Elbasvir

drug
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Also known as Elbasvir component of zepatierMK-8742

Summary

Elbasvir (CHEMBL3039514) is an approved small-molecule antiviral drug (ATC J05AP10); indicated across 4 conditions including chronic hepatitis c virus infection and viral infectious disease.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: J05AP10
  • Indications: 4 conditions
  • Clinical trials: 43
  • Chemistry: 882 Da · C49H55N9O7

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3039514
NameElbasvir
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID71661251
ChEBICHEBI:132967
ATCJ05AP10
Molecular formulaC49H55N9O7
Molecular weight882
InChIKeyBVAZQCUMNICBAQ-PZHYSIFUSA-N

SMILES: CC(C)[C@@H](C(=O)N1CCC[C@H]1C2=NC=C(N2)C3=CC4=C(C=C3)N5[C@@H](OC6=C(C5=C4)C=CC(=C6)C7=CN=C(N7)[C@@H]8CCCN8C(=O)[C@H](C(C)C)NC(=O)OC)C9=CC=CC=C9)NC(=O)OC

IUPAC name: methyl N-[(2S)-1-[(2S)-2-[5-[(6S)-3-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]-6-phenyl-6H-indolo[1,2-c][1,3]benzoxazin-10-yl]-1H-imidazol-2-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamate

ChEBI definition: A complex organic heterotetracyclic compound that is a hepatitis C virus nonstructural protein 5A inhibitor used in combination with grazoprevir (under the brand name Zepatier) for treatment of chronic HCV genotypes 1 or 4 infection in adults.

Pharmacological roles (ChEBI): antiviral drug, hepatoprotective agent, hepatitis C virus nonstructural protein 5A inhibitor.

Also known as: Elbasvir, Elbasvir component of zepatier, MK-8742, ELBASVIR, elbasvir

Patent coverage: 343 distinct patent families (828 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 808 (98%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

4 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
chronic hepatitis C virus infection4MONDO:0005354EFO:0004220
viral infectious disease4MONDO:0005108EFO:0000763
hepatitis C virus infection3MONDO:0005231EFO:0003047
viral hepatitis1MONDO:0006011EFO:0004196

Clinical trials

Total trials: 43.

