boceprevir
Trade name: victrelis
Approved
May 13, 2011
Boceprevir (trade name Victrelis) is first-generation, selective, small molecule inhibitor of the non-structural serine protease (NS3) and NS4A polypeptide complex (NS3/NS4A) and is a direct acting antiviral drug against the hepatitis C virus. It is indicated the treatment of chronic hepatitis C (CHC) genotype 1 infection, in combination with peginterferon alfa and ribavirin, in adult patients (18 years of age and older) with compensated liver disease, including cirrhosis, who are previously untreated or who have failed previous interferon and ribavirin therapy. Boceprevir is not approved as a monotherapy. Upon administration, boceprevir reversibly binds to the active center of the HCV NS3/NS4A and prevents NS3/NS4A protease-mediated polyprotein maturation. This disrupts the processing of viral proteins and the formation of a viral replication complex, which inhibits viral replication in HCV genotrype 1-infected host cells. NS3, a serine protease, is essential for the proteolytic cleavages within the HCV polyprotein and plays a key role during HCV viral RNA replication. NS4A is an activating factor for NS3. — NCATS
Clinical trial activity
52 trials · 48 clinical orgs · 1 marketing orgs
Earliest trial started Sep 1, 2005 (NCT00160251)
Timeline
Indications
Approved for
Studied for
- Coinfection · Phase 3
- Healthy Volunteers · Phase 1/Phase 2
- Hepacivirus · Phase 2/Phase 3
- Hepatitis · Phase 4
- Hepatitis C · Phase 4
- HIV · Phase 4
- HIV Infections · Phase 4
- Kidney Failure, Chronic · Phase 4
- Liver Cirrhosis, Experimental · Phase 2
- Liver Transplantation · Phase 3
- Menopause · Phase 3
- Stomach Diseases · Phase 1
- Thrombocytopenia · Phase 1
Mechanism of action
Hepatitis C virus serine protease, NS3/NS4A inhibitor
Approval history
- approvedPriority reviewMay 13, 2011
Chemistry & pharmacology
SMILES
CC(C)(C)NC(=O)N[C@H](C(=O)N1C[C@H]2[C@@H]([C@H]1C(=O)NC(CC3CCC3)C(=O)C(N)=O)C2(C)C)C(C)(C)C- Mol. weight
- 519.6767 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaBoceprevir ↗
- NCATS89BT58KELH ↗
- ChEMBLCHEMBL218394 ↗
Also known as
- beceprevir
- boceprevir
- boceprevir
- boceprevir
- boceprevir
- boceprevir
- boceprevir
- boceprevir
- boceprevir
- boceprevir
- boceprevir
- boceprevir
- boceprevir
- n-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide
- sch503034
- sch 503034
- sch 503034
- sch-503034
- sch-503034
- sch-503034
- victrelis
- victrelis
- victrelis
- victrelis
- victrelis
- victrelis
- victrellis
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02204475 | Phase 3 | Nov 1, 2014 | Merck |
| NCT01641666 | Phase 3 | May 1, 2014 | Merck |
| NCT01770223 | Phase 4 | Jan 1, 2014 | Merck |
| NCT02160080 | Phase 3 | Jan 1, 2014 | Chang Gung University |
| NCT01653236 | Phase 3 | Dec 1, 2013 | Cairo University |
| NCT02060058 | Phase 3 | Nov 1, 2013 | Kaohsiung Medical University, National Taiwan University |
| NCT01945294 | Phase 3 | Oct 1, 2013 | Merck |
| NCT01949168 | Phase 2 | Sep 1, 2013 | Merck, University of New South Wales |
| NCT01912495 | Phase 2 | Aug 1, 2013 | Erasmus University Rotterdam, Maastricht University, Onze Lieve Vrouw Hospital, Radboud University, Rijnstate Hospital, Slotervaart Hospital, University of Amsterdam, University of Groningen, Utrecht University |
| NCT01925183 | Phase 4 | Aug 1, 2013 | Medical University of Vienna, University of Vienna |
| NCT01909401 | Early Phase 1 (Phase 1) | Jun 1, 2013 | Indiana University, Merck |
| NCT02112630 | N/A | May 1, 2013 | Columbia University, Merck |
| NCT01718301 | Phase 3 | Mar 1, 2013 | University of Barcelona |
| NCT01756079 | Phase 4 | Feb 1, 2013 | Merck |
| NCT01590225 | Phase 3 | Jan 1, 2013 | Merck |
| NCT01731301 | Phase 4 | Jan 1, 2013 | Chronic Liver Disease Foundation, Liver Institute of Virginia, Merck |
| NCT01499498 | Phase 1 | Dec 1, 2012 | University of London |
| NCT01663922 | Phase 1 | Aug 1, 2012 | St Stephens Aids Trust, University of Liverpool, University of Turin |
| NCT01591460 | Phase 4 | Aug 1, 2012 | Roche |
| NCT01657552 | Phase 1 | Aug 1, 2012 | GlaxoSmithKline |
Organizations
Research & Development (48)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Merck | For profit | 32 | 22 | 5 | 2005 |
| Radboud University | Academic/Hospital | 3 | 2 | 2 | 2011 |
| French National Agency for Research on AIDS and Viral Hepatitis | Government | 2 | 2 | 1 | 2011 |
| GlaxoSmithKline | For profit | 2 | 1 | 1 | 2012 |
| National Institute of Allergy and Infectious Diseases (NIAID) | Government | 2 | 2 | 2 | 2011 |
| Roche | For profit | 2 | 2 | 2 | 2011 |
| ViiV Healthcare | For profit | 2 | 2 | 1 | 2012 |
| Aix-University of Marseille | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Bristol-Myers Squibb | For profit | 1 | 1 | 1 | 2011 |
| Cairo University | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Chang Gung University | Academic/Hospital | 1 | 1 | 1 | 2014 |
| Chronic Liver Disease Foundation | Academic/Hospital | 1 | 0 | 1 | 2013 |
| Columbia University | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Debiopharm | For profit | 1 | 1 | 1 | 2011 |
| Department of Veteran Affairs | Government | 1 | 1 | 1 | 2011 |
| Erasmus University Rotterdam | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Hopital Paul Brousse | Academic/Hospital | 1 | 0 | 1 | 2012 |
| Indiana University | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Kaohsiung Medical University | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Liver Institute of Virginia | Academic/Hospital | 1 | 1 | 1 | 2013 |
Marketing (1)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Merck | For profit | NDA | May 13, 2011 |