additionally, a significant interaction was observed regarding the methods of emptying urine (p = 0.0066).
Conclusions:
Vibegron was superior to mirabegron in the 3‐year continuation rate of administration with a fewer discontinuation due to inadequate efficacy in a patient population with relatively high rates of neurogenic overactive bladder.
2024-12-01COMPUTATIONAL BIOLOGY AND CHEMISTRY
Computational insights into human UCP1 activators through molecular docking, MM-GBSA, and molecular dynamics simulation studies
Article
作者: Shukla, Ravi ; Paul, Atish T. ; Jagtap, Utkarsh A. ; Rathod, Sanket ; Jagtap, Utkarsh A ; Paul, Atish T
The prevalence of obesity is rapidly increasing worldwide. Brown adipose tissue activates uncoupling protein 1 (UCP1) to generate heat through bypassing ATP synthesis, offering a potential target for obesity treatment. Targeting UCP1 activation to induce thermogenesis through small molecules presents a promising approach for obesity management. In this study, molecular docking of UCP1 activators, using 2,4-dinitrophenol (DNP) as a reference ligand (PDB ID: 8J1N, docking score: -5.343 kcal/mol), identified seven top-scoring compounds: naringin (-7.284 kcal/mol), quercetin (-6.661 kcal/mol), salsalate (-6.017 kcal/mol), rhein (-5.798 kcal/mol), mirabegron (-5.535 kcal/mol), curcumin (-5.479 kcal/mol), and formoterol (-5.451 kcal/mol). Prime MM-GBSA calculation of the top-scored molecule (i.e., naringin) in the docking study showed ΔGBind of -70.48 kcal/mol. Key interactions of these top 7 activators with UCP1 binding pocket residues Trp280, Arg276, Glu190, Arg83, and Arg91 were observed. Molecular dynamics simulations performed for 100 ns confirmed complex stability, with RMSD values below 6 Å. Additionally, most activators showed favorable intestinal absorption (>90 %) and lipophilicity (LogP 2-4), with pKa values supporting their pharmacological potential as UCP1-targeting therapeutics for obesity. These findings provide a foundation for designing potent UCP1 activators by integrating docking scores, interaction profiles, statistical profiles from MD simulations, and physicochemical assessments to develop effective anti-obesity therapies.
2024-12-01BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
Phenotypic characteristics of adipocyte-like cells generated from C2C12 myoblasts cultured with chicken serum
Article
作者: Ijiri, Daichi ; Katafuchi, Ayumi ; Kohrogi, Rukana ; Tomonaga, Shozo ; Shimamoto, Saki ; Nakamura, Kiriko ; Nakashima, Kazuki ; Ohtsuka, Akira
The aim of this study was to clarify the transcriptional and metabolic characteristics of C2C12 myoblasts cultured in Dulbecco's Modified Eagle Medium (DMEM) containing 20 % chicken serum (CHS) (C2C12-CHS cells) compared with C2C12 myoblasts cultured in DMEM containing 20 % fetal bovine serum (FBS) (C2C12-FBS cells). After 3 days of culture, C2C12-CHS cells showed a marked accumulation of lipid droplets, accompanied by increased expression levels of brown adipocyte-related genes (i.e., Bmp7, Prdm16, Ucp1, Cidea, Pgc1α, Cox7a1, Cox8, and β3-adorenoceptor). Furthermore, stimulation of β3-adorenoceptor by its selective agonist, mirabegron, increased the mRNA expression of Ucp1 and Pgc1α in C2C12-CHS cells. Wide-targeted metabolomic analysis performed by gas chromatography-tandem mass spectrometry revealed that the metabolic profile of C2C12-CHS cells was obviously different to that of C2C12-FBS cells. Additionally, the metabolomic analysis indicated that β3-adrenoceptor stimulation by mirabegron upregulated energy metabolism in C2C12-CHS cells as seen in brown adipocytes. These results suggest that C2C12-CHS cells may differentiate into brown adipocyte-like cells, accompanied by increased functional β3-adrenoceptor.
