EV-077(EV-077) - 药物靶点：TBXA1R x TBXA2R x TXA2 synthase_在研适应症：白蛋白尿，2型糖尿病，糖尿病肾病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [7]

靶点

TBXA1R x TBXA2R x TXA2 synthase

作用机制

TBXA1R拮抗剂(thromboxane A1 receptor antagonists)、TBXA2R拮抗剂(血栓素A2受体拮抗剂)、TXA2 synthase抑制剂(血栓素A2合成酶抑制剂)

治疗领域

内分泌与代谢疾病泌尿生殖系统疾病

在研适应症

白蛋白尿2型糖尿病糖尿病肾病

非在研适应症

非胰岛素依赖型糖尿病2甲型流感病毒感染应激氧化+ [1]

原研机构

在研机构

非在研机构

最高研发阶段临床2/3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C22H23ClO5

InChIKeyWHUIENZXNGAHQI-GKZDNZBASA-N

CAS号1041850-31-0

关联

2

项与 EV-077 相关的临床试验

NCT04881123 / Completed临床2/3期

Randomized, Double-blind, Placebo-controlled, Parallel Groups, Multicenter Pivotal Study Assessing the Efficacy and Safety of 15 mg Twice a Day (BID) of SER150 in Well-controlled Type 2 Diabetic Patients With Diabetic Kidney Disease and Albuminuria in Treatment With an Angiotensin Converting Enzyme Inhibitor or an Angiotensin Receptor Antagonist

This study is to assess the efficacy and safety of SER150 administered for 24 weeks as a 15 mg twice a day BID dose (except on Day 168 15 mg QD) in participants with type 2 diabetes (T2D) and albuminuria in treatment with either an angiotensin converting enzyme inhibitor (ACEi) or an angiotensin receptor antagonist (ARB).

开始日期2021-08-18

申办/合作机构

Serodus ASA

NCT01551381 / Terminated临床2期

Double-blind, Controlled Study in Healthy and Type 2 Diabetic Subjects to Assess Safety, Tolerability and Pharmacokinetics of 28 Days EV-077 Treatment, and the Effects on Platelet Function, Vascular Inflammation and Oxidative Stress.

The principal objective of this study is to evaluate the safety and tolerability of repeated doses of EV-077-3201-2TBS given to diabetic subjects over a 4 week treatment period. The secondary aim of this initial Phase IIa study is to evaluate the effect of multiple oral doses of EV-077-3201-2TBS on platelet function, vascular function, vascular inflammation, vascular oxidative stress, renal function and a selection of exploratory parameters and biomarkers in type 2 diabetic subjects, as well as multiple dose pharmacokinetics in diabetic subjects.
In order to ensure the safety of the diabetic subjects, initial parts of the study will evaluate the safety and tolerability of EV-077-3201-2TBS. In Part A, the safety of different doses EV-077-3201-2TBS will be investigated in healthy subjects treated for 4 weeks. In parallel, Part B will investigate potential interactions between EV-077-3201-2TBS and ASA in healthy subjects. Part C will then investigate the safety, pharmacokinetics and pharmacodynamics of EV-077-3201-2TBS in type 2 diabetic subjects with and without concomitant ASA therapy.

开始日期2012-01-01

申办/合作机构

Evolva SA

100 项与 EV-077 相关的临床结果

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100 项与 EV-077 相关的转化医学

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100 项与 EV-077 相关的专利（医药）

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9

项与 EV-077 相关的文献（医药）

2022-10-01·Environmental Science and Pollution Research

Investigating the role of different maize (Zea mays L.) cultivars by studying morpho-physiological attributes in chromium-stressed environment

Article

作者: Hassan, Amara ; Rasheed, Rizwan ; Parveen, Abida ; Hussain, Iqbal ; Hussain, Saddam

Because of global land surface warming, heavy metal toxicity is expected to occur more often and more intensely, affecting the growth and development of the major cereal crops such as maize (Zea mays L.) in several ways, thus affecting the production component of food security. Hence, it is important to know the best cultivars of Z. mays in abiotic stress environment to fulfill the market demand of this staple food. For this purpose, we investigate the present study to find the best Z. mays cultivar to be grown in chromium (Cr)-contaminated sand (200 µM). In this experiment, we have studied 10 cultivars (Malka, Sadaf, Pearl, CZP, YY, YH, MMRI-yellow, Sahiwal, EV-20, and EV-77) of Z. mays grown in plastic pots for 4 weeks (in addition with seed germination) under Cr - (0 µM) and Cr + (200 µM) in sand medium. Based on the findings of the current experiment, we illustrated that Cr toxicity induced a significant (P < 0.05) reduction in shoot length, root length, shoot fresh weight, root fresh weight, shoot dry weight and root dry weight, chlorophyll a, chlorophyll b, total chlorophyll, and carotenoid content and induced oxidative damage to membrane-bounded organelles by increasing the malondialdehyde and hydrogen peroxide which were manifested by flavonoid and phenolic contents. Moreover, Cr uptake was also higher in the plants grown in the Cr-contaminated sand compared to the plants grown without the Cr-contaminated sand. We also noticed that Pearl, CZP, and Sahiwal cultivars are suggested to be Cr-tolerant cultivars as showed better growth and development in Cr-contaminated sand while Sadaf, MMRI, and EV-77 showed lower growth and composition in Cr-contaminated sand. The overall pattern of Z. mays cultivars grown in Cr-contaminated sand is as follows: Pearl > CZP > Sahiwal > YY > YH > EV-20 > Malka > EV-77 > MMRI-yellow > Sadaf. Conclusively, it can be identified that when grown in Cr-contaminated sand, Pearl, CZP, and Sahiwal have greater ability to grow in polluted soils. Overall, Z. mays cultivars showed better growth in Cr-stressed environment due to defense mechanism but further experiments needed to be conducted on molecular level.

