grazoprevir
Trade name: zepatier
Approved
Jan 28, 2016
Grazoprevir is a second generation NS3/4A protease inhibitor approved in the EU and the USA for the treatment of hepatitis C virus (HCV) genotypes 1 and 4 infections in adult patients in combination with elbasvir (C virus (HCV) NS5A inhibitor) as the fixed-dose combination product Zepatier with or without ribavirin. In phase III trials, 12 or 16 weeks of treatment with once-daily elbasvir/grazoprevir (fixed-dose tablet or as individual agents), taken with or without ribavirin, generally provided high rates of sustained virological response at 12 weeks (SVR12) in treatment-naive and -experienced adult patients with chronic HCV genotype 1a, 1b or 4 infection, including those with or without compensated cirrhosis, HIV co-infection, inherited blood disorders or chronic kidney disease or patients receiving opioid agonist therapy or of Japanese origin. Elbasvir/grazoprevir was generally well tolerated. Thus, elbasvir/grazoprevir, with or without ribavirin, represents an effective new option for the treatment of adults with chronic HCV genotype 1 and 4 infection, including a number of difficult-to-treat populations. — NCATS
Clinical trial activity
73 trials · 56 clinical orgs · 1 marketing orgs
Earliest trial started Feb 1, 2010 (NCT00998985)
Timeline
Indications
Approved for
Studied for
- Carcinoma, Hepatocellular · Phase 3
- Cardiovascular Diseases · Phase 4
- Chronic Kidney Disease-Mineral and Bone Disorder · Phase 4
- Cross Infection · Phase 4
- Deglutition Disorders · Phase 1
- Heart Failure · Phase 1/Phase 2
- Heart Transplantation · Phase 4
- Hepacivirus · Phase 2/Phase 3
- Hepatitis C · Phase 4
- HIV · Phase 4
- Kidney Failure, Chronic · Phase 4
- Kidney Transplantation · Phase 4
- Liver Cirrhosis · Phase 3
- Liver Transplantation · Phase 4
- Lung Diseases · Phase 1/Phase 2
- Metabolic Syndrome · Phase 3
- Renal Dialysis · Phase 4
- Renal Insufficiency · Phase 4
- Renal Insufficiency, Chronic · Phase 4
- Substance Abuse, Intravenous · Phase 4
- Substance-Related Disorders · Phase 4
Mechanism of action
Hepatitis C virus serine protease, NS3/NS4A inhibitor
Combination products
zepatier
with elbasvir
Also known as elbasvir and grazoprevir
Approval history
- approvedPriority reviewBreakthroughJan 28, 2016
Chemistry & pharmacology
SMILES
C=C[C@@H]1C[C@]1(NC(=O)[C@@H]1C[C@@H]2CN1C(=O)[C@H](C(C)(C)C)NC(=O)O[C@@H]1C[C@H]1CCCCCc1nc3ccc(OC)cc3nc1O2)C(=O)NS(=O)(=O)C1CC1- Mol. weight
- 766.92 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL2063090 ↗
- WikipediaGrazoprevir ↗
- NCATS8YE81R1X1J ↗
- ChEMBLCHEMBL3039533 ↗
Also known as
- (1ar,5s,8s,10r,22ar)-5-tert-butyl-n-{(1r,2s)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethenylcyclopropyl}-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8h-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
- (1ar,5s,8s,10r,22ar)-5-tert-butyl-n-{(1r,2s)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethenylcyclopropyl}-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8h-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
- elbasvir / grazoprevir
- elbasvir grazoprevir drug combination
- elbasvir-grazoprevir drug combination
- elbasvir, grazoprevir drug combination
- grazoprevir
- grazoprevir
- grazoprevir
- grazoprevir
- grazoprevir
- grazoprevir
- grazoprevir
- grazoprevir
- grazoprevir
- grazoprevir
- grazoprevir anhydrous
- grazoprevir anhydrous
- grazoprevir anhydrous
- grazoprevir hydrate
- grazoprevir hydrate
- grazoprevir hydrate
- mk5172
- mk5172
- mk5172
- mk 5172
- mk-5172
- mk-5172
- mk-5172
- mk-5172
- zepatier
- zepatier
- zepatier
- zepatier
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04546802 | Phase 3 | Sep 30, 2019 | Merck, Monash University, University of Melbourne |
| NCT03797066 | Phase 4 | Apr 30, 2019 | Hepatitis C Trust, Merck, University of London |
| NCT03817619 | Phase 1 | Mar 28, 2019 | Radboud University |
| NCT03723824 | Phase 4 | Feb 14, 2019 | Taichung Veterans General Hospital |
| NCT03791814 | Phase 4 | Jan 31, 2019 | Davita Clinical Research, Merck, Yeshiva University |
| NCT03724149 | Phase 1/Phase 2 (Phase 2) | Dec 12, 2018 | Merck, University of Pennsylvania |
| NCT03365635 | Phase 4 | Dec 1, 2018 | Merck, University of Pennsylvania |
| NCT03381859 | Phase 4 | Dec 1, 2018 | Cairo University, Merck, University of Maryland |
| NCT03823911 | Phase 4 | Nov 18, 2018 | Merck, National Institutes of Health (NIH), University of Maryland |
| NCT03585101 | Phase 4 | Aug 31, 2018 | Merck, University of California, Los Angeles |
| NCT03578640 | Phase 3 | Jul 1, 2018 | King Fahad Medical City |
| NCT03420300 | Phase 4 | Jun 5, 2018 | National Taiwan University |
| NCT03496233 | Phase 3 | Apr 30, 2018 | University of Palermo |
| NCT03379506 | Phase 2 | Jan 25, 2018 | Merck |
| NCT03236506 | Phase 2 | Jan 19, 2018 | University of Dundee |
| NCT03359746 | Phase 4 | Dec 15, 2017 | King Faisal University, Merck |
| NCT03143998 | Phase 4 | Nov 29, 2017 | Merck |
| NCT03222167 | Phase 3 | Oct 31, 2017 | Institute Of Cardiology & Internal Diseases, Kazakhstan, Merck, Synergy Research |
| NCT03221582 | Phase 4 | Aug 28, 2017 | Department of Veteran Affairs, Merck |
| NCT03249194 | Early Phase 1 (Phase 1) | Aug 17, 2017 | Virginia Commonwealth University |