simeprevir
Trade name: olysio
Small moleculeapprovedFast Track FDA
Approved
Nov 22, 2013
Simeprevir is a hepatitis C virus (HCV) NS3/4A protease inhibitor approved for the treatment of Chronic Hepatitis C (genotype 1 and 4). Inhibiting NS3/4A, simeprevir blocks viral replication. In in vitro assays simeprevir was potent against HCV genotype 1a and 1b. Simeprevir must not be administered as monotherapy and should only be prescribed with both peginterferon alfa and ribavirin. — NCATS
Clinical trial activity
118 trials · 44 clinical orgs · 1 marketing orgs
Phase 1
61
Phase 2
45
Phase 3
20
Phase 4
10
Earliest trial started Aug 1, 2005 (NCT02256735)
Timeline
2010s
- Jan 1, 2011
Johnson and Johnson — Earliest Phase 3 Sponsor(trial)
- Nov 22, 2013
Johnson and Johnson — Earliest FDA Approval
- Nov 22, 2013
Johnson and Johnson — NDA Secondary Org
- Nov 22, 2013
Johnson and Johnson — NDA Organization
Indications
Approved for
Studied for
- Arthritis, Rheumatoid · Phase 1
- Asthma · Phase 1
- Carcinoma, Hepatocellular · Phase 3
- Diarrhea · Phase 1
- Healthy Volunteers · Phase 4
- Hemorrhagic Fever, Ebola · Phase 1/Phase 2
- Hepacivirus · Phase 2
- Hepatitis B, Chronic · Phase 1
- Hepatitis C · Phase 4
- HIV-1 · Phase 1
- HIV Infections · Phase 4
- Hypertension · Phase 1
- Infections · Phase 3
- Infertility, Male · Phase 2/Phase 3
- Kidney Failure, Chronic · Phase 2
- Leukemia, Lymphocytic, Chronic, B-Cell · Phase 1
- Liver Cirrhosis · Phase 4
- Liver Diseases · Phase 2
- Liver Transplantation · Phase 4
- Pharmacokinetics · Phase 1
- Rifampin · Phase 1
- Tuberculosis · Phase 1
- Viruses · Phase 1
Mechanism of action
Hepatitis C virus serine protease, NS3/NS4A inhibitor
Approval history
- approvedPriority reviewFast trackNov 22, 2013
Chemistry & pharmacology
Loading structure…
SMILES
COc1ccc2c(O[C@@H]3C[C@H]4C(=O)N[C@]5(C(=O)NS(=O)(=O)C6CC6)C[C@H]5/C=C\CCCCN(C)C(=O)[C@@H]4C3)cc(-c3nc(C(C)C)cs3)nc2c1C- Mol. weight
- 749.96 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Black box warning
Sources
- ChEMBLCHEMBL501849 ↗
- WikipediaSimeprevir ↗
- NCATS9WS5RD66HZ ↗
- ChEMBLCHEMBL3137358 ↗
Also known as
- olysio
- olysio
- olysio
- olysio
- olysio
- olysio
- olysio
- simeprevir
- simeprevir
- simeprevir
- simeprevir
- simeprevir
- simeprevir
- simeprevir
- simeprevir
- simeprevir
- simeprevir sodium
- simeprevir sodium
- simeprevir sodium
- simeprevir sodium
- tmc435
- tmc435
- tmc-435
- tmc-435
- tmc-435
- tmc435350
- tmc435350
- tmc435350
- tmc435350
- tmc-435350
- tmc-435350
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05616598 | Phase 2/Phase 3 (Phase 3) | Mar 1, 2022 | Benha University |
| NCT03549832 | N/A | Jan 1, 2018 | Assiut University, Sohag University, South Valley University |
| NCT03277755 | Phase 1 | Sep 11, 2017 | Johnson and Johnson |
| NCT03155893 | Phase 1 | May 12, 2017 | Johnson and Johnson |
| NCT03099135 | Phase 3 | Apr 4, 2017 | Johnson and Johnson |
| NCT04387539 | Phase 1/Phase 2 (Phase 2) | Mar 1, 2017 | Beni Suef University |
| NCT03059303 | Phase 1 | Feb 20, 2017 | Johnson and Johnson |
| NCT02993250 | Phase 2 | Dec 21, 2016 | Janssen Pharmaceutica NV, Johnson and Johnson |
| NCT02992457 | Phase 4 | Dec 1, 2016 | Helwan University, Tanta University |
| NCT02932293 | Phase 2 | Dec 1, 2016 | Emory University, Humanity & Health Research Centre, People's Liberation Army of China, University of Maryland |
| NCT02945020 | Phase 1 | Nov 10, 2016 | Johnson and Johnson |
| NCT02765490 | Phase 2 | Nov 9, 2016 | Johnson and Johnson |
| NCT02885454 | Phase 1 | Aug 1, 2016 | Johnson and Johnson |
| NCT02824315 | Phase 1 | May 1, 2016 | Johnson and Johnson |
| NCT02771405 | Phase 3 | Mar 1, 2016 | Cairo University, National Hepatology & Tropical Medicine Research Institute |
| NCT02404805 | N/A | Feb 1, 2016 | University of Colorado, Denver |
| NCT02624063 | Phase 4 | Dec 1, 2015 | University of Sao Paulo |
| NCT02604992 | N/A | Nov 1, 2015 | Insys Therapeutics Inc |
| NCT02569710 | Phase 2 | Oct 31, 2015 | Alios BioPharma |
| NCT02485080 | Phase 4 | Sep 1, 2015 | Janssen Pharmaceutica NV, Stanford University, Yale University |
Showing 20 of 118 trials
Page 1 / 6
Organizations
Research & Development (44)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Johnson and Johnson | For profit | 48 | 45 | 3 | 2009 |
| Janssen Pharmaceutica NV | For profit | 31 | 0 | 4 | 2009 |
| Tibotec | For profit | 30 | 29 | 3 | 2007 |
| Pfizer | For profit | 12 | 12 | 2 | 2009 |
| Merck | For profit | 4 | 4 | 2 | 2010 |
| Ain Shams University | Academic/Hospital | 2 | 2 | 1 | 2014 |
| Alios BioPharma | For profit | 2 | 2 | 2 | 2015 |
| Beni Suef University | Academic/Hospital | 2 | 2 | 1 | 2015 |
| Emory University | Academic/Hospital | 2 | 0 | 1 | 2015 |
| Gilead Sciences | For profit | 2 | 1 | 2 | 2012 |
| Humanity & Health Research Centre | Academic/Hospital | 2 | 2 | 1 | 2015 |
| People's Liberation Army of China | Government | 2 | 0 | 1 | 2015 |
| University of Colorado, Denver | Academic/Hospital | 2 | 2 | 2 | 2015 |
| Achillion Pharmaceuticals | For profit | 1 | 0 | 1 | 2015 |
| Actelion | For profit | 1 | 1 | 1 | 2013 |
| Assiut University | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Azienda Ospedaliera San Camillo Forlanini | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Benha University | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Boehringer Ingelheim | For profit | 1 | 1 | 1 | 2005 |
| Bristol-Myers Squibb | For profit | 1 | 1 | 1 | 2012 |
44 organizations
Page 1 / 3
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Johnson and Johnson | For profit | NDA2 | Nov 22, 2013 |
| Johnson and Johnson | For profit | NDA | Nov 22, 2013 |