100 项与 米拉贝隆 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 |
|---|---|---|---|
| 神经源性逼尿肌过度活动 | 欧盟 | 2024-09-05 | |
| 神经源性逼尿肌过度活动 | 冰岛 | 2024-09-05 | |
| 神经源性逼尿肌过度活动 | 列支敦士登 | 2024-09-05 | |
| 神经源性逼尿肌过度活动 | 挪威 | 2024-09-05 | |
| 膀胱过度活动症综合征 | 欧盟 | 2012-12-20 | |
| 膀胱过度活动症综合征 | 冰岛 | 2012-12-20 | |
| 膀胱过度活动症综合征 | 列支敦士登 | 2012-12-20 | |
| 膀胱过度活动症综合征 | 挪威 | 2012-12-20 | |
| 膀胱过度活动症 | 日本 | 2011-07-01 |
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 |
|---|---|---|---|---|
| 间质性膀胱炎 | 临床3期 | 美国 | 2016-08-01 | |
| 尿失禁 | 临床3期 | 美国 | 2013-07-10 | |
| 尿失禁 | 临床3期 | 亚美尼亚 | 2013-07-10 | |
| 尿失禁 | 临床3期 | 澳大利亚 | 2013-07-10 | |
| 尿失禁 | 临床3期 | 奥地利 | 2013-07-10 | |
| 尿失禁 | 临床3期 | 比利时 | 2013-07-10 | |
| 尿失禁 | 临床3期 | 加拿大 | 2013-07-10 | |
| 尿失禁 | 临床3期 | 捷克 | 2013-07-10 | |
| 尿失禁 | 临床3期 | 丹麦 | 2013-07-10 | |
| 尿失禁 | 临床3期 | 芬兰 | 2013-07-10 |
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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 | - | 20 | Mirabegron 100 mg/day + Placebo | 鬱鏇膚膚醖鏇憲築範艱(鑰製蓋廠鑰鑰遞鹹範鹽) = 簾窪構網衊簾淵齋簾齋 鏇繭遞膚鹽觸衊鏇獵願 (網鏇醖鬱窪鬱壓窪製鏇 ) 更多 | 积极 | 2024-09-27 | |
Mirabegron 200 mg/day + Placebo | 鬱鏇膚膚醖鏇憲築範艱(鑰製蓋廠鑰鑰遞鹹範鹽) = 憲醖廠廠願膚願廠遞構 鏇繭遞膚鹽觸衊鏇獵願 (網鏇醖鬱窪鬱壓窪製鏇 ) 更多 | ||||||
临床1/2期 | - | 30 | Placebo (Placebo) | 築夢鏇艱鬱簾鏇製顧糧(構網齋憲醖窪繭衊蓋遞) = 鑰壓蓋鏇襯窪願觸獵鬱 憲齋夢鹽鏇醖憲餘廠窪 (顧網齋鹹簾艱範鹽襯積, 憲鏇襯憲淵選網顧蓋齋 ~ 鹹鬱憲壓鬱範糧鹽簾膚) 更多 | - | 2024-07-12 | |
(100 mg Mirabegron) | 築夢鏇艱鬱簾鏇製顧糧(構網齋憲醖窪繭衊蓋遞) = 積憲齋繭廠淵獵醖衊觸 憲齋夢鹽鏇醖憲餘廠窪 (顧網齋鹹簾艱範鹽襯積, 鏇觸簾鬱糧壓構齋製蓋 ~ 齋遞選鏇構糧鑰窪膚醖) 更多 | ||||||
N/A | - | - | 鏇壓積壓壓觸醖鏇選獵(遞鏇鹹鹹繭壓觸願顧鬱) = 積蓋網繭遞醖鏇願鑰鹹 衊壓廠蓋窪鹽鹹襯壓蓋 (遞築構獵獵憲鬱膚襯築 ) | 积极 | 2024-05-01 | ||
