Delving into the Latest Updates on Elbasvir with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Elbasvir, Elbasvir (JAN/USAN/INN)

+ [1]

Target

NS5A

Mechanism

NS5A inhibitors(Nonstructural protein 5A inhibitors)

Therapeutic Areas

Infectious DiseasesDigestive System Disorders

Active Indication

Hepatitis CHepatitis C, Chronic

Inactive Indication-

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization

Merck Sharp & Dohme Corp.

Merck & Co., Inc.WuXi AppTec (Shanghai) Co. Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

JP (28 Sep 2016),

Hepatitis C

Regulation-

Login to view timeline

Structure

Molecular FormulaC49H55N9O7

InChIKeyBVAZQCUMNICBAQ-PZHYSIFUSA-N

CAS Registry1370468-36-2

Localized on site testing and treatment of hepatitis C in homeless persons in London: a pilot non-randomised phase 4 interventional clinical trial of grazoprevir and elbasvir ± ribavirin in participants with genotype 1a, 1b or 4 to measure efficacy and adherence to treatment in a homeless population - ATTIC - Access To Treat in the Community

Start Date02 Jan 2019

Sponsor / Collaborator

King's College Hospital NHS Foundation Trust

NCT03037151 / Unknown statusPhase 4IIT

Safety and Fibrosis Improvement of Grazoprevir and Elbasvir for HCV GT1 and GT6 With or Without HIV

This study will evaluate the safety and efficacy of combination treatment with grazoprevir + elbasvir for compensated cirrhotic participants with chronic genotype 1 (GT1) and genotype 6 (GT6) hepatitis C virus (HCV) infection with or without human immunodeficiency virus (HIV) infection.

Start Date01 Aug 2018

Sponsor / Collaborator

The HIV Netherlands Australia Thailand Research Collaboration

[+2]

NCT03379506 / CompletedPhase 2

A Phase IIb Clinical Study to Assess the Pharmacokinetics, Safety, and Efficacy of the Combination Regimen of Elbasvir (EBR)/Grazoprevir (GZR) in Participants Aged 3 to Less Than 18 Years With Chronic Hepatitis C Infection

The purpose of this study is to assess the pharmacokinetics (PK), safety, and efficacy of oral MK-5172 (a fixed dose combination [FDC] tablet containing elbasvir [EBR] 50 mg and grazoprevir [GZR] 100 mg) and EBR/GZR (varying doses) pediatric granules in pediatric hepatitis C virus (HCV)-infected participants who are 3 to <18 years of age. Within each age cohort (Cohort 1: 12 to <18 years of age; Cohort 2: 7 to <12 years of age; and Cohort 3: 3 to <7 years of age), a Mini Cohort of 7 participants will be enrolled first. For the oldest cohort (Cohort 1), the Mini Cohort will assess ability to swallow a placebo tablet prior to administering active FDC tablets; participants in Cohorts 2 and 3 will take pediatric granules instead of a tablet.

Start Date25 Jan 2018

Sponsor / Collaborator

Merck Sharp & Dohme Corp.

100 Clinical Results associated with Elbasvir

Login to view more data

100 Translational Medicine associated with Elbasvir

Login to view more data

100 Patents (Medical) associated with Elbasvir

Login to view more data

368

Literatures (Medical) associated with Elbasvir

01 Dec 2024·Combinatorial Chemistry & High Throughput Screening

Evaluations of FDA-approved Drugs Targeting 3CLP of SARS-CoV-2 Employing a Repurposing Strategy

Article

Author: Ahmad, Syed Sayeed ; Khalid, Mohammad

Background:The SARS-CoV-2 coronavirus (COVID-19) has raised innumerable global concerns, and few effective treatment strategies have yet been permitted by the FDA to lighten the disease burden. SARS-CoV-2 3C-like proteinase (3CLP) is a crucial protease and plays a key role in the viral life cycle, as it controls replication, and thus, it is viewed as a target for drug design.Methods:In this study, we performed structure-based virtual screening of FDA drugs approved during 2015-2019 (a total of 220 drugs) for interaction with the active site of 3CLP (PDB ID 6LU7) using AutoDock 4.2. We report the top ten drugs that outperform the reported drugs against 3CLP (Elbasvir and Nelfinavir), particularly Cefiderocol, having the highest affinity among the compounds tested, with a binding energy of -9.97 kcal/mol. H-bond (LYS102:HZ2-ligand: O49), hydrophobic (ligand-VAL104), and electrostatic (LYS102:NZ-ligand: O50) interactions were observed in the cefiderocol-3CLP complex. The docked complex was subjected to a 50 ns molecular dynamics study to check its stability, and stable RMSD and RMSF graphs were observed.Results:Accordingly, we suggest cefiderocol might be effective against SARS-CoV-2 and urge that experimental validation be performed to determine the antiviral efficacy of cefiderocol against SARS-CoV-2.Discussion:Along with these, cefiderocol is effective for treating respiratory tract pathogens and a wide range of gram-negative bacteria for whom there are limited therapeutic alternativesConclusion:This article aimed to explore the FDA-approved drugs as a repurposing study against 3CLP for COVID-19 management.

