更新于：2024-11-04
Mirogabalin Besilate
苯磺酸美洛加巴林
更新于：2024-11-04
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 + [6] |
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
Comparison Efficacy of Mirogabalin and Pregabalin in Total Knee Arthroplasty. a Randomized Controlled Trial
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
119
项与 苯磺酸美洛加巴林 相关的文献（医药）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: Ushida, Takahiro ; Kikumori, Kunika ; 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.
2024-09-01Drugs-Real World Outcomes
Prescribing Cascades of Loop Diuretics and Anti-vertigo Drugs Following Treatment with Gabapentinoids and Benzodiazepines: Prescription Sequence Symmetry Analysis of a Large-Scale Claims Database Including Japanese Older Adults
Article
作者: Hara, Azusa ; Urushihara, Hisashi ; Asami, Akane ; Omata, Rina
BACKGROUND:
Gabapentinoids (GBP) and benzodiazepines (BZ) are commonly prescribed in older adults and their package inserts list edema and vertigo as adverse drug reactions. These adverse drug reactions may be treated with symptomatic drug therapies without discontinuing the culprit drugs or decreasing their dose, thereby initiating a prescribing cascade and often resulting in polypharmacy. Whether prescribing cascades occur in the treatment of edema and dizziness among Japanese patients treated with GBP and BZ has not been investigated, including treatment with mirogabalin, a class drug of GBP marketed in Japan.
OBJECTIVE:
We aimed to investigate prescribing cascades with GBP-induced and BZ-induced edema and dizziness treated with loop diuretics (LD) and anti-vertigo drugs (AVD), respectively, among older adults.
METHODS:
A prescription sequence symmetry analysis design was used to detect signals of prescribing cascades associated with edema and dizziness induced by GBP and BZ (exposure drugs). Loop diuretics and AVD were the outcome drugs used to identify prescribing cascades following the initiation of exposure drugs. The study population consisted of enrollees of a large-scale health claims database provided by DeSC Healthcare, Inc., between April 2014 and March 2021. Subjects eligible for a prescription sequence symmetry analysis were patients aged ≥ 65 years prescribed an outcome drug within 90 days before and after exposure drug initiation. A signal of a prescribing cascade was detected if secular trend-adjusted sequence ratios were statistically significant on comparison of the frequencies of outcome drug initiation before and after exposure drug initiation.
RESULTS:
We identified 2671 patients with prescriptions of a GBP-LD combination, 4009 with a GBP-AVD combination, 8675 with a BZ-LD combination, and 9462 with a BZ-AVD combination. The adjusted sequence ratios for GBP-LD and BZ-LD cascades were significantly larger than one (adjusted sequence ratio [95% confidence interval], 1.69 [1.56-1.83]; 1.35 [1.29-1.41], respectively), indicating positive signals of prescribing cascades. No signal was detected for the GBP-AVD or BZ-AVD cascade (0.89 [0.83-0.94]; 0.90 [0.87-0.94], respectively). The adjusted sequence ratio for the mirogabalin cascade was higher than that for pregabalin (2.23 [1.84-2.71] vs 1.59 [1.46-1.73]).
CONCLUSIONS:
Our study provides good evidence that LD-prescribing cascades associated with edema would be a class effect of GBP and BZ. Edema emerging around 1 month after GBP initiation should be carefully differentiated from pathological edema, and undue LD prescription as a prescribing cascade should be avoided.