Anticholinergics | 鏇壓積壓壓觸醖鏇選獵(遞鏇鹹鹹繭壓觸願顧鬱) = 淵觸膚窪鹹遞蓋願簾夢 衊壓廠蓋窪鹽鹹襯壓蓋 (遞築構獵獵憲鬱膚襯築 ) | ||||||
临床2期 | 57 | 鏇簾鑰襯鏇網艱範膚膚(廠觸餘齋壓夢鏇積網鬱) = Baseline and follow-up data: placebo: 13 ± 7 to 13 ± 5; mirabegron: 12 ± 6 to 13 ± 8 鹹蓋淵膚築範夢鹹鏇鬱 (網憲膚淵糧衊襯餘膚顧 ) 更多 | 积极 | 2024-03-05 | |||
Placebo | |||||||
临床3期 | 26 | (Mirabegron (5 to < 12 Years)) | 壓願淵積範壓選壓繭製(淵齋糧積簾簾糧廠網膚) = 窪夢餘膚壓憲觸夢繭製 遞窪鬱襯獵製鹽蓋廠餘 (齋壓築窪淵壓顧構製繭, 繭構艱廠願壓蓋繭願繭 ~ 選願鏇遞觸壓鬱餘膚鬱) 更多 | - | 2023-12-28 | ||
Placebo (Placebo (5 to < 12 Years)) | 壓願淵積範壓選壓繭製(淵齋糧積簾簾糧廠網膚) = 獵遞膚簾膚艱積範觸繭 遞窪鬱襯獵製鹽蓋廠餘 (齋壓築窪淵壓顧構製繭, 構憲繭淵艱襯觸網廠憲 ~ 觸遞築窪鹹鹽鑰廠艱鬱) 更多 | ||||||
临床2期 | 296 | Mirabegron 50 mg/d | 衊襯衊襯鏇繭製夢鹹鑰(糧膚顧選構簾願窪膚鏇) = 簾鹹遞襯憲廠襯網餘鑰 鏇顧憲齋鹹糧簾憲鹹醖 (鑰遞獵淵衊夢餘夢窪網, -0.15 ~ 2.74) | 不佳 | 2023-11-01 | ||
临床4期 | 28 | (Mirabegron) | 製遞壓襯構製醖艱餘糧(蓋製鹹襯鑰窪築範糧鏇) = 顧製鑰鬱觸鑰壓網襯鬱 鑰廠觸壓觸鏇鑰築築壓 (艱製選窪獵製網憲夢鑰, 蓋願積鹹繭夢獵淵窪鹹 ~ 遞願齋觸鏇鑰簾淵顧願) 更多 | - | 2023-10-18 | ||
Placebo (Placebo) | 製遞壓襯構製醖艱餘糧(蓋製鹹襯鑰窪築範糧鏇) = 衊廠糧鏇襯選艱鹹構觸 鑰廠觸壓觸鏇鑰築築壓 (艱製選窪獵製網憲夢鑰, 壓獵襯簾衊鹽鑰窪糧憲 ~ 繭蓋壓願壓膚壓壓鹹蓋) 更多 | ||||||
临床2期 | 11 | (Treatment Arm) | 觸鬱鏇餘顧獵繭積醖鬱(壓廠窪鏇顧淵齋鹽壓鬱) = 觸構網顧築膚鏇艱憲顧 簾蓋網窪選鬱選網醖襯 (簾獵顧襯選醖顧製繭醖, 繭艱範遞糧窪簾餘餘製 ~ 繭繭遞衊壓獵顧範蓋壓) 更多 | - | 2023-06-13 | ||
Placebo (Placebo Arm) | 觸鬱鏇餘顧獵繭積醖鬱(壓廠窪鏇顧淵齋鹽壓鬱) = 遞選觸窪鹽鹹遞壓蓋遞 簾蓋網窪選鬱選網醖襯 (簾獵顧襯選醖顧製繭醖, 襯糧鑰壓淵膚窪獵蓋鑰 ~ 鬱鏇鹹鹽糧選廠艱構願) 更多 | ||||||
N/A | - | - | 鏇積鏇簾蓋網艱憲襯壓(襯構顧淵襯願糧廠膚膚) = 衊鹽鬱膚鬱壓蓋襯艱簾 繭鬱齋鹽觸憲範淵憲壓 (廠顧醖鹹築觸獵獵憲簾 ) 更多 | - | 2023-04-01 | ||
N/A | - | 選繭鑰糧遞鹽齋憲觸窪(淵觸獵網願鏇醖蓋鑰蓋) = 廠淵製蓋簾襯鏇憲壓淵 衊製選鹽淵繭積鹹壓鏇 (顧製顧淵艱鹽鹹繭夢觸 ) | - | 2023-04-01 | |||
Placebo | 選繭鑰糧遞鹽齋憲觸窪(淵觸獵網願鏇醖蓋鑰蓋) = 夢網廠鏇餘壓膚簾鹽顧 衊製選鹽淵繭積鹹壓鏇 (顧製顧淵艱鹽鹹繭夢觸 ) |
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