grazoprevir (zepatier) Report issue

Small molecule Approved FDA Priority Review FDA
AACT ChEMBL DrugBank Drug Central KEGG MeSH PubChem repoDB

Active Ingredient History

NOW
  • Now
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

Chemistry

  • SMILES: COc1ccc2nc3CCCCC[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)Oc3nc2c1)C(C)(C)C
  • InChIKey: OBMNJSNZOWALQB-NCQNOWPTSA-N
  • Mol. Mass: 766.92
  • ALogP: 3.3
  • ChEMBL Molecules:
    grazoprevir  
    grazoprevir  
More Chemistry

Pharmacology

Combination drugs

( elbasvir, grazoprevir (zepatier) )

Alternative names

(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 anhydrous | grazoprevir hydrate | mk5172 | mk 5172 | mk-5172 | zepatier

Organizations (55)

Research & Development (55)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (1)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (22)

Approved Indications (2)


 

Hepatitis C (approved 2016)

Hepatitis C, Chronic

Experimental Indications - Clinical Trial Phases 1-4 (22)


 

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)

Hepatitis C, Chronic ()

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)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 73
  • # of Trial Organizations: 55

Trials by Phase

Trial Phase Start Date Organizations Indications

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