2014-04-01·Journal of Thrombosis and Thrombolysis4区 · 医学

Erratum to: Pharmacodynamic effects of EV-077 in patients with diabetes mellitus and coronary artery disease on aspirin or clopidogrel monotherapy: results of an in vitro pilot investigation

4区 · 医学

Article

作者: Patel, Ronakkumar ; Rollini, Fabiana ; Darlington, Andrew ; Desai, Bhaloo ; Sakariassen, Kjell S ; Tello-Montoliu, Antonio ; Franchi, Francesco ; Muñiz-Lozano, Ana ; Bender, Norbert ; Wilson, Ryan E ; Angiolillo, Dominick J

2014-02-01·Journal of Thrombosis and Thrombolysis4区 · 医学

Pharmacodynamic effects of EV-077 in patients with diabetes mellitus and coronary artery disease on aspirin or clopidogrel monotherapy: results of an in vitro pilot investigation

4区 · 医学

Article

作者: Fabiana Rollini ; Ryan E. Wilson ; Francesco Franchi ; Andrew Darlington ; Antonio Tello-Montoliu ; Dominick J. Angiolillo ; Norbert Bender ; Ana Muñiz-Lozano ; Ronakkumar Patel ; Kjell S. Sakariassen ; Bhaloo Desai

Patients with diabetes mellitus (DM) have increased propensity to generate thromboxane A2 (TXA2) and other eicosanoids which can contribute to their heightened platelet reactivity. EV-077 is a potent thromboxane receptor antagonist and thromboxane synthase inhibitor and thus represents an attractive therapy in patients with DM. However, the effects of EV-077 on pharmacodynamic (PD) profiles in patients with DM and coronary artery disease (CAD) while on antiplatelet therapy is poorly explored and represented the aim of this in vitro pilot investigation. Patients with DM and stable CAD (n = 10) on low-dose aspirin (81 mg/day) were enrolled and then switched to clopidogrel (75 mg/day) monotherapy for 7-10 days. PD assessments were conducted while on aspirin and on clopidogrel using light transmittance aggregometry following stimuli with U-46619 [TXA2 stable analogue (7 μM)], arachidonic acid [AA (1 mM)], collagen (3 μg/mL) and adenosine diphosphate [ADP (5 μM and 20 μM)] with and without in vitro EV-077. EV-077 completely inhibited U-46619-stimulated platelet aggregation (p = 0.005 for both aspirin and clopidogrel) and also showed a significant reduction of collagen-induced aggregation (aspirin p = 0.008; clopidogrel p = 0.005). EV-077 significantly reduced AA-induced platelet aggregation in clopidogrel (p = 0.009), but not aspirin (p = 0.667) treated patients. Ultimately, EV-077 significantly reduced ADP-mediated platelet aggregation in both aspirin (ADP 5 μM p = 0.012; ADP 20 μM p = 0.032) and clopidogrel (ADP 5 μM p = 0.007; ADP 20 μM p = 0.008) treated patients. In conclusion, in DM patients with CAD on aspirin or clopidogrel monotherapy, in vitro EV-077 exerts potent platelet inhibitory effects on multiple platelet signaling pathways. These data support that EV-077 has only additive platelet inhibiting effects on top of standard antiplatelet therapies. These findings warrant further investigation in ex vivo settings.

100 项与 EV-077 相关的药物交易

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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
白蛋白尿	临床3期	新西兰	Serodus ASA	2021-08-18
白蛋白尿	临床3期	澳大利亚	Serodus ASA	2021-08-18
2型糖尿病	临床3期	澳大利亚	Serodus ASA	2021-08-18
2型糖尿病	临床3期	新西兰	Serodus ASA	2021-08-18
糖尿病肾病	临床3期	新西兰	Serodus ASA	2021-08-18
糖尿病肾病	临床3期	澳大利亚	Serodus ASA	2021-08-18
非胰岛素依赖型糖尿病2	临床前	德国	Evolva SA	2012-01-01
应激氧化	临床前	德国	Evolva SA	2012-01-01
血管炎	临床前	德国	Evolva SA	2012-01-01
甲型流感病毒感染	药物发现	瑞士	Evolva Holding SA	-