Phase distribution

PhaseTrials
PHASE310
PHASE210
PHASE49
Not specified8
PHASE2/PHASE33
PHASE13

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02902120PHASE4COMPLETEDHCV Treatment Immune Response With Grazoprevir/Elbasvir Before or After Renal Transplant
NCT02940691PHASE4TERMINATEDScale-up of Treatment of Hepatitis C Infection Among People Who Inject Drugs
NCT02945150PHASE4COMPLETEDPreemptive Treatment With Grazoprevir and Elbasvir for Donor HCV Positive to Recipient HCV Negative Kidney Transplant
NCT03022006PHASE4UNKNOWNSafety and Effect of Elbasvir/Grazoprevir Combination Therapy in Hemodialysis Patients With Chronic Hepatitis C
NCT03098121PHASE4COMPLETEDEfficacy and Tolerability of Grazoprevir and Elbasvir in Patients With Chronic Genotype 1 HCV and HIV Co-infection
NCT03105349PHASE4WITHDRAWNA Clinical Trial of 16 Weeks of Duration to Evaluate Retreatment With Elbasvir/Grazoprevir Plus Sofosbuvir and Ribavirin in Patients With Chronic Hepatitis C Genotypes 1,4 Who Have Failed to Treat With a Regime Based on an Inhibitor of the NS5A
NCT03359746PHASE4UNKNOWNGrazoprevir/Elbasvir for Treatment of Hepatitis C Virus Genotype 4 Post Kidney Transplant
NCT03585101PHASE4WITHDRAWNA Single-arm Evaluation of the Effect of HCV Treatment on Cardiovascular Disease Risk
NCT03823911PHASE4COMPLETEDCardiovascular Disease in HIV and Hepatitis C: Risk Outcomes After Hepatitis C Eradication
NCT02092350PHASE2/PHASE3COMPLETEDSafety and Efficacy of Grazoprevir (MK-5172) + Elbasvir (MK-8742) in Participants With Chronic Hepatitis C and Chronic Kidney Disease (MK-5172-052)
NCT02105701PHASE3COMPLETEDStudy of Efficacy and Safety of Grazoprevir (MK-5172) + Elbasvir (MK-8742) With or Without Ribavirin for Participants With Hepatitis C Genotype 1, 4, or 6 Infections Who Have Failed Prior Treatment With Pegylated Interferon + Ribavirin (MK-5172-068)
NCT02115321PHASE2/PHASE3COMPLETEDStudy of Efficacy and Safety of Grazoprevir (MK-5172) + Elbasvir (MK-8742) in Chronic Hepatitis C Participants With Child-Pugh (CP)-B Hepatic Insufficiency (MK-5172-059)
NCT02203149PHASE2/PHASE3COMPLETEDStudy of Grazoprevir (MK-5172) and Elbasvir (MK-8742) in Japanese Participants With Chronic Hepatitis C (MK-5172-058)
NCT02204475PHASE3WITHDRAWNGrazoprevir (MK-5172)/Elbasvir (MK-8742) Versus Boceprevir/Pegylated Interferon/Ribavarin for Chronic Hepatitis C Infection (MK-5172-066)
NCT02251990PHASE3COMPLETEDGrazoprevir (MK-5172) and Elbasvir (MK-8742) Combination in Treatment-Naïve Hepatitis C Virus Participants (MK-5172-067)
NCT02252016PHASE3COMPLETEDGrazoprevir (MK-5172) and Elbasvir (MK-8742) Combination for Chronic Hepatitis C Virus (HCV) Genotypes 1, 4, and 6 (MK-5172-065)
NCT02358044PHASE3COMPLETEDEfficacy and Safety of Combination Grazoprevir (MK-5172)/Elbasvir (MK-8742) Versus Sofosbuvir + Pegylated Interferon + Ribavirin in Hepatitis C Virus Genotype 1, 4 or 6 Infection (MK-5172-077)
NCT02600325PHASE3COMPLETEDDutch Acute HCV in HIV Study (DAHHS-2): Grazoprevir/Elbasvir for Acute HCV
NCT02890719PHASE3WITHDRAWNPilot Study Evaluate Efficacy of Grazoprevir + Elbasvir for 12 or 16 Weeks in Liver Transplant Recipients.
NCT02897596PHASE3UNKNOWNEfficacy of GZR/EBR in Early Chronic Hepatitis C in HIV/HCV Co-infected Patients
NCT02973503PHASE3COMPLETEDStudy to Investigate the Efficacy of Elbasvir/Grazoprevir Fixed-Dose Combination for 8 Weeks in Treatment-Naïve, HCV GT1b-Infected Patients, With Non-severe Fibrosis
NCT04546802PHASE3WITHDRAWNHepATocellular Cancer Hcv Therapy Study
NCT01717326PHASE2COMPLETEDA Study of the Combination Regimen Grazoprevir (MK-5172) and Elbasvir (MK-8742) ± Ribavirin in Participants With Chronic Hepatitis C (MK-5172-035)
NCT01932762PHASE2COMPLETEDEfficacy and Safety of Combination Grazoprevir (MK-5172) + Elbasvir (MK-8742) + Ribavirin (RBV) in Genotype 2 Hepatitis C Infection (MK-5172-047)
NCT02105454PHASE2COMPLETEDStudy of Grazoprevir (MK-5172) + Elbasvir (MK-8742) + Ribavirin in Participants With Chronic Hepatitis C Who Failed Prior Direct-Acting Antiviral Therapy (MK-5172-048)
NCT02332707PHASE2COMPLETEDEfficacy and Safety of Grazoprevir (MK-5172) and Uprifosbuvir (MK-3682) With Elbasvir (MK-8742) or Ruzasvir (MK-8408) for Chronic Hepatitis C Genotype (GT)1 and GT2 Infection (MK-3682-011)
NCT02332720PHASE2COMPLETEDEfficacy and Safety of Grazoprevir (MK-5172) and Uprifosbuvir (MK-3682) With Elbasvir (MK-8742) or Ruzasvir (MK-8408) for Chronic Hepatitis C Virus (HCV) Genotype (GT) 3, GT4, GT5, and GT6 Infection (MK-3682-012)
NCT02601573PHASE2COMPLETEDElbasvir/Grazoprevir (EBR/GZR) and Sofosbuvir (SOF) With and Without Ribavirin (RBV) in Cirrhotic Subjects With Chronic Hepatitis C Virus (HCV) Genotype 3 (GT3) Infection (MK-5172-083)
NCT02647632PHASE2COMPLETEDStudy to Assess Efficacy and Safety of Grazoprevir/Elbasvir Associated With Sofosbuvir and Ribavirin in HCV Genotype 1 or 4-infected Patients Who Failed Direct Acting Antivirals (DAA) Bitherapy With Sofosbuvir
NCT02886624PHASE2COMPLETEDShort Duration Therapy of Acute Hepatitis C Genotypes 1 or 4
NCT02940496PHASE2COMPLETEDPembrolizumab (MK-3475) in Hepatocellular Carcinoma
NCT03379506PHASE2COMPLETEDElbasvir (EBR)/Grazoprevir (GZR) in Pediatric Participants With Chronic Hepatitis C Infection (MK-5172-079)
NCT01532973PHASE1COMPLETEDSafety, Pharmacokinetics and Pharmacodynamics of Elbasvir (MK-8742) in Hepatitis C Infected Males (MK-8742-002)
NCT01797536PHASE1COMPLETEDThe Influence of Hepatic Insufficiency on the Pharmacokinetics of Elbasvir (MK-8742) (MK-8742-009)
NCT01937975PHASE1COMPLETEDThe Pharmacokinetics of Grazoprevir (MK-5172) and Elbasvir (MK-8742) in Participants With Renal Insufficiency (MK-5172-050)
NCT02333292Not specifiedCOMPLETEDEfficacy and Safety of Therapy Against HCV Based on Direct-acting Antivirals in Real-life Conditions
NCT03110055Not specifiedUNKNOWNthe Effect of Grazoprevir/Elbasvir and TACE vs. TACE Alone in Prolonging Survival of Patients With Non-resectable HCV Associated HCC.
NCT03145623Not specifiedCOMPLETEDRetrospective Efficacy and Safety Study With Elbasvir/Grazoprevir in HCV-infected Patients With Chronic Kidney Disease
NCT03407703Not specifiedUNKNOWNHepatitis C (HCV) Cure and Kidney Health
NCT03433326Not specifiedUNKNOWNGrazoprevir and Elbasvir Without Ribavirin for 12 Weeks in Patients With HCV-related Cryoglobulinemic Nephropathy

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).