Ebselen

An organoselenium anti-oxidant.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Experimental

3
Supporting references
0
Contradictory references
28
AI-suggested references
2
Clinical trials

General information

Ebselen is an organoselenium glutathione peroxidase mimetic with anti-inflammatory, antioxidant, and cytoprotective properties. It also inhibits the activity of multiple enzymes (NCIt).

Ebselen on DrugBank
Ebselen on PubChem
Ebselen on Wikipedia


Synonyms

2-phenyl-1,2-benzoselenazol-3-one; Ebselenum; PZ 51; DR3305; SPI-1005

 

Structure image - Ebselen

C1=CC=C(C=C1)N2C(=O)C3=CC=CC=C3[Se]2


Supporting references

Link Tested on Impact factor Notes Publication date
Discovering drugs to treat coronavirus disease 2019 (COVID-19).
in silico Feb/22/2020
Molecular characterization of ebselen binding activity to SARS-CoV-2 main protease
3CLpro Small molecule In silico
in silico 13.12

Predicted to allosterically block the catalytic site of the SARS-CoV-2 3C-like protease.

Oct/04/2020
Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors
3CLpro Crystallization Enzyme assay In vitro In silico
in silico; in vitro enzyme assay; crystallization; Vero E6 cells 42.78

The compound inhibited the SARS-CoV-2 3C-like protease in vitro with IC50 of ca. 0.67 μM and SARS-CoV-2 infection in Vero E6 cells with EC50 of ca. 4.67 μM.

Jun/11/2020

AI-suggested references

Link Publication date
Cysteine Modification by Ebselen Reduces the Stability and Cellular Levels of 14-3-3 Proteins.
May/24/2021
Ebselen suitably interacts with the potential SARS-CoV-2 targets: an in-silico approach.
Aug/30/2021
In vitro and in silico studies of potential coronavirus-specific 3C-like protease inhibitors.
Apr/29/2022
Novel Selenium-based compounds with therapeutic potential for SOD1-linked amyotrophic lateral sclerosis.
Aug/30/2020
Design and Evaluation of Bispidine-Based SARS-CoV-2 Main Protease Inhibitors.
Sep/29/2021
Potential therapeutic use of ebselen for COVID-19 and other respiratory viral infections
Jun/26/2020
Structure-Activity Studies Reveal Scope for Optimisation of Ebselen-Type Inhibition of SARS-CoV-2 Main Protease
Jun/06/2020
Inhibition mechanism of SARS-CoV-2 main protease by ebselen and its derivatives
May/24/2021
Ebsulfur and Ebselen as highly potent scaffolds for the development of potential SARS-CoV-2 antivirals.
Apr/08/2021
Characterization of the SARS-CoV-2 ExoN (nsp14ExoN-nsp10) complex: implications for its role in viral genome stability and inhibitor identification
Feb/17/2022
The Potential Use of Ebselen in Treatment-Resistant Depression
Apr/16/2022
The Se-S Bond Formation in the Covalent Inhibition Mechanism of SARS-CoV-2 Main Protease by Ebselen-like Inhibitors: A Computational Study.
Sep/10/2021
In silico Studies on the Interaction Between Mpro and PLpro From SARS-CoV-2 and Ebselen, its Metabolites and Derivatives
May/21/2021
Multi-targeting of functional cysteines in multiple conserved SARS-CoV-2 domains by clinically safe Zn-ejectors.
Sep/01/2020
Ebselen, Disulfiram, Carmofur, PX-12, Tideglusib, and Shikonin Are Nonspecific Promiscuous SARS-CoV-2 Main Protease Inhibitors.
Oct/09/2020
COVID-19: inflammatory responses, structure-based drug design and potential therapeutics
Aug/20/2020
Identification of ebselen and its analogues as potent covalent inhibitors of papain-like protease from SARS-CoV-2.
Feb/11/2021
The Mpro structure-based modifications of ebselen derivatives for improved antiviral activity against SARS-CoV-2 virus
Oct/30/2021
Invalidation of dieckol and 1,2,3,4,6-pentagalloylglucose (PGG) as SARS-CoV-2 main protease inhibitors and the discovery of PGG as a papain-like protease inhibitor
May/12/2022
Evaluation of SARS-CoV-2 Main Protease Inhibitors Using a Novel Cell-Based Assay.
Feb/02/2022
Site mapping and small molecule blind docking reveal a possible target site on the SARS-CoV-2 main protease dimer interface
Jan/25/2021
Validation and invalidation of SARS-CoV-2 main protease inhibitors using the Flip-GFP and Protease-Glo luciferase assays
May/05/2021
A connectivity map-based drug repurposing study and integrative analysis of transcriptomic profiling of SARS-CoV-2 infection.
Oct/29/2020
Discovery and Mechanism of SARS-CoV-2 Main Protease Inhibitors
Sep/27/2021
Determination of potential inhibitors based on isatin derivatives against SARS-CoV-2 main protease (mpro): a molecular docking, molecular dynamics and structure-activity relationship studies
Apr/05/2021
SAR and QSAR of COVID-19 Main Protease-Inhibitor Interactions of Recently X-ray Crystalized Complexes
Feb/03/2022
Synergistic Inhibition of SARS-CoV-2 Replication Using Disulfiram/Ebselen and Remdesivir.
Mar/26/2021
A VSV-based assay quantifies coronavirus Mpro/3CLpro/Nsp5 main protease activity and chemical inhibition
Jan/28/2022

