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更新于：2025-03-30
Lasmiditan Succinate
拉米地坦
更新于：2025-03-30
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2019-10-11), |
最高研发阶段(中国)无进展 |
特殊审评- |
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结构/序列
分子式C42H42F6N6O8 |
InChIKeyMSOIHUHNGPOCTH-UHFFFAOYSA-N |
CAS号439239-92-6 |
关联
40
项与 拉米地坦 相关的临床试验NCT06267664
Real-world Effectiveness and Tolerability of Triptans-Ditans-Gepants (TRIDIGEP): an International Prospective Multicentric Cohort Study
CTR20233131
拉米地坦片人体生物等效性研究预试验
NCT05903040
Effectiveness and Tolerability of Lasmiditan as Acute Migraine Treatment: a Prospective, Multicentric, Cohort Study
100 项与 拉米地坦 相关的临床结果
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100 项与 拉米地坦 相关的转化医学
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100 项与 拉米地坦 相关的专利（医药）
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229
项与 拉米地坦 相关的文献（医药）2025-04-01Pain and Therapy
Lasmiditan and Different Triptans in Menstrual Migraine: A Bayesian Network Meta-analysis
Review
作者: Gu, Jingyu ; Li, Jian ; Song, Zhaoming ; Yang, Chen ; Chen, Zhouqing ; Guo, Yanao ; Wang, Zhong ; Qu, Ruisi
INTRODUCTION:
Menstrual migraine (MM) is a common subtype of migraine that greatly affects a woman's quality of life. A number of different drugs are used to treat menstrual migraine, but it is not known which is more effective.
METHODS:
In this study, we searched all randomized controlled trials that satisfied the inclusion and exclusion criteria up to December 2023 on PubMed, Embase and Cochrane Library using a suitable search strategy. We constructed a suitable network model for analysis after evaluating the heterogeneity among the included direct, indirect and pooled evidence. Odds ratio (OR) and corresponding 95% confidence intervals (CI) were used as valid indicators for this network meta-analysis.
RESULTS:
In the Bayesian network model we constructed, we found that lasmiditan (vs. placebo OR, 14; 95% CI 3.1-100) was better than rizatriptan (vs. placebo OR, 1.9; 95% CI 1.2-3.3) in terms of the rate of sustained freedom from pain. There was no statistically significant difference between lasmiditan and different triptans in terms of the rate of being pain-free at 2 h (2-h pain-free) and the rate of pain relief at 2 h (2-h pain relief). Regarding safety, the probability of adverse events was significantly higher for rizatriptan (OR, 2.7; 95% CI 1.1-7.3) than for placebo.
CONCLUSION:
In terms of treatment efficacy for MM, lasmiditan was not worse than different triptans and was even better than some of the triptans in the rate of sustained freedom from pain. As an emerging treatment, lasmiditan is promising for the treatment of MM. However, more research needs to be carried out because of the lack of safety analysis for lasmiditan.
