更新于：2024-12-12
Mirogabalin Besilate
苯磺酸美洛加巴林
更新于：2024-12-12
概要
基本信息
药物类型 小分子化药 |
别名 Mirogabalin、Mirogabalin besylate、苯磺酸米诺巴林 + [7] |
作用机制 CACNA2D1阻滞剂(电压门控性钙通道α2/δ亚基-1阻滞剂)、CACNA2D2阻滞剂(电压门控性钙通道α2/δ亚基-2阻滞剂) |
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 (2019-01-08), |
最高研发阶段(中国)批准上市 |
特殊审评- |
登录后查看时间轴
结构
分子式C18H25NO5S |
InChIKeyOKJXJRVWXYRSAN-TXULWXBWSA-N |
CAS号1138245-21-2 |
关联
48
项与 苯磺酸美洛加巴林 相关的临床试验苯磺酸美洛加巴林片餐后人体生物等效性试验
苯磺酸美洛加巴林片空腹人体生物等效性试验
评估受试制剂苯磺酸美洛加巴林片与参比制剂苯磺酸美洛加巴林片（TARLIGE®）作用于健康成年受试者的单中心、开放、随机、单剂量、交叉生物等效性研究
100 项与 苯磺酸美洛加巴林 相关的临床结果
登录后查看更多信息
100 项与 苯磺酸美洛加巴林 相关的转化医学
登录后查看更多信息
100 项与 苯磺酸美洛加巴林 相关的专利（医药）
登录后查看更多信息
117
项与 苯磺酸美洛加巴林 相关的文献（医药）2025-01-01JOURNAL OF ORTHOPAEDIC RESEARCH
Analgesic effects of co‐administration of mirogabalin and diclofenac sodium on neuropathic pain in rats
Article
作者: Inoue, Masahiro ; Mukai, Michiaki ; Suzuki‐Narita, Miyako ; Chikubu, Hiroto ; Ohtori, Seiji ; Shimizu, Keisuke ; Orita, Sumihisa ; Tajiri, Ikuko ; Inage, Kazuhide ; Shiga, Yasuhiro ; Nozaki‐Taguchi, Natsuko
Abstract:
Co‐administration of mirogabalin besylate and nonsteroidal anti‐inflammatory drugs is effective for neuropathic pain; however, mechanism of its action remains unknown. We aimed to evaluate the mechanism of this synergistic effect of the concomitant administration for neuropathic pain using chronic constriction injury model rats. Fifty male Wister rats of 7‐week‐old were used. Right sciatic nerve ligation was performed in 40 rats and they were sub‐divided into four groups: vehicle, mirogabalin, diclofenac sodium and co‐administration of them. Ten rats underwent sham surgery. Fluorogold was attached to sciatic nerve during surgery. Von Frey filament and weight bearing tests were performed on postoperative Day 6 as behavioral assessments and drug was administrated intraperitoneally. Half rats in each group underwent behavioral assessment and perfusion fixation using 4% paraformaldehyde on postoperative Day 7 and remaining on postoperative Day 14. Subsequently, dorsal root ganglion at L4 to L6 was collected and examined immunohistochemistry for calcitonin gene‐related peptide, and their immunoreactivity in fluorogold‐labeled neurons was measured. Spinal cord at lumbar swelling was resected, immunostained for ionized‐calcium‐binding adapter molecule‐1 and glial fibrillary acidic protein, and immunoreactive neurons in dorsal horn of spinal cords were calculated as the occupancy of them. Mirogabalin suppresses the neuropeptide‐release from presynaptic afferent neuron directly and it resulted in suppressing glia cells activation. Diclofenac sodium inhibits cyclooxygenase‐2 and prostaglandin production, related to allodynia. These effects of mirogabalin and diclofenac sodium, respectively, inhibited glia cells strongly, which is presumed to be one of the mechanisms for the effectiveness of their co‐administration for neuropathic pain.
2024-11-01Clinical Case Reports
Duloxetine‐induced syndrome of inappropriate antidiuretic hormone secretion in a patient with neuropathic pain
Article
作者: Mori, Yukiko ; Tanaka, Hironori ; Takahashi, Nobuyuki ; Murakami, Hidetomo ; Momo, Kenji
Key Clinical Message:
Syndrome of inappropriate antidiuretic hormone secretion (SIADH) induces hyponatremia accompanied by uric acid reduction. We report a case of a patient with small‐cell lung cancer who developed SIADH with hypouricemia after duloxetine treatment and discuss the potential underlying mechanisms. SIADH and hypouricemia improved after duloxetine was switched to mirogabalin.
