Telaprevir

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
13
AI-suggested references
0
Clinical trials

General information

Telaprevir is a peptidomimetic drug that selectively inhibits the hepatitis C virus (HCV) serine protease NS3-4A, which hinders the viral replication (NCIt).

Telaprevir on DrugBank
Telaprevir on PubChem
Telaprevir on Wikipedia


Marketed as

INCIVEK

 

Structure image - Telaprevir

CCC[C@@H](C(=O)C(=O)NC1CC1)NC(=O)[C@@H]2[C@H]3CCC[C@H]3CN2C(=O)[C@H](C(C)(C)C)NC(=O)[C@H](C4CCCCC4)NC(=O)C5=NC=CN=C5


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
A drug repurposing screen identifies hepatitis C antivirals as inhibitors of the SARS-CoV2 main protease
3CLpro Enzyme assay In vitro In silico Screening
in silico; in vitro enzyme assay 2.74

Inhibited the SARS-CoV-2 3C-like protease in vitro with IC50 of ca. 15.25 μM.

Feb/01/2021
Inhibition of SARS-CoV-2 main protease 3CLpro by means of α-ketoamide and pyridone-containing pharmaceuticals using in silico molecular docking
3CLpro Small molecule In silico
in silico 2.46

Predicted to inhibit the SARS-CoV-2 3C-like protease.

Jul/10/2020
Malleability of the SARS-CoV-2 3CL Mpro Active-Site Cavity Facilitates Binding of Clinical Antivirals
3CLpro Small molecule Enzyme assay In vitro
in vitro enzyme assay; X-ray crystallography 4.86

When co-crystalized with the SARS-CoV-2 3C-like protease (3CLpro), the drug was observed to interact with and structurally modify the enzyme's active site. The drug also inhibited 3CLpro in vitro (although less potently than <a href=

Nov/08/2020

AI-suggested references

Link Publication date
Uncovering Flexible Active Site Conformations of SARS-CoV-2 3CL Proteases through Protease Pharmacophore Clusters and COVID-19 Drug Repurposing.
Sep/27/2021
Synergistic Interferon-Alpha-Based Combinations for Treatment of SARS-CoV-2 and Other Viral Infections.
Dec/11/2021
Telaprevir is a potential drug for repurposing against SARS-CoV-2: computational and in vitro studies.
Sep/09/2021
Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.
Jun/09/2021
Targeting SARS-CoV-2 M3CLpro by HCV NS3/4a Inhibitors: In Silico Modeling and In Vitro Screening
Feb/04/2021
Repurposing the HCV NS3-4A protease drug boceprevir as COVID-19 therapeutics
Dec/21/2020
Screening of potential inhibitors of COVID-19 with repurposing approach via molecular docking
Feb/04/2022
A computational drug repurposing approach in identifying the cephalosporin antibiotic and anti-hepatitis C drug derivatives for COVID-19 treatment.
Dec/19/2020
Direct Observation of Protonation State Modulation in SARS-CoV-2 Main Protease upon Inhibitor Binding with Neutron Crystallography
Oct/13/2021
Inhibition of SARS-CoV-2 main protease 3CLpro by means of alpha-ketoamide and pyridone-containing pharmaceuticals using in silico molecular docking.
Jul/10/2020
Targeted design of drug binding sites in the main protease of SARS-CoV-2 reveals potential signatures of adaptation.
Mar/26/2021
In search of drugs to alleviate suppression of the host's innate immune responses against SARS-CoV-2 using a molecular modeling approach.
Apr/04/2021
Pre-Steady-State Kinetics of the SARS-CoV-2 Main Protease as a Powerful Tool for Antiviral Drug Discovery.
Dec/06/2021