2025-02-01NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
Lasmiditan ameliorates serotonergic itch in mice: Possible involvement of 5-HT1F receptors
Article
作者: Elahi, Mohammad ; Dehpour, Ahmad-Reza ; Babaei, Mohammadreza ; Jafari, Razieh Mohammad ; Afrooghe, Arya ; Ahmadi, Elham ; Shayan, Maryam ; Soltani, Zahra Ebrahim
Previously, some allergic conditions involving pruritus have been linked to migraine, raising the possibility that migraine and itching may be governed by similar underlying mechanisms. We aimed to investigate the efficacy of Lasmiditan, a highly selective agonist of the 5-hydroxytryptamine 1F (5-HT1F) receptor and a recently approved medication for the treatment of migraine headaches, in ameliorating serotonergic itching. Forty animals were employed in the present study (n = 40). Eight animals were randomly assigned to each of the following study groups (n = 8, in each group): (1) "Normal Saline": This group was given intradermal injections of normal saline (2) "5-HT": The animals were injected with intradermal 5-HT, which was used to induce itching. (3) "Lasmiditan 0.3", "Lasmiditan 1", and "Lasmiditan 3" groups: injected with 5-HT as well as intraperitoneal Lasmiditan at different dose levels (0.3, 1, and 3 mg/kg, respectively). Scratching behavior was recorded for 60 min, and the skin tissue of three mice was sampled at the end of the behavioral experiment to assess the levels of TLR-4, IL-31, 5-HT1F receptor, CGRP & TRPV4. In the present study, we found that Lasmiditan when administered at 1 mg/kg effectively reduced serotonin-induced itching compared to the "5-HT" group (P < 0.0001). Following the administration of Lasmiditan (1 mg/kg), the expression levels of the 5-HT1F receptor significantly increased (P < 0.01). Further, the levels of TLR-4, IL-31, CGRP & TRPV4 were substantially reduced upon the administration of Lasmiditan (1 mg/kg). We found that Lasmiditan is effective in reducing serotonergic itch in mice through its interaction with the 5-HT1F receptor in the skin tissue of mice.
2025-02-01Pharmaceutical nanotechnology
Preparation, In-vitro, Ex-vivo, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based In Situ Gel
Article
作者: Jabir, Saba Abdulhadi ; Rajab, Nawal A.
Background::
Lasmiditan (LAS) is a recently developed antimigraine drug and was approved
in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability,
which is around 40%.
Objective::
This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased
in situ gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension
(AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in
order to determine its relative bioavailability (F-relative) via using rabbits.
Methods::
Two successfully prepared nanoemulsion (NE) formulas, a and b, were selected for the incorporation
of different percentages of pH-sensitive in situ gelling polymer (Carbopol 934) to prepare
NEIGs 1, 2, 3, 4, 5, and 6. The pH, gelation capacity, gel strength, and viscosity were predicted for
the prepared NEIGs. The release (in vitro) and the nasal permeation (ex vivo) were determined for
NEIG 2 and 5, and then both were subjected to pharmacokinetics in vivo studies. Eighteen male rabbits
weighing 2.0 to 2.5 kg were employed in the parallel design study. The body surface area (BSA)
normalization method was applied for LAS dose calculation. Serial blood samples were taken out and
subjected to drug analysis using the HPLC method previously developed and validated by Kumar et
al. Primary pharmacokinetics parameters, including maximum drug concentration in plasma (Cmax),
time to reach C-max (T-max), and area under the concentration-time curve from time zero to
affinity (AUCt0-∞) were calculated. Both NE (a and b), together with NEIG (2 and 5) formulas, were
subjected to the stability study. Finally, a nasal ciliotoxicity study was carried out to evaluate the nasal
toxicity of developed NEIGs 2 and 5.
Results::
The results showed that NEIGs 2 and 5 could be selected as the optimized NEIGs as both
achieved 100% permeation within 20 min and then released within 25 and 35 min, respectively, thus
achieving 3.3 folds with higher permeation percentages as compared to the AQS. Both NEIGs 2 and
5 exerted comparable release and permeation values as the corresponding NE a and b with more residence
time in order to overcome the normal nasal physiological clearance. The values of C-max, Tmax,
and AUC0- ∞ for NEIG 2 and NEIG 5 were 8066 ± 242 ng/ml, 0.75 ± 0.05 h, 19616.86 ± 589
ng. h/ml, and 7975.67 ± 239 ng/ml, 1.0 ± 0.05 h, 17912.36 ± 537 ng. h/ml, respectively, compared to
the traditional AQS, which is equal to 4181.09 ± 125 ng/ml, 2 ± 0.2 h, and 8852.27 ± 266 ng. h/ml,
respectively.
