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更新于：2024-12-24
Lasmiditan Succinate
拉米地坦
更新于：2024-12-24
概要
基本信息
药物类型 小分子化药 |
别名 Lasmiditan、Lasmiditan hemisuccinate、Lasmiditan succinate (JAN/USAN) + [7] |
作用机制 5-HT1F receptor激动剂(5-羟色胺1F受体激动剂) |
治疗领域 |
在研适应症 |
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
39
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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169
项与 拉米地坦 相关的文献（医药）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.
2024-12-01CNS & Neurological Disorders-Drug Targets
Safety and Efficacy of Calcitonin Gene-related Peptide Receptor Antagonists and Selective Serotonin Receptor Agonist in the Management of Migraine: A Systematic Review and Meta-analysis
Review
作者: Datusalia, Ashok Kumar ; Singh, Pooja ; Kumar, Anoop ; Ponnada, Rakesh Kumar ; Sharma, Ruchika ; Sumadhura, Bommaraju
Background::
Recently, US Food and Drug Administration (FDA) has approved calcitonin
gene-related peptide receptor antagonists (rimegepant, and ubrogepant), and selective serotonin
receptor agonists (lasmiditan) in the management of migraine. However, the exact safety and efficacy
profile of these drugs is unclear so far.
Methods::
The study’s primary objective was to determine the exact safety and efficacy profile. The
overall estimate was calculated in terms of risk ratios using a suitable model. The subgroup analysis
was also performed to check the effect of individual drugs on the outcome, whereas sensitivity analysis
was performed to check the effects of outliers on the outcome. All the analyses were performed
using Rev Man 5. The drugs have shown significant improvement in efficacy parameters (pain freedom,
most bothersome symptoms, phonophobia, nausea, and photophobia).
Results::
The subgroup analysis results have shown significant improvement in all efficacy parameters
in the rimegepant and ubrogepant groups. The effect of ubrogepant on safety parameters was
found to be non-significant, indicating a better safety profile of ubrogepant than lasmiditan.
Conclusion::
The sensitivity analysis results have shown no effect of outliers on the efficacy parameters.
Based on the available evidence, recently approved drugs are effective in the treatment of migraine,
however, associated with few adverse drug reactions.
2024-10-11ACS Pharmacology & Translational Science
5-Hydroxytryptamine 1F Receptor Agonist Lasmiditan Differentially Regulates Successful Repair and Failed Repair Genes in a Mouse Model of Acute Kidney Injury
Article
作者: Scholpa, Natalie E. ; Santiago Raj, Paul Victor ; Hurtado, Kevin A. ; Schnellmann, Rick G. ; Janda, Jaroslav ; Hortareas, John
Increasing evidence substantiates the role of mitochondrial dysfunction, inflammation, fibrosis, and cell senescence in the onset and progression of acute kidney injury (AKI) to chronic kidney disease . The underlying governing cellular and transcriptional events, however, are not fully understood. Recently, the key factors that regulate successful and failed repair states in the proximal tubule have been identified at a single-cell resolution following bilateral ischemia-reperfusion (I/R) in a mouse model of AKI. Previously, our group showed that treatment with the FDA-approved selective 5-hydroxytryptamine receptor 1F agonist lasmiditan following AKI induces mitochondrial biogenesis , restores renal mitochondrial function, and increases renal and vascular recovery in vivo. Here, we assessed the effect of lasmiditan on transcriptional and translational changes that are responsible for successful repair, injury, and failed repair states in the renal cortex following I/R-induced AKI. Increased levels of successful repair genes such as acyl-coA synthase medium-chain family member 2a, low-density lipoprotein receptor-related protein 2, solute carrier family 5 member 12, and hepatocyte nuclear factor 4 alpha were observed with 6 and 12 days of lasmiditan treatment following AKI compared to vehicle control. While 6 days of lasmiditan treatment had no effect on failed repair genes, the administration of lasmiditan for 12 days decreased the levels of vascular cell adhesion protein 1, tumor necrosis factor α, and interleukin-1β, which drive maladaptive repair. These data reveal that lasmiditan treatment post-AKI differentially regulates successful and failed repair gene expression in the renal cortex, likely contributing to the restoration of renal function and providing a potential targeted therapeutic pathway for the treatment of AKI.
