Grazoprevir

A hepatitis C virus protease inhibitor.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Used to treat other disease

4
Supporting references
0
Contradictory references
9
AI-suggested references
0
Clinical trials

General information

Grazoprevir is a hepatitis C virus (HCV) serine protease inhibitor. It is used in a combined anti-HCV therapy (DrugBank).

Grazoprevir on PubChem
Grazoprevir on Wikipedia


Marketed as

ZEPATIER (in a fixed dose with ELBASVIR)

 

Structure image - Grazoprevir

CC(C)(C)[C@H]1C(=O)N2C[C@@H](C[C@H]2C(=O)N[C@@]3(C[C@H]3C=C)C(=O)NS(=O)(=O)C4CC4)OC5=NC6=C(C=CC(=C6)OC)N=C5CCCCC[C@@H]7C[C@H]7OC(=O)N1


Supporting references

Link Tested on Impact factor Notes Publication date
Predicting commercially available antiviral drugs that may act on the novel coronavirus (2019-nCoV), Wuhan, China through a drug-target interaction deep learning model
Preprint In silico
in silico Feb/02/2020
In silico structure modelling of SARS-CoV-2 Nsp13 helicase and Nsp14 and repurposing of FDA approved antiviral drugs as dual inhibitors
nsp13 nsp14 Small molecule In silico
in silico 0.61

Predicted to inhibit both the SARS-CoV-2 Nsp13 helicase and Nsp14 exoribonuclease.

Aug/28/2020
Combined in silico and in vitro approaches identified the antipsychotic drug lurasidone and the antiviral drug elbasvir as SARS-CoV2 and HCoV-OC43 inhibitors
RdRpol Small molecule In vitro In silico
in silico; Huh 7-hACE2 cells 4.10

Inhibited SARS-CoV-2 infection in a high content microscopy assay with an EC50 of ca. 16 μM and high selectivity (CC50 of ca. 118). The drug also displayed efficacy in a viral yield reduction assay with an estimated EC50 of ca. 3.3 μM. Based on computational modelling, the antiviral activity stems from RNA-dependent RNA polymerase inhibition.

Mar/10/2021
Computational drug repurposing study elucidating simultaneous inhibition of entry and replication of novel corona virus by Grazoprevir
ACE2 TMPRSS2 Small molecule In silico
in silico 4.00

The drug was computationally modelled to inhibit the host ACE2 and TMPRSS2 enzymes.

Mar/31/2021

AI-suggested references