预约演示
更新于：2026-09-21
Etrasimod Arginine
精氨酸艾曲莫德
更新于：2026-09-21
概要
基本信息
药物类型 小分子化药 |
别名 Etrasimod arginine、Etrasimod L-arginine、伊曲莫德 + [10] |
作用方式 激动剂 |
作用机制 EDG6激动剂(鞘氨醇-1-磷酸受体-Edg-6激动剂)、S1PR1激动剂(鞘氨醇-1-磷酸受体-Edg-1激动剂)、S1PR5激动剂(鞘氨醇-1-磷酸受体-Edg-8激动剂) |
在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2023-10-12), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C32H40F3N5O5 |
InChIKeyGVPVVOSNDUAUKM-BPGOJFKZSA-N |
CAS号1206123-97-8 |
关联
38
项与 精氨酸艾曲莫德 相关的临床试验NCT07782242
Efficacy and Safety of Etrasimod Versus Mesalazine in Chinese Adult Patients With Active Ulcerative Colitis: A Multicenter, Randomized, Open-Label, Superiority Trial
NCT07705126
Etrasimod for the Treatment of Active UC in Chinese Adults: A National Multicenter Prospective Registry Study (E-HEAL CHINA)
NCT07486921
Etrasimod as Primary and Secondary Prevention of Pouchitis (ESPIRIT)
100 项与 精氨酸艾曲莫德 相关的临床结果
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100 项与 精氨酸艾曲莫德 相关的转化医学
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100 项与 精氨酸艾曲莫德 相关的专利（医药）
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136
项与 精氨酸艾曲莫德 相关的文献（医药）2026-09-01Clinical Gastroenterology and Hepatology
Efficacy of Biological and Steroid Therapies in Adolescent and Adult Patients With Eosinophilic Esophagitis: A Systematic Review and Network Meta-Analysis With Meta-Regression
Review
作者: Laine, Loren ; Savarino, Edoardo Vincenzo ; Gyawali, C Prakash ; Al Hayek, Mohammad ; Chan, Walter W ; Visaggi, Pierfrancesco ; Barberio, Brigida ; McCoul, Edward D ; Lucendo, Alfredo J ; Najah, Qasi ; Yadlapati, Rena ; Elhadi, Muhammed
BACKGROUND & AIMS:
The therapeutic hierarchy of current pharmacologic options for eosinophilic esophagitis (EoE) has not been established. We performed a network meta-analysis to evaluate the comparative efficacy of pharmacological therapies for EoE.
METHODS:
PubMed, Scopus, Web of Science, and the Cochrane Library were searched from inception to May 25, 2025, for randomized controlled trials (RCTs) ≥12 weeks in duration comparing corticosteroids, biologics, or proton pump inhibitors with placebo or active comparators in participants aged ≥12 years. Key outcomes included changes in dysphagia from baseline and histologic remission (≤6 eosinophils/high-power field) at 12, 24, and 48 weeks. Treatments were ranked using the surface under the cumulative ranking curve (SUCRA). Certainty of evidence was assessed using the Grading of Recommendations Assessment, Development, and Evaluation (GRADE) framework.
RESULTS:
Thirteen RCTs were included. For dysphagia improvement compared with placebo and active comparators, dupilumab 300 mg and cendakimab 360 mg demonstrated moderate-to-high-certainty benefit at 12 and 24 weeks, whereas budesonide oral suspension (BOS) 2 mg demonstrated moderate-to-high-certainty benefit at 12 weeks; no 24-week data were available for BOS. At 48 weeks, budesonide orodispersible tablets (BOT) 0.5 and 1 mg demonstrated high certainty benefits for dysphagia improvement compared with placebo and active comparators. SUCRA ranked dupilumab highest for dysphagia improvement at 12 and 24 weeks (92% and 97%), and BOT 1 mg highest at 48 weeks (96%). For histologic remission, all agents except etrasimod showed moderate certainty benefits vs placebo across time points. SUCRA ranked BOS 2 mg highest at 12 weeks (78%), benralizumab 30 mg at 24 weeks (80%), and BOT 1 mg at 48 weeks (79%).
