(Acebilustat) - 药物靶点：LTA4H_在研适应症：淋巴水肿_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

LTA4H

作用机制

LTA4H抑制剂(白三烯A4水解酶抑制剂)

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

Celtaxsys, Inc.Celtaxsys Aus Pty Limited

Linear Clinical Research Ltd.

+ [2]

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C29H27N3O4

InChIKeyGERJIEKMNDGSCS-DQEYMECFSA-N

CAS号943764-99-6

关联

9

项与 Acebilustat 相关的临床试验

NCT05203835 / Recruiting临床2期IIT

A Pilot Placebo-Controlled Trial of Acebilustat (CTX-4430) for the Treatment of Human Upper Extremity Lymphedema

This study is designed to investigate the response of unilateral upper extremity (arm) lymphedema, during pharmacologic treatment of lymphedema with oral placebo and oral acebilustat. Participants will receive "study drug" (Acebilustat or placebo), for 9 months. For 3 of these months, the participant will receive placebo; for 6 of these months, the participant will receive active ingredient, acebilustat. The study is blinded which means that the participant will not be told which study pill they are taking.

开始日期2022-07-27

申办/合作机构

Stanford University

NCT04662086 / Completed临床2期IIT

COVID-19 Outpatient Pragmatic Platform Study (COPPS): A Pragmatic Multi-arm, Adaptive, Phase 2, Blinded, Randomized Placebo-controlled Platform Trial to Assess the Efficacy of Different Investigational Therapeutics in Reducing Time to Disease Resolution or Viral Load Cessation, as Compared to Standard Supportive Care in Outpatients With COVID-19

The overall objective of this study is to efficiently evaluate the clinical efficacy and safety of different investigational therapeutics among adults who have COVID-19 but are not yet sick enough to require hospitalization. The overall hypothesis is that through an adaptive trial design, potential effective therapies (single and combination) may be identified for this group of patients.
COVID-19 Outpatient Pragmatic Platform Study (COPPS) is a pragmatic platform protocol designed to evaluate COVID-19 treatments by assessing their ability to reduce viral shedding (Viral Domain) or improve clinical outcomes (Clinical Domain). To be included into the platform, every investigational product will collect data for both Domain primary endpoints. Individual treatments to be evaluated in the platform will be described in separate sub-protocols.

开始日期2021-04-23

申办/合作机构

Stanford University

NCT04662060 / Completed临床2期IIT

COVID-19 Outpatient Pragmatic Platform Study (COPPS): A Pragmatic Multi-arm, Adaptive, Phase 2, Blinded, Randomized Placebo-controlled Platform Trial to Assess the Efficacy of Different Investigational Therapeutics in Reducing Time to Disease Resolution or Viral Load Cessation, as Compared to Standard Supportive Care in Outpatients With COVID-19

The overall objective of this study is to efficiently evaluate the clinical efficacy and safety of different investigational therapeutics among adults who have COVID-19 but are not yet sick enough to require hospitalization. The overall hypothesis is that through an adaptive trial design, potential effective therapies (single and combination) may be identified for this group of patients.
COVID-19 Outpatient Pragmatic Platform Study (COPPS) is a pragmatic platform protocol designed to evaluate COVID-19 treatments by assessing their ability to reduce viral shedding (Viral Domain) or improve clinical outcomes (Clinical Domain). To be included into the platform, every investigational product will collect data for both Domain primary endpoints. Individual treatments to be evaluated in the platform will be described in separate sub-protocols.

开始日期2021-04-23

申办/合作机构

Stanford University

100 项与 Acebilustat 相关的临床结果

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100 项与 Acebilustat 相关的转化医学

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100 项与 Acebilustat 相关的专利（医药）

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10

项与 Acebilustat 相关的文献（医药）

2024-05-01·Current Opinion in Cardiology

Genetic causes of lymphatic disorders: recent updates on the clinical and molecular aspects of lymphatic disease

Review

作者: Rockson, Stanley G ; Bowman, Catharine

Purpose of reviewThe lymphatic system facilitates several key functions that limit significant morbidity and mortality. Despite the impact and burden of lymphatic disorders, there are many remaining disorders whose genetic substrate remains unknown. The purpose of this review is to provide an update on the genetic causes of lymphatic disorders, while reporting on newly proposed clinical classifications of lymphatic disease.Recent findingsWe reviewed several new mutations in genes that have been identified as potential causes of lymphatic disorders including: MDFIC, EPHB4, and ANGPT2. Furthermore, the traditional St. George's Classification system for primary lymphatic anomalies has been updated to reflect the use of genetic testing, both as a tool for the clinical identification of lymphatic disease and as a method through which new sub-classifications of lymphatic disorders have been established within this framework. Finally, we highlighted recent clinical studies that have explored the impact of therapies such as sirolimus, ketoprofen, and acebilustat on lymphatic disorders.SummaryDespite a growing body of evidence, current literature demonstrates a persistent gap in the number of known genes responsible for lymphatic disease entities. Recent clinical classification tools have been introduced in order to integrate traditional symptom- and time-based diagnostic approaches with modern genetic classifications, as highlighted in the updated St. George's classification system. With the introduction of this novel approach, clinicians may be better equipped to recognize established disease and, potentially, to identify novel causal mutations. Further research is needed to identify additional genetic causes of disease and to optimize current clinical tools for diagnosis and treatment.

