Delving into the Latest Updates on Boceprevir with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Boceprevir (INN/USAN)

+ [2]

Target

NS3/NS4A

Action

inhibitors

Mechanism

NS3/NS4A inhibitors(Hepatitis C virus serine protease, NS3/NS4A inhibitors)

Therapeutic Areas

Infectious DiseasesDigestive System Disorders

Active Indication

Hepatitis C

Inactive Indication

AnemiaChronic hepatitis C genotype 1Coinfection+ [5]

Originator Organization

Merck & Co., Inc.

Active Organization

Merck GmbH

Inactive Organization

Merck Sharp & Dohme Ireland Ltd.

Merck Sharp & Dohme Corp.F. Hoffmann-La Roche Ltd.

+ [2]

Drug Highest PhaseApproved

First Approval Date

United States (13 May 2011),

FibrosisHepatitis C, ChronicHepatitis C+ [1]

Regulation-

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Structure/Sequence

Molecular FormulaC27H45N5O5

InChIKeyLHHCSNFAOIFYRV-DOVBMPENSA-N

CAS Registry394730-60-0

Objectives: 1) To evaluate la proportion of hepatitic C virus (HCV)-monoinfected patients who show sustained virologic response (SVR) to treatment including direct-acting antivirals (DAAs) in the clinical practice in clinical units that treat infectious diseases and 2) to determine the frequency of adverse events, including those that are severe and/or cause treatment interruption, in DAA-based therapy in this setting.
Design: Multicentric, prospective post-authorised cohort study. Setting: Hospitals of the Hepatitis Study Group (GEHEP) of the Spanish Society of Infectious Diseases and Microbiology (SEIMC).
Study population: HCV-monoinfected patients that initiate DAA-based treatment outside clinical trials.
Variables: The primary efficacy outcome variable is the proportion of patients who reach undetectable HCV-RNA 12 weeks after the scheduled end of therapy (SVR12). The primary safety outcome variable is the percentage of subjects who discontinue therapy due to adverse events.
Statistical analysis: A descriptive study will be performed, as well as a double sensibility analysis of the frequency of SVR12 using both an intention-to-treat and an on-treatment approach. Those variables that are associated with SVR12 with a p-value <0.2 will be included in a logistic regression analysis in which SVR12 will be the dependent variable.

Start Date01 Dec 2014

Sponsor / Collaborator

Hospital Universitario de Canarias

[+6]

NCT01641666

/ WithdrawnPhase 3

An Open-Label Study to Assess the Safety and Tolerability of Boceprevir in Combination With Peginterferon Alfa-2b Plus Ribavirin for Treatment of Vietnamese Subjects With Chronic Hepatitis C Genotype 1 Who Failed Prior Treatment With Any Interferon Plus Ribavirin in Vietnam

This study is designed to assess the safety and tolerability of boceprevir dosed 800 mg three times daily (TID) orally (PO) in combination with Peginterferon alfa-2b (PEG2b) 1.5 mcg/kg once a week (QW) administered subcutaneously (SC) plus ribavirin (RBV) (800 to 1400 mg/day) PO in Response Guided Therapy (RGT) in adult Vietnamese subjects with Chronic Hepatitis C, Genotype 1 (CHC GT1) who failed prior treatment with any interferon and ribavirin in Vietnam.

Start Date01 May 2014

Sponsor / Collaborator

Merck Sharp & Dohme Corp.

NCT02118597

/ TerminatedNot Applicable

Non-interventional Study to Observe Triple Combination Therapy With Boceprevir or Simeprevir Plus Peginterferon Alfa-2a Plus Ribavirin for Re-treatment of Chronic Hepatitis C in Hungary (IMPERIAL)

This prospective, national, multicenter, non-interventional study examined the use of triple combination therapy with boceprevir, pegylated interferon (peginterferon) alfa-2a and ribavirin in re-treating participants with genotype 1 chronic hepatitis C (CHC) infection. Dosing and treatment duration were at the discretion of the investigator in accordance with local clinical practice and local labeling. Participants were to be observed for the duration of their triple combination therapy and for up to 24 weeks thereafter.

