Other substances

Boceprevir

A tripeptide hepatitis C virus inhibitor.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Used to treat other disease

Supporting references

Contradictory references

AI-suggested references

Clinical trials

General information

Boceprevir is a synthetic tripeptide inhibitor of hepatitis C virus (HCV) genotype 1. It prevents NS3/NS4A protease-mediated viral polyprotein maturation and thereby inhibits viral replication (NCIt).

Boceprevir on DrugBank
Boceprevir on PubChem
Boceprevir on Wikipedia

Synonyms

Victrelis

Marketed as

VICTRELIS

CC1([C@@H]2[C@H]1[C@H](N(C2)C(=O)[C@H](C(C)(C)C)NC(=O)NC(C)(C)C)C(=O)NC(CC3CCC3)C(=O)C(=O)N)C

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
Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease 3CLpro Crystallization Small molecule Enzyme assay In vitro	in vitro enzyme assay; crystallization; Vero 76 cells; SARS-CoV-2 strain USA-WA1/2020	20.51	Inhibited SARS-CoV-2 3C-like protease with an IC50 of ca. 4.13 μM in vitro. Inhibited SARS-CoV-2 infection in primary CPE assay with an EC50 of ca. 1.31 μM and an SI of >76.3.	Jun/15/2020
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. 0.95 μM.	Feb/01/2021
Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease 3CLpro Small molecule Enzyme assay In vitro	Vero cells; enzyme assay	12.12	Inhibit SARS-CoV-2 3C-like protease in vitro via catalytically active site binding.	Sep/04/2020
Potential clinical drugs as covalent inhibitors of the priming proteases of the spike protein of SARS-CoV-2 TMPRSS2 Cathepsin B Cathepsin L Small molecule In silico	in silico	6.02	Predicted to inhibit the host TMPRSS2 protease and thereby inhibit the SAS-CoV-2 entry.	Aug/26/2020
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.	Nov/08/2020
Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2 3CLpro Small molecule Enzyme assay In vitro	in vitro enzyme assay	3.75	Inhibited the SARS-CoV-2 3C-like protease in vitro with IC50 of 5.4 μM.	Oct/25/2020
Identification of existing pharmaceuticals and herbal medicines as inhibitors of SARS-CoV-2 infection 3CLpro PapainLpro Enzyme assay Animal model In vitro In silico	in silico; in vitro enzyme assay; Vero E6 cells; golden Syrian hamsters; SARS-CoV-2 clinical isolate hCoV-19/Taiwan/4/2020	9.41	Inhibited (not potently) SARS-CoV-2 infection in Vero E6 cells. Inhibited SARS-CoV-2 3C-like protease in vitro.	Jan/15/2021
Systematic Search for SARS-CoV-2 Main Protease Inhibitors for Drug Repurposing: Ethacrynic Acid as a Potential Drug 3CLpro Enzyme assay In vitro In silico	in silico; in vitro enzyme assay	3.82	Predicted to inhibit the SARS-CoV-2 3C-like protease.	Jan/13/2021
Identification of 3-chymotrypsin like protease (3CLPro) inhibitors as potential anti-SARS-CoV-2 agents 3CLpro Small molecule Enzyme assay In vitro In silico	in silico; in vitro enzyme assay		Partialy inhibits (IC50 of 31.4 µM; 45% inhibition at 50 µM) the SARS-CoV-2 3C-like protease in vitro.	Jan/20/2021
Development of a Cell-Based Luciferase Complementation Assay for Identification of SARS-CoV-2 3CLpro Inhibitors 3CLpro Small molecule Enzyme assay In vitro	in vitro enzyme assay	3.82	The compound inhibited the SARS-CoV-2 3C-like protease in vitro with EC50 of 38.6 μM and CC50 of >100 μM.	Jan/24/2021
Dual inhibition of SARS-CoV-2 and human rhinovirus with protease inhibitors in clinical development 3CLpro Cathepsin L Small molecule Enzyme assay In vitro	in vitro enzyme assay	4.10	The compound inhibited the SARS-CoV-2 3C-like protease with IC50 of 15.6 μM and human cathepsin L with IC50 of 2.3 μM in vitro. The cathepsin L inhibition was relatively weak compared to some other inhibitors.	Jan/27/2021
Boceprevir, Calpain Inhibitors II and XII, and GC-376 Have Broad-Spectrum Antiviral Activity against Coronaviruses Biophysical assay Cathepsin L Enzyme assay In vitro Mechanism	in vitro enzyme assay; in vitro biophysical assay; Vero cells; Caco-2 cells; (HIV-1) SARS-CoV-2 Spike pseudovirus	4.61	The compound inhibited SARS-CoV-2 replication in Caco-2 cells with an EC50 of ca. 2.97 μM and low cytotoxicity (CC50 >100 μM).	Mar/01/2021

AI-suggested references

Link	Publication date
Virtual screening of natural products inspired in-house library to discover potential lead molecules against the SARS-CoV-2 main protease.	Nov/30/2020
Uncovering Flexible Active Site Conformations of SARS-CoV-2 3CL Proteases through Protease Pharmacophore Clusters and COVID-19 Drug Repurposing.	Sep/27/2021
Computational insights into binding mechanism of drugs as potential inhibitors against SARS-CoV-2 targets.	Aug/30/2021
Apigenin analogues as SARS-CoV-2 main protease inhibitors: In-silico screening approach	Jan/21/2022
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
Artificial intelligence approach fighting COVID-19 with repurposing drugs	May/15/2020
Supervised Molecular Dynamics (SuMD) Insights into the mechanism of action of SARS-CoV-2 main protease inhibitor PF-07321332	Jul/23/2021
Repurposing the HCV NS3-4A protease drug boceprevir as COVID-19 therapeutics	Dec/21/2020
Structural and conformational analysis of SARS CoV 2 N-CTD revealing monomeric and dimeric active sites during the RNA-binding and stabilization: Insights towards potential inhibitors for N-CTD.	May/15/2021
Differing pan-coronavirus antiviral potency of boceprevir and GC376 in vitro despite discordant molecular docking predictions	Feb/16/2022
Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors	May/30/2021
Covalent narlaprevir- and boceprevir-derived hybrid inhibitors of SARS-CoV-2 main protease	Apr/27/2022
Identification of high affinity and low molecular alternatives of boceprevir against SARS-CoV-2 main protease: A virtual screening approach	May/15/2020
Naturally occurring anthraquinones as potential inhibitors of SARS-CoV-2 main protease: an integrated computational study	Mar/01/2022
Targeted design of drug binding sites in the main protease of SARS-CoV-2 reveals potential signatures of adaptation.	Mar/26/2021
Potential Role of Colchicine in Combating COVID-19 Cytokine Storm and Its Ability to Inhibit Protease Enzyme of SARS-CoV-2 as Conferred by Molecular Docking Analysis	Sep/09/2020
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
A VSV-based assay quantifies coronavirus Mpro/3CLpro/Nsp5 main protease activity and chemical inhibition	Jan/28/2022

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