2023-07-26·Clinical infectious diseases : an official publication of the Infectious Diseases Society of America

Evaluation of Acebilustat, a Selective Inhibitor of Leukotriene B4 Biosynthesis, for Treatment of Outpatients With Mild-Moderate Coronavirus Disease 2019: A Randomized, Double-Blind, Placebo-Controlled Phase 2 Trial.

Article

作者: Lee, Justin ; Moss, Richard B ; Lu, Di ; Desai, Manisha ; Langguth, Jamison J ; Duong, Sophie ; Parsonnet, Julie ; Pinsky, Benjamin A ; Khosla, Chaitan ; Hedlin, Haley ; Bollyky, Jenna ; Nicolls, Mark R ; Springman, Eric ; Rogers, Angela J ; Bunning, Bryan ; Bonilla, Hector F ; Levitt, Joseph E ; Zamanian, Roham T ; Elkarra, Nadia ; Heffernan, Eileen

BACKGROUNDThe vast majority of coronavirus disease 2019 (COVID-19) disease occurs in outpatients where treatment is limited to antivirals for high-risk subgroups. Acebilustat, a leukotriene B4 inhibitor, has potential to reduce inflammation and symptom duration.METHODSIn a single-center trial spanning Delta and Omicron variants, outpatients were randomized to 100 mg/d of oral acebilustat or placebo for 28 days. Patients reported daily symptoms via electronic query through day 28 with phone follow-up on day 120 and collected nasal swab samples on days 1-10. The primary outcome was sustained symptom resolution to day 28. Secondary 28-day outcomes included time to first symptom resolution, area under the curve (AUC) for longitudinal daily symptom scores, duration of viral shedding through day 10, and symptoms on day 120.RESULTSSixty participants were randomized to each study arm. At enrollment, the median duration was 4 days (interquartile range, 3-5 days), and the median number of symptoms was 9 (7-11). Most patients (90%) were vaccinated, with 73% having neutralizing antibodies. A minority of participants (44%; 35% in the acebilustat arm and 53% in placebo) had sustained symptom resolution at day 28 (hazard ratio, 0.6 [95% confidence interval, .34-1.04]; P = .07 favoring placebo). There was no difference in the mean AUC for symptom scores over 28 days (difference in mean AUC, 9.4 [95% confidence interval, -42.1 to 60.9]; P = .72). Acebilustat did not affect viral shedding or symptoms at day 120.CONCLUSIONSSustained symptoms through day 28 were common in this low-risk population. Despite this, leukotriene B4 antagonism with acebilustat did not shorten symptom duration in outpatients with COVID-19. Clinical Trials Registration. NCT04662060.

2023-04-01·Nanotoxicology

Multi-walled carbon nanotubes induce arachidonate 5-lipoxygenase expression and enhance the polarization and function of M1 macrophages in vitro.

Article

作者: Porter, Dale W. ; Kashon, Michael ; Ma, Qiang ; Lim, Chol Seung ; Veltri, Brandon

Fibrogenic carbon nanotubes (CNTs) induce the polarization of M1 and M2 macrophages in mouse lungs. Polarization of the macrophages regulates the production of proinflammatory and pro-resolving lipid mediators (LMs) to mediate acute inflammation and its resolution in a time-dependent manner. Here we examined the molecular mechanism by which multi-walled CNTs (MWCNTs, Mitsui-7) induce M1 polarization in vitro. Treatment of murine macrophages (J774A.1) with Mitsui-7 MWCNTs increased the expression of Alox5 mRNA and protein in a concentration- and time-dependent manner. The MWCNTs induced the expression of CD68 and that induction persisted for up to 3 days post-exposure. The expression and activity of inducible nitric oxide synthase, an intracellular marker of M1, were increased by MWCNTs. Consistent with M1 polarization, the MWCNTs induced the production and secretion of proinflammatory cytokines tumor necrosis factor-α and interleukin-1β, and proinflammatory LMs leukotriene B4 (LTB4) and prostaglandin E2 (PGE2). The cell-free media from MWCNT-polarized macrophages induced the migration of neutrophilic cells (differentiated from HL-60), which was blocked by Acebilustat, a specific leukotriene A4 hydrolase inhibitor, or LY239111, an LTB4 receptor antagonist, but not NS-398, a cyclooxygenase 2 inhibitor, revealing LTB4 as a major mediator of neutrophil chemotaxis from MWCNT-polarized macrophages. Knockdown of Alox5 using specific small hairpin-RNA suppressed MWCNT-induced M1 polarization, LTB4 secretion, and migration of neutrophils. Taken together, these findings demonstrate the polarization of M1 macrophages by Mitsui-7 MWCNTs in vitro and that induction of Alox5 is an important mechanism by which the MWCNTs promote proinflammatory responses by boosting M1 polarization and production of proinflammatory LMs.