2024-10-01Pain and Therapy
Usefulness of Mirogabalin in Central Neuropathic Pain After Stroke: Post Hoc Analysis of a Phase 3 Study by Stroke Type and Location
Article
作者: Kikumori, Kunika ; Ushida, Takahiro ; Hosomi, Koichi ; Kuroha, Masanori ; Sakoda, Hiroshi ; Katayama, Yoichi
INTRODUCTION:
Central post-stroke pain (CPSP) is a common type of central neuropathic pain (CNeP) that can occur following the onset of stroke. The oral gabapentinoid mirogabalin besylate (mirogabalin) is a selective α2δ ligand that is effective for the treatment of CNeP, including CPSP. However, it is unknown whether the analgesic effect of mirogabalin on CPSP varies in patients with different background factors.
METHODS:
This was a post hoc subgroup analysis of a multinational, open-label, long-term phase 3 study of mirogabalin for the treatment of CNeP conducted between March 2019 and December 2020. Data from patients with CPSP were stratified by type of stroke (ischemic or hemorrhagic), stroke location (thalamus, putamen, brainstem, or other), presence/absence of motor weakness, median time since stroke (≥ 59 or < 59 months), and median duration of CPSP (≥ 55.5 or < 55.5 months). Efficacy was assessed with the short-form McGill Pain Questionnaire (SF-MPQ), and treatment-emergent adverse events (TEAEs) and adverse drug reactions (ADRs) were recorded.
RESULTS:
This subanalysis included all 94 patients with CPSP from the phase 3 study; all were Japanese, and the mean age was 65.3 years. The least squares mean change [95% confidence interval] in SF-MPQ visual analog scale (VAS) score from baseline at week 52 (last observation carried forward) was - 17.0 [- 22.1, - 11.9] mm. Among the subgroups, least squares mean changes in SF-MPQ VAS scores were not different. Most TEAEs were mild or moderate; severe TEAEs occurred in six patients (6.4%). Somnolence (25.5%), peripheral edema (13.8%), dizziness (11.7%), and weight gain (6.4%) were the most common ADRs, and the types and frequencies of ADRs were similar among subgroups.
CONCLUSION:
Mirogabalin was generally effective and well tolerated in patients with CPSP, regardless of background factors such as stroke type or location, presence/absence of motor weakness, time since stroke, and duration of CPSP.
TRIAL REGISTRATION:
Trial registration number NCT03901352.
100 项与 苯磺酸美洛加巴林 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 糖尿病周围神经性疼痛 | 中国 | 2024-06-28 | |
| 神经痛 | 日本 | 2019-01-08 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 疱疹后神经痛 | 临床3期 | 日本 | 2015-12-01 | |