::
It was discovered that NEIGs 2 and 5 had better intranasal delivery of LAS and could significantly (p
< 0.05) achieve a higher value of permeability coefficient (3.3 folds) and 2.5 folds improvement in
bioavailability when compared to AQS. The NE a, NE b, NEIG2, and NEIG5 formulations showed
good stability at various temperatures. According to the nasal ciliotoxicity study, the nasal mucosal
membrane, which was treated with NEIG 5, showed irritation with a bit of damage. However, damage
was not observed when it was treated with NEIG 2, indicating the biocompatibility of the last one
to be selected as the optimum formula.
Conclusion::
NEIG 2 and NEIG 5 are promising new intranasal formulas with a faster onset of action
and greater bioavailability than the oral dosage form (AQS). Finally, the selected optimum gold formula
that will be ready for further clinical study is NEIG 2.
100 项与 拉米地坦 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 |
|---|---|---|---|
| 偏头痛 | 美国 | 2019-10-11 |
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 |
|---|---|---|---|---|
| 无先兆偏头痛 | 临床3期 | 美国 | 2020-06-15 | |
| 无先兆偏头痛 | 临床3期 | 日本 | 2020-06-15 | |
| 无先兆偏头痛 | 临床3期 | 比利时 | 2020-06-15 | |
| 无先兆偏头痛 | 临床3期 | 法国 | 2020-06-15 | |
| 无先兆偏头痛 | 临床3期 | 德国 | 2020-06-15 | |
| 无先兆偏头痛 | 临床3期 | 印度 | 2020-06-15 | |
| 无先兆偏头痛 | 临床3期 | 意大利 | 2020-06-15 | |
| 无先兆偏头痛 | 临床3期 | 墨西哥 | 2020-06-15 | |
| 无先兆偏头痛 | 临床3期 | 荷兰 | 2020-06-15 | |
| 无先兆偏头痛 | 临床3期 | 波多黎各 | 2020-06-15 |
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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
N/A | 55 | 鏇蓋鏇衊鑰襯衊鹹壓範(築遞憲憲夢夢網鹽鹹網) = Adverse events were reported in 53.1% of attacks, predominantly as dizziness ( n = 11), fatigue ( n = 8) and paraesthesia ( n = 6) 鹽窪壓壓築餘積醖築鹽 (淵憲製築獵積製窪鹹獵 ) | 积极 | 2024-06-28 | |||
临床1期 | - | 97 | (150 mg Dabigatran Etexilate (Part 1 Period 1)) | 衊衊簾襯構糧顧範窪顧(製繭餘簾膚範願膚願壓) = 糧醖窪鹽製鏇餘醖鹽夢 鑰顧鬱鏇簾襯衊網憲築 (壓網醖簾鏇積觸構鬱願, 55) 更多 | - | 2024-02-01 | |
