塞曲西坦(Seletracetam) - 药物靶点：SV2A_在研适应症：急性反复发作_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(2S)-2-((4S)-4-(2,2-Difluoroethenyl)-2-oxopyrrolidin-1-yl)butanamide、Seletracetam (USAN/INN)

+ [4]

靶点

SV2A

作用方式

调节剂

作用机制

SV2A调节剂(突触囊泡蛋白2A调节剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

非在研机构

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C10H14F2N2O2

InChIKeyANWPENAPCIFDSZ-RQJHMYQMSA-N

CAS号357336-74-4

关联

5

项与塞曲西坦相关的临床试验

NCT00175851

/ Withdrawn临床3期

An Open-label, Multicenter, Follow-up Trial to Evaluate the Long-term Safety and Efficacy of Seletracetam Used as Adjunctive Treatment Using a Flexible Dosing Scheme of 4 to 80 mg b.i.d. in Subjects Aged 16 Years or Older Suffering From Epilepsy

This is a safety and efficacy study of add-on therapy with seletracetam in epilepsy patients who have participated in a previous seletracetam study

开始日期2008-05-01

申办/合作机构

UCB Pharma GmbH

NCT00422110

/ Withdrawn临床2/3期

A Phase IIb/III, Double-blind, Parallel-group, Placebo-controlled, Randomized Study: Evaluation of the Efficacy and Safety of Seletracetam as Adjunctive Treatment in Subjects (≥16 to 70 Years Old) With Refractory Partial Onset Seizures.

This study will evaluate the effectiveness and safety of seletracetam when it is used in addition to other anti-epileptic medications by patients with partial onset seizures. It will also help to determine the best dose to use.

开始日期2008-05-01

申办/合作机构

UCB Pharma GmbH

NCT00175864

/ Withdrawn临床3期

Open Label, Multicenter Study of the Safety and Efficacy of Oral Treatment With Immediate Release Seletracetam (Ucb 44212) at Individualized Doses up to a Maximum of 160mg/Day in Refractory Epileptic Patients.

This is a safety and efficacy study of add on therapy with seletracetam in patients experiencing refractory epilepsy.

开始日期2006-02-01

申办/合作机构

UCB Pharma GmbH

100 项与塞曲西坦相关的临床结果

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100 项与塞曲西坦相关的转化医学

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100 项与塞曲西坦相关的专利（医药）

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26

项与塞曲西坦相关的文献（医药）

2025-03-01·Epilepsy & Behavior

A multicenter Phase II randomized, placebo-controlled single-blind trial with the SV2A ligand seletracetam in photosensitive epilepsy patients

Article

作者: Genton, Pierre ; Löscher, Wolfgang ; Stockis, Armel ; Masnou, Pascal ; Abou-Khalil, Bassel W ; Hirsch, Edouard ; Kasteleijn-Nolst Trenité, Dorothee ; French, Jacqueline A

The objective of this study was to evaluate the effect of seletracetam (SEL), a potent modulator of synaptic vesicle glycoprotein 2A (SV2A), in patients with photoparoxysmal EEG response (PPR) to intermittent photic stimulation (IPS) as proof-of-principle of efficacy in patients with epilepsy. In this multicenter, single-blind Phase II study, adults with photosensitive epilepsy, with/without concomitant antiseizure medication therapy, underwent IPS under 3 eye conditions (at eye closure, eyes closed and eyes open) after a single oral dose of placebo (day - 1) or SEL (day 1; 0.5, 1, 2, 4, 10, or 20 mg). Complete suppression was a standardized photosensitivity range reduction to 0 over ≥ 1 time points for all eye conditions. Partial suppression was a ≥ 3-point reduction over ≥ 3 testing times vs the same time points on day - 1 in ≥ 1 eye condition. In addition, pharmacokinetics and safety were assessed. Of 27 evaluable patients, 9 reentered to receive a 2nd dosing 1-6 months later, providing a total of 36 individual exposures. At all doses administered - even the lowest -, several subjects reached a complete abolishment of PPR, with a rapid onset of effect. Overall, complete abolishment of PPR was obtained in 40-71 % of the patients; the effect increasing with the dose. In terms of effective doses to suppress PPR, SEL was at least 1,500 times more potent than levetiracetam and 10-20 times more potent than brivaracetam. Adverse events of SEL, including dizziness and somnolence, were mild to moderate. Pharmacokinetics of SEL demonstrated rapid absorption and a linear dose:plasma level relationship. This proof-of-principle study demonstrates that - based on our own experience - SEL is the most potent compound ever tested in the photosensitivity model.