100 项与 Acebilustat 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB15385

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
寻常痤疮	临床2期	新西兰	Celtaxsys, Inc.	-
寻常痤疮	临床2期	澳大利亚	Celtaxsys, Inc.	-
囊性纤维化	临床1期	法国	Celtaxsys, Inc.	2015-10-30
囊性纤维化	临床1期	美国	Celtaxsys, Inc.	2015-10-30
囊性纤维化	临床1期	加拿大	Celtaxsys, Inc.	2015-10-30
囊性纤维化	临床1期	英国	Celtaxsys, Inc.	2015-10-30
囊性纤维化	临床1期	意大利	Celtaxsys, Inc.	2015-10-30
囊性纤维化	临床1期	德国	Celtaxsys, Inc.	2015-10-30
寻常痤疮	临床1期	新西兰	Celtaxsys, Inc.	-
寻常痤疮	药物发现	澳大利亚	Celtaxsys, Inc.	-

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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


NCT04662086 \| NCT04662060 (Pubmed)	临床2期	新型冠状病毒感染	120	Acebilustat 100 mg	壓願蓋夢壓鏇夢鏇願獵(遞衊願壓衊艱淵艱窪醖) = 襯網壓廠鹹鬱膚醖齋繭範蓋糧糧鏇襯顧壓醖壓 (鏇構鏇襯襯齋獵艱願糧 )	不佳	2023-03-30
				Placebo	壓願蓋夢壓鏇夢鏇願獵(遞衊願壓衊艱淵艱窪醖) = 積觸願醖獵壓窪壓鏇鹽範蓋糧糧鏇襯顧壓醖壓 (鏇構鏇襯襯齋獵艱願糧 )
NCT04662060 (CTgov)	临床2期	新型冠状病毒感染	120	Acebilustat	選膚糧膚餘餘餘鹹繭醖(壓願淵襯窪醖鑰憲顧積) = 顧鹽憲衊獵醖夢積窪鹹鑰艱鑰餘衊醖願顧網蓋 (窪鑰醖鏇顧網鏇築膚鹹, 糧夢簾鏇衊製淵窪鹹膚 ~ 選簾製製觸壓衊鏇網膚) 更多	-	2023-06-13
NCT02443688 (CTgov)	临床2期	囊性纤维化	200	CTX-4430 (100 mg CTX-4430)	憲網選鏇遞衊窪築顧窪(選觸襯壓觸網簾膚範膚) = 簾廠齋繭夢齋積醖網觸選鏇窪憲窪鬱壓網壓鑰 (夢獵廠網窪醖齋獵鏇簾, 網廠淵蓋觸選鑰淵艱觸 ~ 遞憲醖襯積壓襯願蓋膚) 更多	-	2019-07-25
				CTX-4430 (50 mg CTX-4430)	憲網選鏇遞衊窪築顧窪(選觸襯壓觸網簾膚範膚) = 鹽遞積壓築鏇齋鑰醖構選鏇窪憲窪鬱壓網壓鑰 (夢獵廠網窪醖齋獵鏇簾, 鑰鏇憲積選簾簾糧鏇膚 ~ 夢齋鏇築壓鏇鹽遞製製) 更多
NCT04662086 (CTgov)	临床2期	新型冠状病毒感染	122	Acebilustat (Acebilustat)	壓襯遞鏇選艱醖鏇築獵(艱願選壓蓋簾獵夢範壓) = 構網窪襯簾顧築襯觸願選選衊廠觸窪鑰艱顧築 (壓願夢醖憲積網襯網襯, 糧憲艱繭選鬱鬱淵簾衊 ~ 遞淵憲餘壓淵簾鏇網廠) 更多	-	2023-05-30
				Camostat (Camostat)	壓襯遞鏇選艱醖鏇築獵(艱願選壓蓋簾獵夢範壓) = 糧繭鏇鏇鏇醖鏇淵獵築選選衊廠觸窪鑰艱顧築 (壓願夢醖憲積網襯網襯, 繭廠淵窪窪齋獵蓋鹹鹽 ~ 糧網艱鏇廠鏇廠構鹹糧) 更多