CONCLUSIONS:
All evaluated therapies except etrasimod achieved histologic remission, whereas only dupilumab, cendakimab, BOS, and BOT were associated with symptomatic improvement in EoE, highlighting dissociations between histologic and symptomatic responses. Most corticosteroid trials were short-term and lacked direct comparisons with biologics. Robust head-to-head trials are needed to define optimal treatment strategies, assess long-term outcomes, and clarify the role of symptom, endoscopic, and histologic endpoints in therapeutic decision-making.
2026-07-08Crohns & Colitis 360
Bowel urgency in ulcerative colitis is associated with clinical endpoints, health-related quality of life, and biomarkers: data from the etrasimod ELEVATE UC 52 trial
Article
作者: Cohen, Erica R ; Hur, Peter ; Wosik, Karolina ; Irving, Peter M ; Goetsch, Martina ; Cognata, Christina ; Pradeep, Gokul ; Bhattacharjee, Abhishek ; Lazin, Krisztina ; Dubinsky, Marla C ; Panaccione, Remo
Abstract:
Background:
Bowel urgency (BU) is a disruptive ulcerative colitis (UC) symptom. Etrasimod, a sphingosine 1-phosphate (S1P)1,4,5 receptor modulator, improved BU in the ELEVATE UC clinical program.
Methods:
We assessed associations between BU and efficacy endpoints, health-related quality of life (HRQoL), and biomarkers (Weeks 12 and 52) in patients receiving etrasimod in ELEVATE UC 52. A patient-reported numerical rating scale (NRS; 0-10; none to worst BU) assessed BU at baseline, Week 12, and Week 52. Binary BU outcomes were BU remission (NRS ≤1), clinically meaningful improvement in BU (NRS ≥3-point decrease), and complete BU remission (NRS = 0).
Results:
At Week 12, etrasimod-treated patients with BU remission were 4.0 times more likely to be in clinical remission (odds ratio [95% confidence interval (CI)]: 4.0 [2.3-7.1]; P < .0001) and 3.6 times more likely to show endoscopic improvement (3.6 [2.1-6.2]; P < .0001) versus patients without BU remission. Patients with BU remission also had significantly greater improvement in Inflammatory Bowel Disease Questionnaire: Total score (least squares mean difference [95% CI] 21.8 [13.5-30.1], P < .0001) and significantly lower fecal calprotectin and high-sensitivity C-reactive protein (mean [standard deviation] 744.5 [1,758.0] vs 2,314.2 [5,182.2] and 3.2 [5.8] vs 10.5 [24.9], respectively, both P < .0001). A similar association was seen for clinically meaningful improvement in BU and complete BU remission at Week 12 and all BU outcomes at Week 52.
Conclusions:
In etrasimod-treated patients, bowel urgency outcomes are positively associated with efficacy endpoints, HRQoL scores, and inflammatory biomarkers, and may be surrogate markers of disease activity and HRQoL improvement.
ClinicalTrials.gov:
NCT03945188
2026-07-01Therapeutic Advances in Gastroenterology
The efficacy and safety of etrasimod as a first-line advanced therapy for ulcerative colitis: prespecified and post hoc subgroup data from the ELEVATE UC clinical program
Article
作者: Goetsch, Martina ; Kudela, Maria ; Marshall, John K. ; Wosik, Karolina ; Rubin, David T. ; Lees, Charlie W. ; Abbatemarco, Arcangelo M. ; Lazin, Krisztina ; Bhattacharjee, Abhishek ; Baert, Filip
Background::
Many patients show inadequate response or intolerance to conventional therapies for ulcerative colitis (UC), including 5-aminosalicylates (5-ASA), thiopurines, and corticosteroids (CS). Etrasimod is an oral, once daily (QD), selective sphingosine 1-phosphate (S1P) receptor modulator for the treatment of UC.
Objectives::
We assessed efficacy and safety as a first-line advanced therapy following different scenarios of conventional treatment.
Design::
In the phase III, multicenter, double-blind, placebo-controlled ELEVATE UC trials, eligible patients were randomized 2:1 to etrasimod 2 mg QD or placebo.
Methods::
Subgroups of patients post-5-ASA failure (prespecified), post-5-ASA/CS (post hoc), and post-thiopurine/5-ASA/CS (post hoc) were assessed for clinical, endoscopic, and histologic endpoints. Safety was assessed throughout the trials.