Clinical trials

ID Title Status Phase Start date Completion date
NCT04484025 SPI-1005 Treatment in Moderate COVID-19 Patients Enrolling by invitation Phase 2 Oct/12/2021 Aug/01/2022
  • Alternative id - SPI-1005-291
  • Interventions - Drug: Ebselen|Drug: Placebo
  • Study type - Interventional
  • Study results - No Results Available
  • Locations - Yale University, New Haven, Connecticut, United States|St. Luke's Cystic Fibrosis Center of Idaho, Boise, Idaho, United States|Kansas University Medical Center, Kansas City, Kansas, United States|Washington University in St. Louis, Saint Louis, Missouri, United States|Duke University, Durham, North Carolina, United States|Wake Forest University, Winston-Salem, North Carolina, United States|University of Texas Southwestern, Dallas, Texas, United States
  • Study designs - Allocation: Randomized|Intervention Model: Parallel Assignment|Masking: Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)|Primary Purpose: Treatment
  • Enrollment - 60
  • Age - 18 Years and older   (Adult, Older Adult)
  • Outcome measures - Number of participants with treatment-related adverse events|WHO Ordinal Scale|Degree of supplemental oxygen|Peripheral Oxygen Saturation (SpO2)
NCT04483973 SPI-1005 Treatment in Severe COVID-19 Patients Enrolling by invitation Phase 2 Aug/27/2021 Aug/01/2022
  • Alternative id - SPI-1005-292
  • Interventions - Drug: Ebselen|Drug: Placebo
  • Study type - Interventional
  • Study results - No Results Available
  • Locations - Yale University, New Haven, Connecticut, United States|St. Luke's Cystic Fibrosis Center of Idaho, Boise, Idaho, United States|Kansas University Medical Center, Kansas City, Kansas, United States|Washington University in St. Louis, Saint Louis, Missouri, United States|Duke University, Durham, North Carolina, United States|Wake Forest University, Winston-Salem, North Carolina, United States|University of Texas Southwestern, Dallas, Texas, United States
  • Study designs - Allocation: Randomized|Intervention Model: Parallel Assignment|Masking: Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)|Primary Purpose: Treatment
  • Enrollment - 60
  • Age - 18 Years and older   (Adult, Older Adult)
  • Outcome measures - Number of participants with treatment-related adverse events|WHO Ordinal Scale|Degree of supplemental oxygen|Peripheral Oxygen Saturation (SpO2)