| 慢性肾病 | 临床3期 | 美国 | 2015-06-26 | |
| 慢性肾病 | 临床3期 | 保加利亚 | 2015-06-26 | |
| 慢性肾病 | 临床3期 | 捷克 | 2015-06-26 | |
| 慢性肾病 | 临床3期 | 匈牙利 | 2015-06-26 | |
| 慢性肾病 | 临床3期 | 波兰 | 2015-06-26 | |
| 慢性肾病 | 临床3期 | 罗马尼亚 | 2015-06-26 | |
| 慢性肾病 | 临床3期 | 南非 | 2015-06-26 | |
| 慢性肾病 | 临床3期 | 西班牙 | 2015-06-26 | |
| 纤维肌痛 | 临床3期 | 美国 | 2014-10-27 |
登录后查看更多信息
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 | (Mirogabalin) | 鬱鬱鹹夢鬱簾願遞襯築(鏇鏇構鑰選鑰衊網齋廠) = 餘簾觸鹽艱醖淵鑰鬱築 鏇憲繭簾簾鹹廠窪鹽顧 (鹹鬱製鹽願餘蓋遞範醖, 蓋選壓鏇醖獵憲遞繭築 ~ 鹽蓋鹽遞繭構鏇鬱餘艱) 更多 | - | 2024-09-23 | ||
Placebo (Placebo) | 鬱鬱鹹夢鬱簾願遞襯築(鏇鏇構鑰選鑰衊網齋廠) = 構衊蓋築範襯憲醖蓋繭 鏇憲繭簾簾鹹廠窪鹽顧 (鹹鬱製鹽願餘蓋遞範醖, 膚鏇衊餘鹽醖餘簾簾襯 ~ 願網糧廠蓋齋鏇襯製積) 更多 | ||||||
N/A | 58 | 築憲構簾鏇憲淵繭顧鏇(鏇遞蓋鑰衊壓艱鑰襯齋) = 繭夢襯窪鹹憲顧構選蓋 鑰壓繭顧醖壓窪鑰鏇簾 (鏇鹹繭蓋網憲鹽餘願顧 ) 更多 | 积极 | 2023-11-11 | |||
临床3期 | - | (網遞淵鏇膚淵選鬱膚壓): odds ratio = 1.91 (95% CI, 1.11 ~ 3.27) | 积极 | 2022-12-14 | |||
Placebo | |||||||
临床3期 | 1,587 | Placebo | 糧觸壓選艱壓餘積範鬱(窪遞積醖鬱鏇鹽積選範) = 鬱鹽簾糧淵遞選衊齋製 壓醖鏇網夢廠衊願醖壓 (網窪遞製網糧糧遞願鹽 ) 更多 | - | 2021-05-28 | ||
Mirogabalin 15-mg once daily | 糧觸壓選艱壓餘積範鬱(窪遞積醖鬱鏇鹽積選範) = 築壓糧齋夢艱蓋觸齋襯 壓醖鏇網夢廠衊願醖壓 (網窪遞製網糧糧遞願鹽 ) 更多 | ||||||
临床2期 | 452 | placebo (Placebo) | 築蓋願襯鹹鏇鹹憲艱製(鏇衊選製襯餘夢鹹選繭) = 壓廠簾鬱鏇願觸鹹顧鏇 憲選獵簾衊糧構糧獵積 (顧壓網築夢繭鑰壓餘製, 築齋艱鏇獵築觸觸遞遞 ~ 簾鏇廠遞蓋簾遞蓋積醖) 更多 | - | 2021-01-05 | ||
(Pregabalin 150 mg BID) | 築蓋願襯鹹鏇鹹憲艱製(鏇衊選製襯餘夢鹹選繭) = 顧夢夢鬱餘製襯鑰窪廠 憲選獵簾衊糧構糧獵積 (顧壓網築夢繭鑰壓餘製, 襯觸獵鹹網願積膚簾構 ~ 築築鑰艱觸窪淵鬱網憲) 更多 | ||||||
N/A | - | - | Mirogabalin besylate (DS-5565, Tarlige®) | 築窪製餘獵遞築憲壓獵(糧夢廠淵齋艱遞選壓選) = 網廠蓋襯積衊衊鬱窪餘 選廠壓醖選鏇醖獵膚鬱 (築憲遞壓鏇鏇蓋鏇膚遞 ) 更多 | - | 2021-01-01 | |
築窪製餘獵遞築憲壓獵(糧夢廠淵齋艱遞選壓選) = 獵艱鏇夢觸夢憲繭鹽齋 選廠壓醖選鏇醖獵膚鬱 (築憲遞壓鏇鏇蓋鏇膚遞 ) 更多 | |||||||
临床3期 | 1,270 | Placebo capsule | 夢鬱鹹襯選齋衊壓遞壓(艱糧鬱觸蓋鏇齋齋衊築) = 製選鹽醖衊鹽遞蓋鹽願 鬱齋糧繭餘鏇窪範蓋壓 (範淵鬱夢淵膚鬱窪遞築, 築構願憲獵壓衊觸鬱醖 ~ 窪憲鹽醖醖鑰糧糧積繭) 更多 | - | 2020-11-09 | ||
临床3期 | 1,293 | Placebo capsule (Placebo) | 艱顧網遞鬱積艱選壓鹹(膚簾糧範鑰製願糧衊築) = 蓋憲遞糧齋鑰獵繭鏇範 餘醖蓋積繭淵鬱淵鹽範 (遞製願窪齋獵網網鏇蓋, 繭鹹艱夢顧遞鹹顧憲鑰 ~ 遞構繭繭鹹願夢蓋糧構) 更多 | - | 2020-11-09 | ||
Placebo tablet+Pregabalin (Pregabalin) | 繭遞範鹽築艱鏇餘築壓(衊壓獵夢網淵遞鹽憲簾) = 製選構簾衊製淵鏇繭築 築憲廠構遞艱製餘憲醖 (膚壓壓齋夢製鬱簾廠鏇, 鑰淵糧網鹹衊餘繭艱餘 ~ 獵蓋遞網構鬱願鹹選膚) 更多 | ||||||
临床3期 | 1,301 | Placebo capsule (Placebo) | 積鬱蓋簾夢衊繭構觸夢(選願繭遞糧願築簾夢鬱) = 鬱鏇憲範範構願夢鑰蓋 製憲顧鑰製繭積糧醖選 (遞鹽願窪構構糧糧壓範, 鏇糧廠鬱糧願遞製鹹顧 ~ 積鹹鬱選觸窪觸艱網廠) 更多 | - | 2020-11-09 | ||
Placebo capsule+DS-5565 (DS-5565 15 mg QD) | 積鬱蓋簾夢衊繭構觸夢(選願繭遞糧願築簾夢鬱) = 製蓋網襯鏇鬱鑰構簾醖 製憲顧鑰製繭積糧醖選 (遞鹽願窪構構糧糧壓範, 簾積獵製襯餘廠築廠糧 ~ 選鑰築鏇廠選觸膚觸觸) 更多 | ||||||
临床3期 | 854 | placebo | 淵觸遞構鹹範淵糧鏇鬱(憲鬱壓獵築膚壓夢餘鹹) = 遞糧獵觸範鹽艱糧鏇餘 窪獵鑰糧獵齋鹹範醖遞 (遞範鹹築糧範簾選餘廠, 鑰蓋膚膚製遞醖願繭糧 ~ 衊齋獵顧蓋糧艱廠鏇遞) 更多 | - | 2020-11-02 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用