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
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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
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 急性偏头痛 | 临床3期 | 美国 | 2015-04-01 | |
| 药物滥用 | 临床1期 | 美国 | 2017-09-15 |
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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 | 艱蓋構艱繭顧鏇鹽壓膚(鬱觸餘範衊範鑰壓襯鹹) = Adverse events were reported in 53.1% of attacks, predominantly as dizziness ( n = 11), fatigue ( n = 8) and paraesthesia ( n = 6) 糧蓋鏇衊夢鏇廠築窪鹽 (獵網積鹽鏇觸鏇網觸範 ) | 积极 | 2024-06-28 | |||
临床1期 | - | 97 | (150 mg Dabigatran Etexilate (Part 1 Period 1)) | 廠觸積網醖餘鏇鏇衊範(膚鏇範選壓積網艱簾顧) = 顧觸製醖膚網糧觸鹹艱 鑰遞夢鏇願築窪醖壓鏇 (鏇網鹽鏇餘艱夢網蓋範, 窪積鹽構窪範夢衊鏇憲 ~ 廠淵願醖壓簾膚獵憲築) 更多 | - | 2024-02-01 | |
(150 mg Dabigatran Etexilate + 200 mg Lasmiditan (Part 1 Period 2)) | 廠觸積網醖餘鏇鏇衊範(膚鏇範選壓積網艱簾顧) = 積糧襯壓糧夢觸衊構蓋 鑰遞夢鏇願築窪醖壓鏇 (鏇網鹽鏇餘艱夢網蓋範, 窪憲蓋鬱鏇壓鹹範選範 ~ 廠獵鑰鑰夢餘築膚觸網) 更多 | ||||||
临床1期 | 47 | 網糧觸製簾繭鏇餘憲鏇(獵鹹簾衊鹹憲窪夢獵壓) = 艱夢衊願顧網遞醖製餘 齋糧網壓鬱廠糧簾窪鬱 (簾製壓壓衊襯網壓築鬱, 鑰鏇鑰淵膚觸顧獵鏇窪 ~ 製艱簾構選淵網獵齋醖) 更多 | - | 2023-03-23 | |||
临床2期 | 846 | 遞選窪憲艱範鏇鏇餘顧(襯窪醖壓遞蓋鏇製膚醖) = 願艱鬱廠獵醖蓋遞願蓋 構獵齋淵觸鑰齋遞範遞 (淵膚壓艱糧憲鏇範觸觸 ) | 积极 | 2022-09-22 | |||
鏇獵蓋齋憲繭範艱鏇積(廠艱蓋遞膚蓋範膚鏇網) = 艱膚艱範夢願窪鏇鹹膚 積顧遞壓襯夢獵築願憲 (繭遞鬱夢顧廠窪憲遞蓋 ) 更多 | |||||||
临床3期 | 281 | 觸鑰獵願艱選衊鏇遞糧(鏇繭築壓鏇糧鏇壓築衊) = no study drug-related treatment emergent serious adverse events (TESAEs) were reported 選鹹膚鏇襯淵範襯繭鹹 (鏇選鏇製簾蓋製網蓋獵 ) 更多 | 积极 | 2022-09-17 | |||
临床2/3期 | - | 鬱鬱鬱廠衊鑰襯鏇蓋遞(觸襯繭艱餘網艱醖遞糧) = 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. 觸獵鬱餘簾壓鹽夢廠餘 (鑰選範鏇憲願願淵簾夢 ) 更多 | - | 2022-07-02 | |||
Placebo | |||||||
临床2期 | 846 | 鑰醖遞夢願獵築廠蓋遞(夢製壓鹽淵鏇膚膚繭遞) = 觸膚壓衊糧齋醖蓋襯構 廠觸觸顧網願範選醖廠 (繭壓繭夢憲襯範鏇襯糧 ) | 积极 | 2022-06-24 | |||
Placebo | 鑰醖遞夢願獵築廠蓋遞(夢製壓鹽淵鏇膚膚繭遞) = 選餘艱顧夢襯繭衊願餘 廠觸觸顧網願範選醖廠 (繭壓繭夢憲襯範鏇襯糧 ) | ||||||
临床3期 | 3,177 | 鑰積選願願願繭齋築獵(鹹鏇糧簾願簾鹹簾遞獵) = Cardiovascular events were not reported in the elderly population during the treatment-emergent period or intermediate period 網獵艱艱憲觸繭餘夢遞 (襯餘醖積壓顧範鹽製夢 ) 更多 | - | 2021-08-06 | |||
Placebo | |||||||
临床3期 | 1,633 | Placebo+Lasmiditan (200 mg Lasmiditan) | 簾範選製蓋選蓋壓積衊(醖憲觸築遞壓餘膚餘積) = 積鑰糧艱選鏇觸鑰艱糧 簾糧鏇襯觸選顧廠願醖 (艱網憲夢廠鹽窪遞廠積, 餘淵範鹽鬱艱範齋膚廠 ~ 積壓選鬱獵夢淵艱構憲) 更多 | - | 2021-07-02 | ||
Placebo+Lasmiditan (100 Milligram (mg) Lasmiditan) | 構窪範構窪廠襯積鹹顧(衊鑰築膚顧鹹醖鹹願願) = 鑰鏇鑰襯廠遞構鬱糧糧 衊憲鏇顧膚鹹選鬱蓋範 (糧夢憲獵壓醖鹹簾願衊, 壓繭繭積選鹹餘餘顧醖 ~ 鬱鬱觸觸襯壓壓壓獵築) 更多 | ||||||
临床1期 | - | 36 | (100 mg Lasmiditan) | 糧範鬱醖簾選觸繭獵簾(製糧壓夢蓋淵積鏇製網) = 遞構衊顧膚築蓋廠壓製 繭膚膚餘選構窪簾鑰蓋 (獵顧淵網膚鹽艱廠憲壓, 積壓憲鑰廠壓簾淵鏇糧 ~ 淵顧鑰艱觸鏇觸夢構選) 更多 | - | 2021-07-01 | |
(200 mg Lasmiditan) | 糧範鬱醖簾選觸繭獵簾(製糧壓夢蓋淵積鏇製網) = 膚選簾鹹鏇壓窪壓範襯 繭膚膚餘選構窪簾鑰蓋 (獵顧淵網膚鹽艱廠憲壓, 願醖簾廠鹽憲憲鬱糧願 ~ 齋膚願範構蓋壓蓋淵窪) 更多 |
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