Start Date01 May 2014

Sponsor / Collaborator

Hoffmann-La Roche, Inc.

100 Clinical Results associated with Boceprevir

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100 Translational Medicine associated with Boceprevir

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100 Patents (Medical) associated with Boceprevir

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1,507

Literatures (Medical) associated with Boceprevir

01 May 2025·Antiviral Research

Assessment of repurposed compounds against coronaviruses highlights the antiviral broad-spectrum activity of host-targeting iminosugars and confirms the activity of potent directly acting antivirals

Article

Author: Makower, Laetitia L ; Zitzmann, Nicole ; Rangel, Victor ; Alonzi, Dominic S ; Hill, Michelle L ; Kiappes, J L ; Dwek, Raymond A ; von Delft, Annette ; Gileadi, Carina ; Brun, Juliane ; Arman, Benediktus Yohan ; Witt, Karolina D

The COVID-19 pandemic highlights the need for novel antiviral drug discovery approaches that could dramatically shorten timelines from compound discovery to clinical development. At the beginning of the pandemic, repurposing approaches were at the forefront of early research efforts to screen for antiviral activity against SARS-CoV-2 in over 2500 compounds. Here, we report cellular screening results of 100 FDA-approved and experimental compounds against SARS-CoV-2 in the human Calu-3 cell line. We observed 13 compounds showing antiviral activity against SARS-CoV-2, including seven FDA-approved compounds (remdesivir, boceprevir, amiloride, nafamostat, cisplatin, silmitasertib, and miglustat), and six compounds in pre-clinical and clinical development (tarloxotinib, lucerastat (NB-DGJ), MON-DNJ, NAP-DNJ, NN-DGJ and NN-DNJ). Further, we observed that our screening hits include several host-targeting antivirals, namely iminosugars, that are largely non-toxic and offer a large therapeutic window. The most-developed iminosugar MON-DNJ (UV-4B), which has been evaluated in a Phase 1 clinical trial, shows antiviral activity against SARS-CoV-2 wild type as well as alpha, beta, gamma, delta, and Omicron variants. Its activity also extended to another betacoronavirus HCoV OC43, but not alphacoronavirus HCoV 229E. Our cellular screening results add to the body of knowledge on antivirals against coronaviruses and confirm the antiviral efficacy of iminosugars in cellular assays using the human lung-cell line Calu-3.

01 Feb 2025·Journal of Medical Virology

Systematic Reevaluation of Repurposed Drugs Against the Main Protease of SARS‐CoV‐2 via Combined Experiments

Article

Author: Zhou, Jiahao ; Xu, Tao ; Ye, Jiankai ; Chen, Yunyu ; Liu, Xiaoping ; Zhang, Rui

ABSTRACTThe main protease (Mpro) of SARS‐CoV‐2 is an attractive drug target for antivirals, as this enzyme plays a key role in virus replication. Drug repurposing is a promising option for the treatment of coronavirus disease 2019 (COVID‐19). Recently, a number of FDA‐approved drugs have been identified as Mpro inhibitors, but stringent hit validation is lacking. In this study, we rigorously reevaluated the in vitro inhibition of the Mpro enzyme by repurposed drugs via combined experiments, including the fluorescence resonance energy transfer (FRET) assay, fluorescence polarization (FP) assay, and protease biosensor cleavage assay. Our results from a set of in vitro assays revealed that boceprevir is a potential Mpro inhibitor, but other repurposed drugs, including atazanavir, dipyridamole, entrectinib, ethacridine, glecaprevir, hydroxychloroquine, ivermectin, meisoindigo, pelitinib, raloxifene, roxatidine acetate, saquinavir, teicoplanin, thonzonium bromide, and valacyclovir, are not. Our research highlights that the use of candidate Mpro inhibitors from primary screening warrants further comprehensive studies before the reporting of new findings.

