A tripeptide hepatitis C virus inhibitor.

Phase of research

Potential treatment - pre-clinical evidence

How it helps


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



Marketed as



Structure image - Boceprevir


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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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).


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.
Uncovering Flexible Active Site Conformations of SARS-CoV-2 3CL Proteases through Protease Pharmacophore Clusters and COVID-19 Drug Repurposing.
Computational insights into binding mechanism of drugs as potential inhibitors against SARS-CoV-2 targets.
Apigenin analogues as SARS-CoV-2 main protease inhibitors: In-silico screening approach
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.
Targeting SARS-CoV-2 M3CLpro by HCV NS3/4a Inhibitors: In Silico Modeling and In Vitro Screening
Artificial intelligence approach fighting COVID-19 with repurposing drugs
Supervised Molecular Dynamics (SuMD) Insights into the mechanism of action of SARS-CoV-2 main protease inhibitor PF-07321332
Repurposing the HCV NS3-4A protease drug boceprevir as COVID-19 therapeutics
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.
Differing pan-coronavirus antiviral potency of boceprevir and GC376 in vitro despite discordant molecular docking predictions
Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors
Covalent narlaprevir- and boceprevir-derived hybrid inhibitors of SARS-CoV-2 main protease
Identification of high affinity and low molecular alternatives of boceprevir against SARS-CoV-2 main protease: A virtual screening approach
Naturally occurring anthraquinones as potential inhibitors of SARS-CoV-2 main protease: an integrated computational study
Targeted design of drug binding sites in the main protease of SARS-CoV-2 reveals potential signatures of adaptation.
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
In search of drugs to alleviate suppression of the host's innate immune responses against SARS-CoV-2 using a molecular modeling approach.
Pre-Steady-State Kinetics of the SARS-CoV-2 Main Protease as a Powerful Tool for Antiviral Drug Discovery.
A VSV-based assay quantifies coronavirus Mpro/3CLpro/Nsp5 main protease activity and chemical inhibition