01 Nov 2024·Annales Pharmaceutiques Françaises

Validated LC/MS method for simultaneous determination of elbasvir and grazoprevir in human plasma

Article

Author: Bensghaier, Rafika ; Labidi, Aymen ; Latrous, Latifa ; Jebali, Sami

A sensitive and accurate LC/MS method for the determination of elbasvir (ELB) and grazoprevir (GZP) in human plasma was established using daclatasvir (DCT) as an internal standard. The analytes were separated on a Waters Spherisorb phenyl column (150mm×4.6mm ID, 5μm particle size) maintained at 40°C±2°C. Gradient elution, at a flow rate of 0.8mLmin^-1, was used. The mobile phase consists of 90% of acetonitrile mixed to 10% of a 5mM ammonium formate buffer (+0.1% v/v of trimethylamine, pH was adjusted to 3.2 by formic acid) as phase A and 10% of acetonitrile mixed to 90% of the same buffer as phase B. Liquid-liquid extraction with ethyl acetate solvent was used to recuperate compounds from plasma. The method was validated over a concentration range of 2 and 100ng/mL for GZP and between 1 and 50ng/mL for ELB. The intra- and inter-day precision and accuracy of the quality control samples at low, medium, and high concentration levels exhibited relative standard deviations (RSD)<15%, and the accuracy values ranged from 94.2 to 107.8%. The robustness of the method was established using a two-level full factorial design.

01 Sep 2024·International Immunopharmacology

Genomic and computational-aided integrative drug repositioning strategy for EGFR and ROS1 mutated NSCLC

Article

Author: Kirtipal, Nikhil ; Khare, Aishwarya ; Shukla, Divyanshi ; Bharadwaj, Shiv ; Tripathi, Varsha ; Ranjan, Vandana

Non-small cell lung cancer (NSCLC) has been marked as the major cause of death in lung cancer patients. Due to tumor heterogeneity, mutation burden, and emerging resistance against the available therapies in NSCLC, it has been posing potential challenges in the therapy development. Hence, identification of cancer-driving mutations and their effective inhibition have been advocated as a potential approach in NSCLC treatment. Thereof, this study aims to employ the genomic and computational-aided integrative drug repositioning strategy to identify the potential mutations in the selected molecular targets and repurpose FDA-approved drugs against them. Accordingly, molecular targets and their mutations, i.e., EGFR (V843L, L858R, L861Q, and P1019L) and ROS1 (G1969E, F2046Y, Y2092C, and V2144I), were identified based on TCGA dataset analysis. Following, virtual screening and redocking analysis, Elbasvir, Ledipasvir, and Lomitapide drugs for EGFR mutants (>-10.8 kcal/mol) while Indinavir, Ledipasvir, Lomitapide, Monteleukast, and Isavuconazonium for ROS1 mutants (>-8.8 kcal/mol) were found as putative inhibitors. Furthermore, classical molecular dynamics simulation and endpoint binding energy calculation support the considerable stability of the selected docked complexes aided by substantial hydrogen bonding and hydrophobic interactions in comparison to the respective control complexes. Conclusively, the repositioned FDA-approved drugs might be beneficial alone or in synergy to overcome acquired resistance to EGFR and ROS1-positive lung cancers.

100 Deals associated with Elbasvir

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D10625	Elbasvir	J05AP10	DB11574

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Hepatitis C	JP	Merck Sharp & Dohme Corp.	28 Sep 2016

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Hepatitis C	Preclinical	SE	Merck Sharp & Dohme Corp.	25 Jan 2018
Hepatitis C	Preclinical	DE	Merck Sharp & Dohme Corp.	25 Jan 2018
Hepatitis C	Preclinical	PL	Merck Sharp & Dohme Corp.	25 Jan 2018
Hepatitis C	Preclinical	US	Merck Sharp & Dohme Corp.	25 Jan 2018
Hepatitis C, Chronic	Preclinical	-	Merck Sharp & Dohme Corp.	23 May 2014

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Pubmed	Phase 2/3	Chronic hepatitis C genotype 1b	1,070	Elbasvir 50 mg + Grazoprevir 100 mg	(afkoymkncn) = stboroefkc nfayuxlaoi (leiysxfafm ) View more	-	01 May 2018
NCT01797536 (8742-009, CTgov)	Phase 1	Hepatic Insufficiency	31	Elbasvir (Mild Hepatic Insufficiency)	sugwzyczlw(kwpjdeccbo) = rhsfkfcwjj puxkgiexao (vkrzeawdtk, flyhurwgdj - mogjhvrenr) View more	-	18 Nov 2016
NCT01797536 (8742-009, CTgov)	Phase 1	Hepatic Insufficiency	31	Elbasvir (Moderate Hepatic Insufficiency)	sugwzyczlw(kwpjdeccbo) = qgnplsnvmz puxkgiexao (vkrzeawdtk, qhqogemico - sbxgbhqumn) View more	-	18 Nov 2016
NCT02105454 (5172-048 \| C-SALVAGE, CTgov)	Phase 2	Hepatitis C, Chronic	79	Grazoprevir (GZR)+Elbasvir (EBR)+ribavirin (RBV)	enzyjkuqmr(nrbmwhflzx) = zkzuseulkf ewaeazhauc (jpnyzyopbr, rypbjbdvro - bfsxmjzavr) View more	-	04 Mar 2016
ASN2015	Not Applicable	Hepatitis C \| Chronic Kidney Diseases	224	Grazoprevir 100 mg + Elbasvir 50 mg	rbktaqpmmq(tqzmapvcyf) = At FW12 for GZR+EBR, GH improved from baseline (mean change score:4.5(95% CI:1.2-7.9)) ltrulzuzin (ezsxpcttkf )	Positive	03 Nov 2015
NCT02105454 (5172-048 \| C-SALVAGE, Pubmed \| J Hepatol) Manual	Phase 2	Hepatitis C, Chronic	79	Grazoprevir and elbasvir+ribavirin	(uoaovywegn) = lbqlapoebw vkfskbeqjm (awpgiglqza )	Positive	01 Sep 2015