Delving into the Latest Updates on Eprosartan Mesylate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(E)-2-butyl-1-(p-carboxybenzyl)-α-2-thenylimidazole-5-acrylic acid, (E)-3-[2-n-butyl-1-{(4-carboxyphenyl)methyl}-1H-imidazol-5-yl]-2-(2-thienyl)methyl-2-propenoic acid, (E)-α{[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazole-5-yl]methylene}-2-thiopheneproprionic acid

+ [18]

Target

AT1R

Mechanism

AT1R antagonists(Angiotensin II Receptor Type 1 antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

HypertensionEssential Hypertension

Inactive Indication-

Originator Organization

AbbVie, Inc.

Active Organization

Abbott Healthcare Products BVViatris Pty Ltd.Viatris Healthcare GmbH

+ [1]

Inactive Organization

Alere, Inc.

AbbVie, Inc.

Solvay Pharmaceuticals, Inc.

Drug Highest PhaseApproved

First Approval Date

US (22 Dec 1997),

Hypertension

Regulation-

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Structure/Sequence

Molecular FormulaC24H28N2O7S2

InChIKeyDJSLTDBPKHORNY-XMMWENQYSA-N

CAS Registry144143-96-4

View All Structures (2)

SARS-CoV-2 is a member of a class of viruses: angiotensin converting enzyme 2 (ACE2)-binding viruses that study calls "ABVs". The World Health Organization (WHO) and others are performing randomized controlled trials (RCTs) of vaccines and novel antivirals to address SARS-CoV-2 directly. However, the critical illness complications of COVID-19 are caused in part by SARS-CoV-2's binding and inhibiting ACE2 and the consequent host response.
ACE 2 is the receptor for H1N1, H5N1, and SARS-CoV-2. After binding ACE2, SARS-CoV-2 is endocytosed, and surface ACE2 is down-regulated, increasing angiotensin II (ATII a potent vasoconstrictor) in COVID-19. The original ARBs limits lung injury in murine influenza H7N9 and decreases viral titre and RNA.
Study has a unique opportunity to complement vaccine and anti-viral RCTs with an RCT modulating the host response using an angiotensin II type 1 receptor blocker (ARBs) to decrease the mortality of hospitalized COVID-19 patient.

Start Date09 Oct 2020

Sponsor / Collaborator

University of British Columbia

[+1]

EUCTR2010-019155-22-DE

/ Not yet recruitingNot Applicable

A Prospective, Randomized, Double-Blind, Parallel-Group Study to Compare the Effect of Eprosartan and Eprosartan Mesylate on Blood Pressure in Subjects with Essential Hypertension

Start Date25 Jun 2012

Sponsor / Collaborator-

NCT01631227

/ CompletedPhase 3

A Prospective, Randomized Double-blind Parallel Group Study to Compare the Effect of Eprosartan and Eprosartan Mesylate on Blood Pressure in Subjects With Mild to Moderate Essential Hypertension

Aim of this study is to compare the blood pressure lowering effect of a new drug formulation of eprosartan. Eprosartan belongs to a class of blood pressure lowering agents used worldwide since years with proven efficacy. The new formulation is compared to the currently marketed eprosartan tablet. Equivalent efficacy in blood pressure lowering effects should be demonstrated.

Start Date01 Jun 2012

Sponsor / Collaborator

Alere, Inc.

[+2]

100 Clinical Results associated with Eprosartan Mesylate

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100 Translational Medicine associated with Eprosartan Mesylate

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100 Patents (Medical) associated with Eprosartan Mesylate

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450

Literatures (Medical) associated with Eprosartan Mesylate

02 Oct 2024·Expert Review of Cardiovascular Therapy

The role of eprosartan in the management of essential hypertension: literature review and expert opinion

Review

Author: Escobar, Carlos ; Mazón, Pilar ; Rivadulla, Claudio ; Chandrappa, Shukrath

INTRODUCTIONEprosartan is an angiotensin receptor blocker (ARB) used for management of essential hypertension. With unique pharmacological characteristics, dual action mechanism, and clinical effectiveness, eprosartan offers additional advantages over other ARBs in specific patient populations.AREAS COVEREDA comprehensive review of the literature was performed across publicly available databases, with no time limitations, to ensure the inclusion of all relevant studies. The review focuses on presenting the efficacy and safety profile of eprosartan, alone or in combination with other agents. Additionally, it explores the etiology of hypertension concerning the structure and function of angiotensin II type 1 receptors. Further, the efficacy of eprosartan in special populations and its additional benefits are also discussed.EXPERT OPINIONEprosartan effectively reduces blood pressure (BP), with a 24-hour BP-lowering effect at 600 mg/day. Eprosartan demonstrates similar or better efficacy than other ARBs, such as telmisartan and losartan, particularly in managing coagulation-related abnormalities and peripheral resistance. In combination therapy, eprosartan with hydrochlorothiazide significantly enhances BP reduction. Eprosartan is well-tolerated, with a low incidence of adverse events, making it a reliable choice for long-term hypertension management across various patient populations, such as those with comorbid diabetes and renal disease and older adults.