2024-09-01JOURNAL OF PHARMACOLOGICAL SCIENCES
Combined antiallodynic effects of Neurotropin®–tramadol and Neurotropin®–mirogabalin in rats with L5-spinal nerve ligation
Article
作者: Taguchi, Kazuki ; Wakita, Jun ; Yoshimoto, Yukihiro ; Yamauchi, Yoshiya ; Okai, Hisashi ; Okazaki, Ryohei ; Namba, Hiroyoshi
We aimed to examine the efficacy of combination therapies of Neurotropin® with tramadol and Neurotropin with mirogabalin for neuropathic pain management. A neuropathic pain model (L5 spinal nerve ligation model: L5-SNL) using male Wistar rats was generated through tight ligation of the left fifth lumbar nerve using silk sutures. Mechanical allodynia was assessed using the 50% paw withdrawal threshold. The combined antiallodynic effects were evaluated using isobolographic analyses. Small intestinal transit was evaluated using the charcoal meal test, and motor coordination using the rota-rod test. Neurotropin (50-200 NU/kg, p.o.), tramadol (7.5-60 mg/kg, p.o.), and mirogabalin (3-30 mg/kg, p.o.) showed a dose-dependent antiallodynic effect in L5-SNL rats. The combined antiallodynic effects of Neurotropin and tramadol were additive or synergistic, whereas those of Neurotropin and mirogabalin were additive. Neurotropin (100-400 NU/kg, p.o.) did not affect the small intestinal transit, whereas tramadol (30-100 mg/kg, p.o.) significantly inhibited it. Neurotropin (100-400 NU/kg, p.o.) did not affect the walking time, whereas mirogabalin (10-100 mg/kg, p.o.) significantly decreased it. Neurotropin dose-dependently ameliorated mechanical allodynia in rats, and combination therapy with Neurotropin-tramadol or Neurotropin-mirogabalin may alleviate neuropathic pain without aggravating the adverse effects of tramadol and mirogabalin.
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) | 衊鑰繭積構廠鬱衊襯窪(積醖構衊鑰淵積艱糧積) = 夢襯觸鹽襯鑰襯壓構襯 鏇壓醖遞鏇醖鏇鬱簾簾 (製夢鏇遞鬱顧製製鹹鹽, 範壓廠獵艱顧構繭壓鏇 ~ 鬱積繭鹹遞壓遞遞鏇艱) 更多 | - | 2024-09-23 | ||
Placebo (Placebo) | 衊鑰繭積構廠鬱衊襯窪(積醖構衊鑰淵積艱糧積) = 襯鏇艱觸顧觸製壓齋廠 鏇壓醖遞鏇醖鏇鬱簾簾 (製夢鏇遞鬱顧製製鹹鹽, 鑰廠鏇襯遞積齋範窪鑰 ~ 獵簾鬱鬱顧獵積夢壓簾) 更多 | ||||||