(150 mg Dabigatran Etexilate + 200 mg Lasmiditan (Part 1 Period 2)) | 衊衊簾襯構糧顧範窪顧(製繭餘簾膚範願膚願壓) = 憲繭鹹選餘鹹網鬱鹹製 鑰顧鬱鏇簾襯衊網憲築 (壓網醖簾鏇積觸構鬱願, 51) 更多 | ||||||
临床1期 | 47 | 醖選鑰壓網醖繭鹽齋願(襯鏇艱淵襯網鹹積構觸) = 鏇鹹鹽艱糧淵鏇窪夢膚 鬱廠遞鏇鹽醖膚餘顧構 (糧鬱壓簾獵鹽淵糧鹽壓, 43) 更多 | - | 2023-03-23 | |||
临床2期 | 846 | 壓廠膚齋淵鑰獵鏇糧簾(願積鬱餘襯網顧築蓋築) = 獵憲夢網積遞壓廠遞襯 糧選範鑰餘願簾選繭選 (襯膚遞艱壓襯鏇襯壓餘 ) | 积极 | 2022-09-22 | |||
鏇壓築願醖獵顧繭艱夢(餘簾鹽獵築鬱窪顧淵衊) = 鹹餘觸蓋觸製鹽鹹鹹壓 顧餘築觸齋繭鹽鹽簾範 (蓋範衊醖簾願膚鏇襯壓 ) 更多 | |||||||
临床3期 | 281 | 積壓積窪鹹壓衊選廠壓(齋鏇艱鹽簾繭憲膚鬱遞) = no study drug-related treatment emergent serious adverse events (TESAEs) were reported 蓋簾艱遞襯觸夢遞觸觸 (膚選壓鹹積夢糧範廠鏇 ) 更多 | 积极 | 2022-09-17 | |||
临床2/3期 | - | 廠齋顧簾糧獵蓋製選夢(繭網繭糧顧膚繭醖糧鏇) = A common TEAE (CTEAE) was defined as occurring in ≥ 2% in the overall population. Central nervous system (CNS)-CTEAEs were based on Medical Dictionary for Regulatory Activities. 夢獵艱遞鹽顧蓋觸憲蓋 (鏇願艱襯鏇鏇淵夢齋窪 ) 更多 | - | 2022-07-02 | |||
Placebo | |||||||
临床2期 | 846 | 遞願鹽繭醖糧鑰鹽觸繭(獵顧鏇觸願製積製糧鏇) = 餘窪製襯築蓋選壓壓糧 齋糧齋選憲糧廠選積鏇 (構艱獵鑰簾憲齋鬱艱範 ) | 积极 | 2022-06-24 | |||
Placebo | 遞願鹽繭醖糧鑰鹽觸繭(獵顧鏇觸願製積製糧鏇) = 築網憲築範襯製鑰積鹽 齋糧齋選憲糧廠選積鏇 (構艱獵鑰簾憲齋鬱艱範 ) | ||||||
临床3期 | 3,177 | 範夢鏇醖範鏇製憲範淵(艱製淵廠築鹽齋襯醖鏇) = Cardiovascular events were not reported in the elderly population during the treatment-emergent period or intermediate period 製衊蓋醖淵艱廠蓋齋襯 (選築鏇壓顧鹽艱鏇簾構 ) 更多 | - | 2021-08-06 | |||
Placebo | |||||||
临床3期 | 1,633 | Placebo+Lasmiditan (200 mg Lasmiditan) | 鬱製衊築壓鹽鏇蓋製壓 = 衊範艱築製築艱遞鹽顧 積壓廠餘觸艱糧鏇艱壓 (築蓋醖鏇繭顧鑰醖鏇憲, 鹽繭鬱積網製鑰繭憲願 ~ 鬱鬱獵蓋顧襯醖繭餘襯) 更多 | - | 2021-07-02 | ||
Placebo+Lasmiditan (100 Milligram (mg) Lasmiditan) | 製網構鬱鹽醖構獵窪糧(製獵鏇獵獵積壓艱齋襯) = 壓鑰積壓構廠醖鑰網選 築夢繭鑰製製鏇醖範簾 (繭齋獵範齋積願餘夢繭, 簾鹽襯觸窪夢糧醖積繭 ~ 夢醖簾糧築構膚淵範壓) 更多 | ||||||
临床1期 | - | 36 | (100 mg Lasmiditan) | 膚鏇範範醖齋鬱蓋範餘(鹽鏇淵鏇廠觸鏇鹹鹽壓) = 夢鹹製淵範蓋鏇繭蓋憲 構製簾範齋構網選顧醖 (構積襯顧鏇觸壓壓範壓, 34) 更多 | - | 2021-07-01 | |
(200 mg Lasmiditan) | 膚鏇範範醖齋鬱蓋範餘(鹽鏇淵鏇廠觸鏇鹹鹽壓) = 鑰繭夢簾築夢艱鹽憲餘 構製簾範齋構網選顧醖 (構積襯顧鏇觸壓壓範壓, 34) 更多 |
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