01 Jan 2025·Journal of Biological Chemistry

The zymogenic form of SARS-CoV-2 main protease: A discrete target for drug discovery

Article

Author: Bach, Kathrin ; Stanchev, Stancho ; Günterová, Jana ; Zgarbová, Michala ; Humpolíčková, Jana ; Majerová, Taťána ; Majer, Pavel ; Stříšovský, Kvido ; Starková, Jana ; Konvalinka, Jan ; Weber, Jan ; Novotný, Pavel ; Nováková, Veronika ; Kryštůfek, Robin ; Hradilek, Martin ; Moravcová, Adéla

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (M^pro) autocatalytically releases itself out of the viral polyprotein to form a fully active mature dimer in a manner that is not fully understood. Here, we introduce several tools to help elucidate differences between cis (intramolecular) and trans (intermolecular) proteolytic processing and to evaluate inhibition of precursor M^pro. We found that many mutations at the P1 position of the N-terminal autoprocessing site do not block cis autoprocessing but do inhibit trans processing. Notably, substituting the WT glutamine at the P1 position with isoleucine retains M^pro in an unprocessed precursor form that can be purified and further studied. We also developed a cell-based reporter assay suitable for compound library screening and evaluation in HEK293T cells. This assay can detect both overall M^pro inhibition and the fraction of uncleaved precursor form of M^pro through separable fluorescent signals. We observed that inhibitory compounds preferentially block mature M^pro. Bofutrelvir and a novel compound designed in-house showed the lowest selectivity between precursor and mature M^pro, indicating that inhibition of both forms may be possible. Additionally, we observed positive modulation of precursor activity at low concentrations of inhibitors. Our findings help expand understanding of the SARS-CoV-2 viral life cycle and may facilitate development of strategies to target precursor form of M^pro for inhibition or premature activation of M^pro.

2

News (Medical) associated with Boceprevir

08 Feb 2023

·www.biospace.com

Infectious disease specialist Dr. Regis A. Vilchez is appointed CMO of MicuRx Pharmaceuticals, Inc.

SHANGHAI, Feb. 8, 2023 /PRNewswire/ -- Shanghai MicuRx Pharmaceutical Co., Ltd. ("MicuRx," 688373) announced recently that it has appointed Regis A. Vilchez, MD, PhD, an experienced R&D biopharmaceutical executive and infectious disease expert, as Chief Medical Officer of its American subsidiary, MicuRx Pharmaceuticals, Inc. He oversees new drug development programs and clinical activities in the United States, Europe and other regions. Dr. Vilchez earned an M.D. from the Universidad Autónoma de Centro América in Costa Rica and a Ph.D. from Baylor College of Medicine in Houston, Texas, the United States. He completed an internal medicine residency at Robert Wood Johnson Medical School, a clinical infectious diseases fellowship at the University of Pittsburgh, and a molecular virology fellowship at Baylor College of Medicine. Prior to entering the biopharmaceutical industry, Dr. Vilchez was full time faculty in the Departments of Medicine and Molecular Virology & Microbiology at Baylor College of Medicine. Dr. Vilchez has served in multiple R&D roles at Boehringer Ingelheim, Merck, Roche, Abbott/AbbVie, Mallinckrodt Pharmaceuticals and other smaller biotechnology companies. In those roles, Dr. Vilchez has been a key contributor to the global development of new therapies such as Vicriviroc, Victrelis, Viekirax, Technivie, Ocaliva, Terlivaz, and StrataGraft. Dr. Vilchez has co-authored more than 100 peer-reviewed scientific publications in high impact biomedical journals such as the New England Journal of Medicine, The Lancet, and Clinical Microbiology Reviews. The leadership of Dr. Vilchez will enhance MicuRx's global R&D programs and clinical activities. MicuRx is rapidly expanding its business and assembling an international expert team with extensive experience and an innovative spirit to develop a robust global R&D organization. Moving forward, MicuRx will remain focused on advancing its anti-infective product pipeline, and provide more effective and safer treatment options for patients around the world. View original content to download multimedia: SOURCE MicuRx Pharmaceuticals Company Codes: Shanghai:688373, Shanghai:688373.SS