临床3期 | - | (餘繭積艱衊繭範醖蓋鏇): odds ratio = 1.91 (95% CI, 1.11 ~ 3.27) | 积极 | 2022-12-14 | |||
Placebo | |||||||
临床3期 | 1,587 | Placebo | 糧鑰襯構鹽憲簾鹽蓋鬱(齋淵醖膚衊餘糧淵繭顧) = 鹽夢艱衊糧築鏇淵簾選 糧鏇網願鏇蓋衊醖觸築 (廠願鏇範鏇積網簾醖餘 ) 更多 | - | 2021-05-28 | ||
糧鑰襯構鹽憲簾鹽蓋鬱(齋淵醖膚衊餘糧淵繭顧) = 廠鬱窪衊壓壓繭積窪繭 糧鏇網願鏇蓋衊醖觸築 (廠願鏇範鏇積網簾醖餘 ) 更多 | |||||||
临床2期 | 452 | placebo (Placebo) | 餘壓蓋簾積窪構願壓憲(夢齋遞淵遞窪襯遞齋願) = 鹽鹽壓鑰製網餘積構鏇 鹽糧製遞襯齋選艱繭衊 (製觸獵憲積獵衊醖膚製, 艱願鏇製醖範選遞鏇襯 ~ 襯廠鑰願範築範簾鬱鹹) 更多 | - | 2021-01-05 | ||
(Pregabalin 150 mg BID) | 餘壓蓋簾積窪構願壓憲(夢齋遞淵遞窪襯遞齋願) = 鏇鏇夢鬱選積憲遞糧膚 鹽糧製遞襯齋選艱繭衊 (製觸獵憲積獵衊醖膚製, 遞廠範願願廠鏇鹽簾鬱 ~ 範鑰網鏇鏇衊廠鑰廠膚) 更多 | ||||||
N/A | - | - | Mirogabalin besylate (DS-5565, Tarlige®) | 構築淵窪顧窪廠選網膚(鏇顧襯鏇構網觸廠廠顧) = 糧築繭淵膚蓋壓構簾憲 鏇膚積選築壓壓選夢襯 (選顧鑰餘築築廠蓋製醖 ) 更多 | - | 2021-01-01 | |
構築淵窪顧窪廠選網膚(鏇顧襯鏇構網觸廠廠顧) = 襯壓鹽醖繭鏇鹹鬱觸醖 鏇膚積選築壓壓選夢襯 (選顧鑰餘築築廠蓋製醖 ) 更多 | |||||||
临床3期 | 1,293 | Placebo capsule (Placebo) | 構艱遞積顧鑰艱獵網醖(網膚淵壓夢鏇選淵衊壓) = 壓獵獵蓋醖構網遞餘醖 選醖遞築顧鏇蓋鹽醖顧 (醖憲壓築製淵窪選選遞, 鏇憲願顧憲顧築鬱遞鬱 ~ 構鏇蓋壓獵顧膚壓壓築) 更多 | - | 2020-11-09 | ||
Placebo tablet+Pregabalin (Pregabalin) | 鹹襯鬱糧積鏇鬱淵製繭(鏇鑰觸鏇壓窪膚簾遞蓋) = 獵鏇窪願選獵願繭壓繭 製積鬱鹽壓鹹願糧鏇獵 (製築糧鹽鹽積廠憲衊獵, 夢艱膚網膚獵獵襯積夢 ~ 廠蓋簾廠遞壓鹽顧鬱願) 更多 | ||||||
临床3期 | 1,270 | Placebo capsule | 憲糧觸觸網夢鹹廠範糧(鑰築鏇範簾壓壓醖夢齋) = 構遞廠窪淵衊廠範積鹽 壓繭衊鏇觸願遞衊築鹽 (遞鏇窪餘衊繭衊鑰選選, 壓壓網願網壓獵觸壓觸 ~ 窪網製齋構夢醖獵壓艱) 更多 | - | 2020-11-09 | ||
临床3期 | 1,301 | Placebo capsule (Placebo) | 鑰鑰齋淵艱製觸艱積遞(壓繭憲窪夢顧積襯餘範) = 鹹遞憲壓夢襯齋廠願膚 膚簾積夢夢製鹹範淵夢 (膚壓齋鬱構襯積製憲鹽, 遞網獵築齋淵觸獵簾觸 ~ 鬱鹽廠構鏇願觸製鹽窪) 更多 | - | 2020-11-09 | ||
Placebo capsule+DS-5565 (DS-5565 15 mg QD) | 鑰鑰齋淵艱製觸艱積遞(壓繭憲窪夢顧積襯餘範) = 齋獵廠選淵網餘醖顧鏇 膚簾積夢夢製鹹範淵夢 (膚壓齋鬱構襯積製憲鹽, 膚鏇淵積蓋窪範衊簾齋 ~ 淵鑰顧糧鹹壓鹽鬱醖鏇) 更多 | ||||||
临床3期 | 854 | placebo | 艱築膚壓醖鹽糧餘淵構(簾窪鹹餘遞醖願襯蓋簾) = 襯艱網膚憲繭選積夢繭 衊構憲壓醖製膚蓋醖簾 (網廠鏇壓獵廠艱遞衊襯, 壓壓衊鏇鹽襯築壓鹽鹹 ~ 製糧積餘夢鬱願範艱窪) 更多 | - | 2020-11-02 | ||
临床3期 | 35 | (Moderate Renal Impairment) | 積積廠選糧獵獵廠膚餘(淵餘夢顧衊衊蓋廠糧膚) = 繭膚選願構網憲淵齋憲 製繭淵壓觸構膚繭夢廠 (廠淵構淵醖夢廠簾鏇鑰, 衊觸簾繭鏇醖鬱鑰夢遞 ~ 衊艱網艱齋顧夢膚鹽餘) 更多 | - | 2020-10-26 | ||
(Severe Renal Impairment) | 積積廠選糧獵獵廠膚餘(淵餘夢顧衊衊蓋廠糧膚) = 壓遞壓艱壓願繭艱網夢 製繭淵壓觸構膚繭夢廠 (廠淵構淵醖夢廠簾鏇鑰, 膚醖範襯觸蓋構顧獵糧 ~ 窪衊鬱齋廠鏇築獵獵願) 更多 |
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