2022-11-14·Angewandte Chemie International Edition

Nickel‐Catalyzed Defluorinative Asymmetric Cyclization of Fluoroalkyl‐Substituted 1,6‐Enynes for the Synthesis of Seletracetam

Article

作者: Wang, Kuai ; Liu, Wenfeng ; Kong, Wangqing ; Chen, Jiachang

AbstractThe introduction of fluorine‐containing groups into organic molecules can significantly affect their physical and chemical properties and has long been used as an effective strategy for drug discovery and development. Consequently, the development of catalytic asymmetric methods for the synthesis of fluorine‐containing heterocycles is highly desirable and sought after. Herein, we describe a nickel‐catalyzed defluorinative asymmetric cyclization of fluoroalkyl‐substituted 1,6‐enynes, providing an expedient access to synthetically attractive 4‐fluorovinyl‐substituted 2‐pyrrolidones in good yields with remarkable high levels of chemo‐, regio‐, and enantioselectivities (90–99 % ee,>35 examples). This protocol features readily available starting materials and excellent functional group compatibility, and exhibits complementary regioselectivity. The utility of this strategy was demonstrated in the enantioselective synthesis of the antiepileptic drug Seletracetam.

2022-01-01·Chinese Journal of Organic Chemistry

Nickel-Catalyzed Defluorinative Asymmetric Cyclization of Fluoroalkyl-Substituted 1,6-Enynes for the Synthesis of Seletracetam

作者: Lin, Quan ; Gong, Hegui

The paper introduced a nickel-catalyzed defluorinated asym. arylation cyclization reaction of fluoroalkyl substituted 1,6-ene alkyne, which can synthesize a variety of attractive 4-fluoroalkyl substituted 2-pyrrolidone with excellent chem. selectivity, regional selectivity and enantioselectivity.The process had mild reaction conditions, good functional group compatibility, obvious advantages of gram-level reaction and further transformation, and broad application prospects.

100 项与塞曲西坦相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D05817	塞曲西坦	-	DB05885

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
癫痫部分性发作	临床2期	-	UCB Pharma GmbH	2008-05-01
癫痫部分性发作	临床2期	-	UCB Pharma GmbH	2008-05-01
耐药性癫痫	临床2期	-	UCB Pharma GmbH	2006-02-01
耐药性癫痫	临床2期	-	UCB Pharma GmbH	2006-02-01
癫痫发作	临床2期	美国	UCB Pharma SA	2005-08-31
癫痫发作	临床2期	加拿大	UCB Pharma SA	2005-08-31
急性反复发作	临床前	美国	Prevep, Inc.	2025-02-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00152451 (CTgov)	临床2期	癫痫部分性发作 \| 耐药性癫痫	31	Seletracetam (ucb 44212)	繭築構構廠夢糧顧艱築(繭鹽膚夢壓觸餘鑰鏇獵) = 觸艱構糧積鹹壓衊範憲窪齋齋觸餘夢繭觸構範 (廠窪窪構鏇簾廠齋觸齋, 鬱積製鹹餘顧鑰壓餘窪 ~ 獵窪築廠憲夢鹹膚遞獵) 更多	-	2024-03-29
NCT00152503 (CTgov)	临床2期	癫痫发作 \| 癫痫部分性发作 \| 耐药性癫痫	59	Seletracetam (UCB44212)	襯淵簾網築範選積窪積(製淵鹹醖選衊鏇願選範) = 遞觸齋淵壓廠壓醖糧觸鹽膚鬱網餘蓋願艱築獵 (願願餘餘廠壓廠襯壓顧, 簾壓憲餘憲衊鏇壓鏇膚 ~ 積鹽簾顧積觸鹹獵蓋憲) 更多	-	2023-09-07