Executive Change

01 Nov 2010

·www.biospace.com

Merck & Co., Inc.'s Investigational Medicine Boceprevir Achieved Significantly Higher SVR Rates In Treatment-Failure and Treatment-Naïve Adult Patients with Chronic Hepatitis C Genotype 1 Compared to Control

BOSTON--(BUSINESS WIRE)--Merck reported today that final results from two pivotal Phase III studies of boceprevir, its investigational oral hepatitis C protease inhibitor, demonstrated significantly higher sustained virologic response (SVR)1 rates in adult patients who previously failed treatment (treatment-failure; HCV RESPOND-2) and in adult patients who were new to treatment (treatment-naïve; HCV SPRINT-2) for chronic hepatitis C virus (HCV) genotype 1 compared to control, the primary objective of the studies. The results for the primary endpoints of these studies, which were first reported in a news release in August 20102, and a broad range of further data analyses from these studies are being presented in oral and poster presentations at the 61st Annual Meeting of the American Association for the Study of Liver Diseases (AASLD).

100 Deals associated with Boceprevir

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External Link

KEGG	Wiki	ATC	Drug Bank
D08876	Boceprevir	J05AP03	DB08873

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hepatitis C	Brazil	Merck GmbH	07 Sep 2011

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic hepatitis C genotype 1	Phase 2	-	Merck Sharp & Dohme Corp.	01 Aug 2008
Fibrosis	Preclinical	United States	Merck Sharp & Dohme Corp.	13 May 2011
Hepatitis C	Preclinical	United States	Merck Sharp & Dohme Corp.	13 May 2011
Hepatitis C, Chronic	Preclinical	United States	Merck Sharp & Dohme Corp.	13 May 2011
Anemia	Preclinical	-	Merck Sharp & Dohme Corp.	07 Dec 2009
Chronic hepatitis C genotype 1	Preclinical	-	Merck Sharp & Dohme Corp.	01 Aug 2008