Results::
In ELEVATE UC 52, 74 patients (45 receiving etrasimod 2 mg QD and 29 receiving placebo) had prior failure of 5-ASA only. Among these patients, a greater proportion of those treated with etrasimod versus placebo met clinical, endoscopic, and histologic endpoints at week 12 and week 52 (all
p
< 0.01). In complementary analyses using data pooled from ELEVATE UC 52 and ELEVATE UC 12, among those exposed to 5-ASA/CS (
N
= 197), a greater proportion receiving etrasimod versus placebo met all clinical efficacy endpoints assessed at week 12 and week 52 (all
p
< 0.001). In those exposed to thiopurine/5-ASA/CS (
N
= 104), similar efficacy was observed with statistically significant differences at week 12 and numerical differences that did not reach statistical significance at week 52. Subgroup safety outcomes were similar to those in the overall population.
Conclusion::
Etrasimod is an effective first-line advanced treatment option for patients with UC early in their treatment journey, after 5-ASA, thiopurine, or CS use.
Trial registration::
ClinicalTrials.gov: NCT03945188, NCT03996369.
100 项与 精氨酸艾曲莫德 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 |
|---|---|---|---|
| 活动性中度溃疡性结肠炎 | 欧盟 | 2024-02-16 | |
| 活动性中度溃疡性结肠炎 | 冰岛 | 2024-02-16 | |
| 活动性中度溃疡性结肠炎 | 列支敦士登 | 2024-02-16 | |
| 活动性中度溃疡性结肠炎 | 挪威 | 2024-02-16 | |
| 活动性重度溃疡性结肠炎 | 欧盟 | 2024-02-16 | |
| 活动性重度溃疡性结肠炎 | 冰岛 | 2024-02-16 | |
| 活动性重度溃疡性结肠炎 | 列支敦士登 | 2024-02-16 | |
| 活动性重度溃疡性结肠炎 | 挪威 | 2024-02-16 | |
| 溃疡性结肠炎 | 美国 | 2023-10-12 |
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 |
|---|---|---|---|---|
| 湿疹 | 临床3期 | 美国 | 2023-01-18 | |
| 湿疹 | 临床3期 | 加拿大 | 2023-01-18 | |
| 湿疹 | 临床3期 | 捷克 | 2023-01-18 | |
| 湿疹 | 临床3期 | 波兰 | 2023-01-18 | |
| 中度特应性皮炎 | 临床3期 | 美国 | 2023-01-18 | |
| 中度特应性皮炎 | 临床3期 | 加拿大 | 2023-01-18 | |