01 Jun 2024·Molecular Diversity

Targeting lipid-sensing nuclear receptors PPAR (α, γ, β/δ): HTVS and molecular docking/dynamics analysis of pharmacological ligands as potential pan-PPAR agonists

Article

Author: Sharma, Pankaj Kumar ; Muzaffar-Ur-Rehman, Mohammed ; Kumar, Banoth Karan ; Sankaranarayanan, Murugesan ; Mandal, Sumit Kumar ; Puri, Sonakshi ; Deepa, P R

The global prevalence of obesity-related systemic disorders, including non-alcoholic fatty liver disease (NAFLD), and cancers are rapidly rising. Several of these disorders involve peroxisome proliferator-activated receptors (PPARs) as one of the key cell signaling pathways. PPARs are nuclear receptors that play a central role in lipid metabolism and glucose homeostasis. They can activate or suppress the genes responsible for inflammation, adipogenesis, and energy balance, making them promising therapeutic targets for treating metabolic disorders. In this study, an attempt has been made to screen novel PPAR pan-agonists from the ZINC database targeting the three PPAR family of receptors (α, γ, β/δ), using molecular docking and molecular dynamics (MD) simulations. The top scoring five ligands with strong binding affinity against all the three PPAR isoforms were eprosartan, canagliflozin, pralatrexate, sacubitril, olaparib. The ADMET analysis was performed to assess the pharmacokinetic profile of the top 5 molecules. On the basis of ADMET analysis, the top ligand was subjected to MD simulations, and compared with lanifibranor (reference PPAR pan-agonist). Comparatively, the top-scoring ligand showed better protein-ligand complex (PLC) stability with all the PPARs (α, γ, β/δ). When experimentally tested in in vitro cell culture model of NAFLD, eprosartan showed dose dependent decrease in lipid accumulation and oxidative damage. These outcomes suggest potential PPAR pan-agonist molecules for further experimental validation and pharmacological development, towards treatment of PPAR-mediated metabolic disorders.

01 May 2024·Annals of Pharmacotherapy

Angiotensin Receptor Blocker–Related Sprue-like Enteropathy: Review of Food and Drug Administration Adverse Event Reporting System

Article

Author: Dang, Hoang ; Ahdi, Hardeep ; Ehrenpreis, Eli D ; Meader, Ryan ; Papasotiriou, Sam

Background: Sprue-like enteropathy (SE) related to olmesartan use was first reported in 2012. In 2017, the manufacturer of Benicar paid $300 million for 2300 claims for olmesartan-related SE. Objective: A study in 2019 suggested that SE was related to olmesartan and with the possibility of angiotensin receptor blocker (ARB) class effect. To further characterize this condition, our group examined reports of ARB-related SE to Food and Drug Administration Adverse Event Reporting System (FAERS). Methods: All reports of ARB-related SE from January 2017 to December 2021 were downloaded from the FAERS database. Gastrointestinal adverse events including SE were reviewed. Reporter categories included physicians, pharmacists, other health care professionals, consumers, and attorneys. Results: A total of 106 590 reports of ARB-related adverse effects were analyzed. Sprue-like enteropathy was identified in 4337 cases (4.1% of total reports). Of these, 4240 cases (98.0%) of ARB-related SE were reported in patients using products with olmesartan, and 97 cases of SE were reported for all other ARBs (eprosartan, losartan, telmisartan, irbesartan, valsartan, and candesartan). Reports of olmesartan-related SE increased rapidly in 2017, continued at a high rate in 2018 and 2019, and essentially stopped in 2020 and 2021. Conclusions and Relevance: Reports to FAERS for ARB-related SE are mostly related to olmesartan. There was a steep decline in reports of olmesartan-related SE following the lawsuit with potential of lawyer interference. There are reports of SE related to ARBs other than olmesartan, with increased physician awareness and the potential to discover a class effect with future studies.

100 Deals associated with Eprosartan Mesylate

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External Link

KEGG	Wiki	ATC	Drug Bank
D02082	Eprosartan Mesylate	C09CA02	DB00876

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	CN	Abbott Healthcare Products BV	28 Dec 2007
Essential Hypertension	AU	Viatris Pty Ltd.	15 Jun 1998

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Essential Hypertension	Phase 3	CA	Solvay Pharmaceuticals, Inc.	08 Sep 2000

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ESC2018	Not Applicable	Essential Hypertension N-terminal pro-brain natriuretic peptide (NT-proBNP)	165	Eprosartan	xqrbeflsgk(ztwuaaxawx) = muztriyexb ozaahtwpor (nixnoqgrup )	-	27 Aug 2018
[PP.31.06] (ESH2016)	Not Applicable	Essential Hypertension NT-proBNP levels \| LVH	154	Eprosartan	(rleatadlqs) = pqiuicjdmo vdhatqjcmj (enmeblzxhz )	Positive	01 Sep 2016
NCT01631227 (CTgov)	Phase 3	Essential Hypertension	665	Placebo Eprosartan mesylate+Eprosartan (Eprosartan)	abucczylbu(zctzvakyoo) = zpjqvpozuw hqdrmychqa (nbtryqojma, lfnxoehage - kdktbzwvhb) View more	-	26 May 2014
				Placebo Eprosartan+Eprosartan Mesylate (Eprosartan Mesylate)	abucczylbu(zctzvakyoo) = byuxywmfno hqdrmychqa (nbtryqojma, jrdfbvqbpl - kxjzjmulvl) View more
PP.24.479 (ESH2010)	Not Applicable	Hypertension	120	Enalapril 20 mg/day	(pevoxrrzqs) = ixzirqykch jjlbnlquyx (kqgqxmnujj ) View more	Positive	01 Jun 2010
				Eprosartan 600 mg/day	(pevoxrrzqs) = dgrsvrbewi jjlbnlquyx (kqgqxmnujj ) View more
MOSES (Pubmed \| Stroke)	Phase 4	Stroke	1,405	Eprosartan	(umzcapqcvr) = eidbhfobdz ihriyrrqoc (cwtussfoiw )	-	01 Jun 2005
				Nitrendipine	(umzcapqcvr) = qzoswclzkl ihriyrrqoc (cwtussfoiw )