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02060058 (BOLERO-CB, CTgov)	Phase 3	-	12	boceprevir+ribavirin (Patients With 32 Week Therapy)	ehtiekxcxp(decsniaxaj) = qknkyyksub rvxyryyxbr (ykqnlspalb, zvmvibusyl - ybivxdrwsd) View more	-	13 Mar 2018
				boceprevir+ribavirin (Patients With 48 Weeks Therapy)	vyyioraexx(cvnwdgcrkc) = obzifnigkp bkbhzyfzxi (krtqmbrslk, cplsdsttpx - fpbyfpunyw) View more
NCT01925183 (HIVCOBOC-RGT, CTgov)	Phase 4	HIV Infections \| Hepatitis C, Chronic	6	Pegylated interferon alpha-2a+Boceprevir+Ribavirin (28 Weeks of Treatment Duration)	zkeaqyhajx(fupgtpmuqf) = tyolxazsko esepscbrhy (baorsqjpwl, yhuphyoyeb - bukszzosaz) View more	-	09 Feb 2017
				Pegylated interferon alpha-2a+Boceprevir+Ribavirin (48 Weeks of Treatment Duration)	zkeaqyhajx(fupgtpmuqf) = tyipicasif esepscbrhy (baorsqjpwl, fweovpiqkd - zseepxtkmd) View more
NCT01945294 (3034-107, CTgov)	Phase 3	Chronic hepatitis C genotype 1	257	Boceprevir+Peg-interferon alfa-2b+Ribavirin (Arm 1: 16-week Treatment Arm)	dxbukhvruu(kiaxaqirsr) = myistdagdk fnihgbeijc (pexjthypou, wcvieohoqw - fiekkfjhgi) View more	-	23 Nov 2016
				Boceprevir+Peg-interferon alfa-2b+Ribavirin (Arm 2: 28-week Treatment Arm)	dxbukhvruu(kiaxaqirsr) = xmafmwdvwx fnihgbeijc (pexjthypou, xgovguaopo - gepxmekyzz) View more
NCT01756079 (3034-105, CTgov)	Phase 4	Chronic hepatitis C genotype 1 \| Fibrosis	58	boceprevir+RBV (Overall Participants)	mxoixdafew(mrmqvluxpq) = ttkipwrtpu uhjcxuegil (wupwhhzjgb, zasuqvcnim - iqeaqxluhb) View more	-	21 Nov 2016
				boceprevir+RBV (Overall Participants: Lead-in, Treatment and Follow-up)	bjsgxrlddy(xmykeunmww) = eposvkmsct dsxrtwrohk (sfsuifzxnx, ymneguxyhg - ublootsixj) View more
NCT01591460 (TriCo, Pubmed \| Infect Dis Ther) Manual	Phase 4	Hepatitis C	165	Peginterferon Alfa-2a+Ribavirin+Boceprevir	(lukihmcggw) = tsicyfrtyc ovyrpasnly (qkmoeapbmb, 74 - 86)	Positive	01 Jun 2016
NCT01544920 (P07755, CTgov)	Phase 3	Chronic hepatitis C genotype 1	737	peg-Interferon alfa-2a+Boceprevir+Ribavirin (Arm 1: Peg-IFN + RBV)	bamqjvrxcn(abgkaqevib) = rtniafdiyy piopvqvnfk (qptuirlgzh, rckxzlnotx - uquncysnzk) View more	-	30 May 2016
				peg-Interferon alfa-2a+Boceprevir+Ribavirin (Arm 2: BOC + Peg-IFN + RBV)	bamqjvrxcn(abgkaqevib) = lfbvbnmnor piopvqvnfk (qptuirlgzh, fvfsvawrpu - tytgmhktna) View more
NCT01912495 (DAHHS, Pubmed \| J Hepatol) Manual	Phase 2	HIV Infections \| Hepatitis C	127	ribavirin+peginterferon+boceprevir	(ajyttbbhft) = wpbqcbgydf ssbegzxnpx (goufshanym ) View more	Positive	01 Apr 2016
				ribavirin+peginterferon	(uysrmeemnr) = ejxkrtuihg vklskskngm (ivclhqmpdy )
NCT01912495 (DAHHS, CTgov)	Phase 2	Coinfection \| HIV Infections \| Hepatitis C	65	Peginterferon+Boceprevir+Ribavirin (Boceprevir, Peginterferon and Ribavirin)	rntrsoppec(tocjukdwym) = eadhnptlzu lismqceted (bkewmhazlf, chpwgthwkk - uwevfyvdlm) View more	-	01 Apr 2016
				Boceprevir Peginterferon+Ribavirin (Boceprevir Peginterferon Ribavirin)	ywoqjjzvzq(floporbzar) = ilisoewrrg rwdgphnylj (hdwbjcwwqj, hdkbkhjfth - aslolcvhdr)
NCT01335529 (BocepreVIH, Pubmed) Manual	Phase 2	HIV Infections \| Hepatitis C	64	ribavirin+PEGylated-interferonα2b+boceprevir	(tofjjuiyrm) = kymuawjthk qhlfcohnge (xqxqyvkiyn, 43 - 63) View more	Positive	01 Mar 2016
NCT01425203 (P08160, Pubmed \| World J Hepatol) Manual	Phase 3	Hepatitis C, Chronic	238	peginterferon+ribavirin+Boceprevir	(hysumtphon) = gsxocnjlwc ktwsdmkipy (ytuginjzdw )	Positive	28 Feb 2016
				peginterferon+ribavirin+Placebo	(hysumtphon) = hixaklkriz ktwsdmkipy (ytuginjzdw )