telaprevir
Trade name: incivek
Approved
May 23, 2011
Telaprevir (marketed under the brand names Incivek and Incivo) is a direct-acting antiviralagent against the hepatitis C virus (HCV). It is a hepatitis C virus NS3/4A protease inhibitor indicated for the treatment of genotype 1 chronic hepatitis C (CHC) in adult patients with compensated liver disease, including cirrhosis, who are treatment-naïve or who have been previously treated with interferon-based treatment, including prior null responders, partial responders, and relapsers in combination with peginterferon alfa and ribavirin. Telaprevir is not used as a monotherapy. It is necessary for the proteolytic cleavage of the HCV encoded polyprotein into mature forms of the NS4A, NS4B, NS5A and NS5B proteins and essential for viral replication. It belongs to the chemical class of alpha-ketoamids and binds to NS3/4A in a covalent but reversible manner. — NCATS
Clinical trial activity
86 trials · 42 clinical orgs · 2 marketing orgs
Earliest trial started Oct 1, 2005 (NCT00251199)
Timeline
Indications
Approved for
Studied for
- Acquired Immunodeficiency Syndrome · Phase 1
- Depression · Phase 2
- Drugs, Investigational · Phase 1
- Healthy Volunteers · Phase 1
- Hemophilia A · Phase 1
- Hepacivirus · Phase 3
- Hepatic Insufficiency · Phase 1
- Hepatitis C · Phase 4
- Hepatitis C, Chronic · Phase 4
- HIV · Phase 3
- HIV Infections · Phase 2
- Infections · Phase 3
- Kidney Diseases · Phase 1
- Liver Diseases · Phase 1
- Opioid-Related Disorders · Phase 1
- Thrombocytopenia · Phase 1
Mechanism of action
Hepatitis C virus serine protease, NS3/NS4A inhibitor
Approval history
- approvedPriority reviewMay 23, 2011
Chemistry & pharmacology
SMILES
CCC[C@H](NC(=O)[C@@H]1[C@H]2CCC[C@H]2CN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)C3=NC=CN=C3)C4CCCCC4)C(C)(C)C)C(=O)C(=O)NC5CC5- Mol. weight
- 679.8493 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaTelaprevir ↗
- NCATS655M5O3W0U ↗
- ChEMBLCHEMBL231813 ↗
Also known as
- (1s,3ar,6as)-(2s)-2-cyclohexyl-n-(pyrazinylcarbonyl)glycyl-3-methyl-l-valyl-n-((1s)-1-((cyclopropylamino)oxoacetyl)butyl)octahydrocyclopenta(c)pyrrole-1-carboxamide
- (1s,3ar,6as)-(2s)-2-cyclohexyl-n-(pyrazinylcarbonyl)glycyl-3-methyl-l-valyl-n-((1s)-1-((cyclopropylamino)oxoacetyl)butyl)octahydrocyclopenta(c)pyrrole-1-carboxamide
- incivek
- incivek
- incivek
- incivek
- incivek
- incivo
- incivo
- incivo
- mp-424
- mp-424
- mp-424
- telapravir
- telaprevir
- telaprevir
- telaprevir
- telaprevir
- telaprevir
- telaprevir
- telaprevir
- telaprevir
- telaprevir
- telaprevir
- telaprevir
- telaprevir
- telaprevir
- vrt-111950
- vrt-111950
- vx 950
- vx 950
- vx-950
- vx-950
- vx-950
- vx-950
- vx950 cpd
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02087111 | Phase 4 | Apr 1, 2014 | Johnson and Johnson, University of Leeds, University of London, University of Nottingham |
| NCT02006745 | Phase 3 | Jan 1, 2014 | St Stephens Aids Trust, University of London |
| NCT01994486 | Phase 2 | Dec 1, 2013 | University of Florida, Vertex |
| NCT01890772 | Phase 2/Phase 3 (Phase 3) | Aug 1, 2013 | Department of Veteran Affairs, Southern California Institute for Research and Education, Vertex |
| NCT01872936 | Phase 2 | Jun 1, 2013 | Santaris Pharma A/S |
| NCT01854528 | Phase 3 | Jun 1, 2013 | AbbVie |
| NCT01858961 | Phase 3 | May 1, 2013 | Boehringer Ingelheim |
| NCT01841502 | Phase 2 | May 1, 2013 | Janssen Pharmaceutica NV, Radboud University |
| NCT01821963 | Phase 3 | Apr 1, 2013 | University of Texas at Houston, Vertex |
| NCT01766115 | Phase 4 | Apr 1, 2013 | Harvard University |
| NCT01854697 | Phase 3 | Mar 1, 2013 | AbbVie |
| NCT01766167 | Phase 1 | Feb 1, 2013 | Mitsubishi Tanabe |
| NCT01786382 | Phase 1 | Feb 1, 2013 | Presidio Pharmaceuticals, Spaulding Clinical Research Inc. |
| NCT01718158 | Phase 3 | Jan 1, 2013 | Bristol-Myers Squibb |
| NCT01701063 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2013 | Janssen Pharmaceutica NV, Vertex |
| NCT01753557 | Phase 3 | Dec 1, 2012 | Mitsubishi Tanabe |
| NCT01704521 | Phase 1 | Dec 1, 2012 | Genentech, National Heart, Lung, and Blood Institute (NHLBI), University of Cincinnati, Vertex |
| NCT01753570 | Phase 3 | Dec 1, 2012 | Mitsubishi Tanabe, Toray Industries, Inc |
| NCT01818856 | Phase 1 | Dec 1, 2012 | Bristol-Myers Squibb, University of Seville |
| NCT01718145 | Phase 3 | Nov 1, 2012 | Bristol-Myers Squibb |
Organizations
Research & Development (42)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Vertex | For profit | 38 | 22 | 4 | 2005 |
| Tibotec | For profit | 19 | 12 | 3 | 2007 |
| Johnson and Johnson | For profit | 13 | 11 | 5 | 2010 |
| Mitsubishi Tanabe | For profit | 11 | 11 | 3 | 2007 |
| Janssen Pharmaceutica NV | For profit | 7 | 0 | 3 | 2010 |
| Toranomon Hospital | Academic/Hospital | 6 | 0 | 3 | 2007 |
| Bristol-Myers Squibb | For profit | 5 | 4 | 2 | 2012 |
| GlaxoSmithKline | For profit | 3 | 2 | 2 | 2012 |
| AbbVie | For profit | 2 | 2 | 1 | 2013 |
| Department of Veteran Affairs | Government | 2 | 1 | 2 | 2011 |
| Santaris Pharma A/S | For profit | 2 | 2 | 2 | 2012 |
| Spaulding Clinical Research Inc. | For profit | 2 | 0 | 1 | 2012 |
| University of Cincinnati | Academic/Hospital | 2 | 1 | 2 | 2008 |
| University of London | Academic/Hospital | 2 | 1 | 2 | 2014 |
| ViiV Healthcare | For profit | 2 | 2 | 1 | 2012 |
| Boehringer Ingelheim | For profit | 1 | 1 | 1 | 2013 |
| Cornell University | Academic/Hospital | 1 | 1 | 1 | 2009 |
| Croix-Rousse Hospital, Lyon | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Erasmus University Rotterdam | Academic/Hospital | 1 | 0 | 1 | 2008 |
| French National Agency for Research on AIDS and Viral Hepatitis | Government | 1 | 1 | 1 | 2011 |
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Vertex | For profit | NDA | May 23, 2011 |
| Watson Pharmaceuticals | For profit | NDA2 | May 23, 2011 |