Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C38H50N6O9S |
Molecular Weight | 766.903 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 7 / 7 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=NC3=C(CCCCC[C@@H]4C[C@H]4OC(=O)N[C@H](C(=O)N5C[C@@H](C[C@H]5C(=O)N[C@@]6(C[C@H]6C=C)C(=O)NS(=O)(=O)C7CC7)O3)C(C)(C)C)N=C2C=C1
InChI
InChIKey=OBMNJSNZOWALQB-NCQNOWPTSA-N
InChI=1S/C38H50N6O9S/c1-6-22-19-38(22,35(47)43-54(49,50)25-13-14-25)42-32(45)29-18-24-20-44(29)34(46)31(37(2,3)4)41-36(48)53-30-16-21(30)10-8-7-9-11-27-33(52-24)40-28-17-23(51-5)12-15-26(28)39-27/h6,12,15,17,21-22,24-25,29-31H,1,7-11,13-14,16,18-20H2,2-5H3,(H,41,48)(H,42,45)(H,43,47)/t21-,22-,24-,29+,30-,31-,38-/m1/s1
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.
CNS Activity
Originator
Approval Year
PMID
Title | Date | PMID |
---|---|---|
Identification of the E5 open reading frame of human papillomavirus type 16. | 1988 Mar |
|
Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor. | 2012 Apr 12 |
|
MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants. | 2012 Aug |
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Grazoprevir and Elbasvir in Patients with Genotype 1 Hepatitis C Virus Infection: A Comprehensive Efficacy and Safety Analysis. | 2017 |
|
Unraveling the structural basis of grazoprevir potency against clinically relevant substitutions in hepatitis C virus NS3/4A protease from genotype 1a. | 2017 Apr 14 |
|
Elbasvir/grazoprevir. | 2017 Feb |
|
Elbasvir/Grazoprevir (Zepatier) for Hepatitis C Virus Infection. | 2017 Mar 15 |
|
Elbasvir/Grazoprevir: A Review in Chronic HCV Genotypes 1 and 4. | 2017 May |
|
Elbasvir/grazoprevir does not worsen renal function in patients with hepatitis C virus infection and pre-existing renal disease. | 2017 Nov |
|
Elbasvir/Grazoprevir for Patients With Hepatitis C Virus Infection and Inherited Blood Disorders: A Phase III Study. | 2017 Sep |
|
Elbasvir/Grazoprevir Use in Postliver Transplantation Patients on Hemodialysis. | 2017 Sep |
Patent
Sample Use Guides
ZEPATIER is a two-drug, fixed-dose combination product containing 50 mg of elbasvir and 100 mg of grazoprevir in a single tablet. The recommended dosage of ZEPATIER is one tablet taken orally once daily with or without food
Route of Administration:
Oral
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Code System | Code | Type | Description | ||
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1350514-68-9
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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PRIMARY | |||
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N0000190114
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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PRIMARY | Cytochrome P450 3A Inhibitors [MoA] | ||
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9857
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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PRIMARY | |||
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SUB174126
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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PRIMARY | |||
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1206524-75-5
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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SUPERSEDED | |||
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1871173
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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PRIMARY | |||
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1356446-42-8
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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SUPERSEDED | |||
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N0000182638
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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PRIMARY | HCV NS3/4A Protease Inhibitors [MoA] | ||
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1350514-68-9
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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PRIMARY | |||
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44603531
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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PRIMARY | SWITZERF | ||
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N0000190113
Created by
admin on Tue Mar 06 11:10:32 UTC 2018 , Edited by admin on Tue Mar 06 11:10:32 UTC 2018
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PRIMARY | Breast Cancer Resistance Protein Inhibitors [MoA] |
ACTIVE MOIETY