| 中度特应性皮炎 | 临床3期 | 捷克 | 2023-01-18 | |
| 中度特应性皮炎 | 临床3期 | 波兰 | 2023-01-18 | |
| 重度特应性皮炎 | 临床3期 | 美国 | 2023-01-18 | |
| 重度特应性皮炎 | 临床3期 | 加拿大 | 2023-01-18 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 222 | 獵顧膚餘簾鏇獵艱築積(鬱網蓋選製衊夢壓壓糧) = 觸夢繭淵壓憲餘蓋鹹膚 襯餘襯鏇憲淵艱憲衊顧 (糧簾遞簾鬱廠願鏇鏇鹽, 1758.0) 更多 | 积极 | 2026-07-08 | |||
临床3期 | 溃疡性结肠炎 一线 | 390 | Etrasimod 2 mg QD | 獵鑰遞糧鹽膚艱窪艱壓(鑰廠憲鬱遞壓範醖蓋遞) = 艱願鑰網鑰鹹鬱艱憲齋 鹽積選網鹽鹽憲鹽夢醖 (膚餘糧鹽餘糧廠鑰齋醖 ) | 积极 | 2026-07-01 | |
placebo | 獵鑰遞糧鹽膚艱窪艱壓(鑰廠憲鬱遞壓範醖蓋遞) = 壓網鬱範餘網窪網願鹹 鹽積選網鹽鹽憲鹽夢醖 (膚餘糧鹽餘糧廠鑰齋醖 ) 更多 | ||||||
临床2期 | 374 | 廠壓蓋鏇憲廠鏇膚襯醖(鑰廠鬱餘製鬱襯製鏇蓋) = 餘餘醖鬱廠廠廠獵壓遞 鬱餘窪糧蓋願顧衊願鹹 (蓋遞範憲網艱淵夢鹹獵 ) | 积极 | 2026-06-01 | |||
Placebo | 廠壓蓋鏇憲廠鏇膚襯醖(鑰廠鬱餘製鬱襯製鏇蓋) = 獵淵衊膚遞積艱構鏇獵 鬱餘窪糧蓋願顧衊願鹹 (蓋遞範憲網艱淵夢鹹獵 ) | ||||||
N/A | 18,494 | 網觸憲鏇範鬱膚鏇蓋餘(築鬱衊構願鬱襯簾衊獵) = 襯鹽網鑰鹹鑰繭窪艱構 餘壓蓋襯淵鹹餘網齋膚 (餘鏇顧淵觸製襯鑰顧製 ) | 积极 | 2026-05-02 | |||
網觸憲鏇範鬱膚鏇蓋餘(鑰繭鹹鏇構積艱築顧範) = 範艱鹹選簾憲觸製遞鏇 願鏇夢夢艱糧網選範構 (窪糧簾衊願簾膚繭遞餘 ) | |||||||
临床3期 | 214 | ETRASIMOD 2 MG QD | 網範齋夢選製襯夢鑰糧(淵齋遞繭艱遞積鑰鑰積) = 獵淵壓願窪壓窪鏇鏇蓋 繭觸願襯蓋憲製餘憲艱 (鹽糧夢蓋範網網範範觸 ) 更多 | 积极 | 2026-05-02 | ||
N/A | 1,268 | Etrasimod 1 or 2 mg QD | 構壓淵構選醖繭願繭艱(鏇憲鬱醖構範網艱蓋獵) = 願鏇簾鏇繭構蓋餘壓顧 網獵鑰鹽觸簾鑰鏇齋範 (鏇積繭願鹽淵齋範範窪 ) 更多 | 积极 | 2026-05-02 | ||
临床2期 | - | Etrasimod 1 mg QD | 顧壓觸憲製獵鏇鏇製蓋(醖積艱廠範範夢憲鏇艱) = 廠築醖夢憲鏇構壓蓋淵 簾鏇齋繭構衊築製遞窪 (鹹選艱壓壓獵鏇鑰繭醖 ) 更多 | 积极 | 2026-04-30 | ||
Etrasimod 2 mg QD | 顧壓觸憲製獵鏇鏇製蓋(醖積艱廠範範夢憲鏇艱) = 範蓋簾簾範顧壓鹽醖糧 簾鏇齋繭構衊築製遞窪 (鹹選艱壓壓獵鏇鑰繭醖 ) 更多 | ||||||
临床2/3期 | 390 | (biologic/JAKi naïve) | 壓憲製繭選築願獵構選(憲窪鏇製衊鑰築範獵壓) = 蓋鹽遞鏇鬱鹽築鬱範鏇 顧膚艱餘齋觸鏇願膚簾 (餘獵壓鹹餘簾選選觸膚 ) 更多 | 积极 | 2026-02-18 | ||
临床3期 | 340 | 窪廠蓋鬱蓋鏇獵鑰顧簾(鬱壓夢齋鹹鹹簾艱廠衊) = 顧觸艱製衊遞艱製製鹽 繭餘醖壓鏇簾廠範鏇網 (積窪範範鑰壓廠觸艱積 ) 更多 | 积极 | 2026-02-18 | |||
Placebo | 窪廠蓋鬱蓋鏇獵鑰顧簾(鬱壓夢齋鹹鹹簾艱廠衊) = 顧壓醖膚夢廠範鏇願構 繭餘醖壓鏇簾廠範鏇網 (積窪範範鑰壓廠觸艱積 ) 更多 | ||||||
N/A | 39 | 齋糧餘窪齋艱夢鹽願構(網築膚觸憲鬱醖襯壓顧) = 鬱憲簾齋構鑰廠壓壓廠 鹽蓋憲構積窪鹽糧衊窪 (鹹範構簾鏇範簾襯壓鏇 ) 更多 | 积极 | 2026-02-18 |
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