Delving into the Latest Updates on EV-077 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [7]

Target

TBXA1R x TBXA2R x TXA2 synthase

Mechanism

TBXA1R antagonists(thromboxane A1 receptor antagonists), TBXA2R antagonists(Thromboxane A2 receptor antagonists), TXA2 synthase inhibitors(Thromboxane A2 synthase inhibitors)

Therapeutic Areas

Endocrinology and Metabolic DiseaseUrogenital Diseases

Active Indication

AlbuminuriaDiabetes Mellitus, Type 2Diabetic Nephropathies

Inactive Indication

Diabetes Mellitus, Noninsulin-Dependent, 2Influenza A virus infectionstress oxidative+ [1]

Originator Organization

Evolva Holding SA

Active Organization

Serodus ASA

Evolva Holding SA

Inactive Organization

Evolva SA

Drug Highest PhasePhase 2/3

First Approval Date-

Regulation-

Login to view timeline

Structure

Molecular FormulaC22H23ClO5

InChIKeyWHUIENZXNGAHQI-GKZDNZBASA-N

CAS Registry1041850-31-0

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).

Start Date18 Aug 2021

Sponsor / Collaborator

Serodus ASA

NCT01551381 / TerminatedPhase 2

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.

Start Date01 Jan 2012

Sponsor / Collaborator

Evolva SA

100 Clinical Results associated with EV-077

Login to view more data

100 Translational Medicine associated with EV-077

Login to view more data

100 Patents (Medical) associated with EV-077

Login to view more data

9

Literatures (Medical) associated with EV-077

01 Oct 2022·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

Author: 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.

01 Apr 2014·Journal of Thrombosis and ThrombolysisQ4 · MEDICINE

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

Q4 · MEDICINE

Article

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

01 Feb 2014·Journal of Thrombosis and ThrombolysisQ4 · MEDICINE

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

Q4 · MEDICINE

Article

Author: Fabiana Rollini ; Ryan E. Wilson ; Francesco Franchi ; Andrew Darlington ; Antonio Tello-Montoliu ; Dominick J. Angiolillo ; Ana Muñiz-Lozano ; Norbert Bender ; 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 Deals associated with EV-077

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Albuminuria	Phase 3	NZ	Serodus ASA	18 Aug 2021
Albuminuria	Phase 3	AU	Serodus ASA	18 Aug 2021
Diabetes Mellitus, Type 2	Phase 3	AU	Serodus ASA	18 Aug 2021
Diabetes Mellitus, Type 2	Phase 3	NZ	Serodus ASA	18 Aug 2021
Diabetic Nephropathies	Phase 3	NZ	Serodus ASA	18 Aug 2021
Diabetic Nephropathies	Phase 3	AU	Serodus ASA	18 Aug 2021
Diabetes Mellitus, Noninsulin-Dependent, 2	Phase 1	DE	Evolva SA	01 Jan 2012
stress oxidative	Phase 1	DE	Evolva SA	01 Jan 2012
Vasculitis	Phase 1	DE	Evolva SA	01 Jan 2012
Influenza A virus infection	Discovery	CH	Evolva Holding SA	-