ombitasvir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antivirals, hepatitis C Virus (HCV) NS5A inhibitors 4912 1258226-87-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ombitasvir hydrate
  • ombitasvir heminonahydrate
  • ombitasvir
  • ABT-267
inhibits HCV NS5A protein
  • Molecular weight: 894.13
  • Formula: C50H67N7O8
  • CLOGP: 8.39
  • LIPINSKI: 3
  • HAC: 15
  • HDO: 4
  • TPSA: 178.72
  • ALOGS: -5.67
  • ROTB: 16
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 2.32 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.68 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 28.49 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.917 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 67.920 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.119 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 8.690 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 0.160 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 0.330 % High 1
herg hERG pIC50 4.653 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 4.498 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 15.885 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.300 % High 1
kinase-safety-class EIF2AK3,GRK2,ITK,PDK1,PDK2,PDK4 6
kinase-selectivity-class GRK2,PDK1 2
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 18.239 High 1
mh-clint Mouse hepatocyte intrinsic clearance 10.304 High 1
mppb Mouse plasma protein binding (% unbound) 0.140 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 56.624 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 0.100 % High 1
rh-clint Rat hepatocyte intrinsic clearance 4.667 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 0.440 % High 1
rppb Rat plasma protein binding (% unbound) 0.210 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 2.729 uM High 1

Approvals:

DateAgencyCompanyOrphan
Dec. 19, 2014 FDA ABBVIE INC
Nov. 20, 2014 EMA AbbVie Ltd

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug interaction 101.71 58.95 50 378 266949 42353958
Erosive duodenitis 59.75 58.95 11 417 1778 42619129

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug interaction 163.09 56.55 71 567 500112 110088549
Drug level increased 66.30 56.55 20 618 47699 110540962
Erosive duodenitis 63.07 56.55 11 627 2280 110586381

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AP52 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
ATC J05AP53 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
FDA EPC N0000191256 Hepatitis C Virus NS5A Inhibitor
FDA MoA N0000191272 UGT1A1 Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:36044 antiviral drug
CHEBI has role CHEBI:64951 anti-HBV agent
CHEBI has role CHEBI:85185 hepatitis C virus nonstructural protein 5A inhibitor

Related Drugs by ATC class:

J05AP Antivirals for treatment of HCV infections 18 drugs
asunaprevirbeclabuvirboceprevirdaclatasvirdasabuvirelbasvirglecaprevirgrazoprevirledipasvirparitaprevirpibrentasvirribavirin show all 18 →

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Chronic hepatitis C indication 128302006




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.81 acidic
pKa2 4.5 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 8501238 Sept. 17, 2028 USE OF DASABUVIR TO INHIBIT VIRAL REPLICATION FOR THE TREATMENT OF HCV INFECTION.
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 9139536 Nov. 9, 2028 TREATMENT OF HCV INFECTION USING DASABUVIR
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 8188104 May 17, 2029 USE OF DASABUVIR TO INHIBIT VIRAL REPLICATION FOR THE TREATMENT OF HCV INFECTION.
12.5MG;75MG;50MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** TECHNIVIE ABBVIE N207931 July 24, 2015 DISCN TABLET ORAL 8642538 Sept. 10, 2029 TREATMENT OF HCV INFECTION USING PARITAPREVIR
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 8642538 Sept. 10, 2029 TREATMENT OF HCV INFECTION USING PARITAPREVIR
12.5MG;75MG;50MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** TECHNIVIE ABBVIE N207931 July 24, 2015 DISCN TABLET ORAL 9006387 June 10, 2030 TREATMENT OF HCV INFECTION USING OMBITASVIR
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 9006387 June 10, 2030 TREATMENT OF HCV INFECTION USING OMBITASVIR
12.5MG;75MG;50MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** TECHNIVIE ABBVIE N207931 July 24, 2015 DISCN TABLET ORAL 9044480 April 10, 2031 TREATMENT OF HCV INFECTION USING PARITAPREVIR
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 9044480 April 10, 2031 TREATMENT OF HCV INFECTION USING PARITAPREVIR
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 10201584 May 17, 2032 TREATMENT OF HCV INFECTION USING DASABUVIR/OMBITASVIR/PARITAPREVIR/RITONAVIR FIXED DOSE COMBINATION
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 8466159 Sept. 4, 2032 TREATMENT OF HCV INFECTION USING PARITAPREVIR, OMBITASVIR, RITONAVIR, AND DASABUVIR WITH RIBAVIRIN.
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 8492386 Sept. 4, 2032 TREATMENT OF HCV INFECTION USING PARITAPREVIR, OMBITASVIR, RITONAVIR, AND DASABUVIR, WITHOUT RIBAVIRIN
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 8680106 Sept. 4, 2032 TREATMENT OF HCV INFECTION USING PARITAPREVIR, OMBITASVIR, RITONAVIR, AND DASABUVIR WITH RIBAVIRIN.
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 8685984 Sept. 4, 2032 TREATMENT OF HCV INFECTION USING PARITAPREVIR, OMBITASVIR, RITONAVIR, AND DASABUVIR, WITHOUT RIBAVIRIN
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 10105365 Jan. 2, 2035 TREATMENT OF HCV INFECTION USING DASABUVIR/OMBITASVIR/PARITAPREVIR/RITONAVIR FIXED DOSE COMBINATION
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 9333204 Jan. 2, 2035 TREATMENT OF HCV INFECTION USING DASABUVIR/OMBITASVIR/PARITAPREVIR/RITONAVIR FIXED DOSE COMBINATION
EQ 200MG BASE;8.33MG;50MG;33.33MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** VIEKIRA XR ABBVIE N208624 July 22, 2016 DISCN TABLET, EXTENDED RELEASE ORAL 9744170 Jan. 2, 2035 TREATMENT OF HCV INFECTION USING DASABUVIR/OMBITASVIR/PARITAPREVIR/RITONAVIR FIXED DOSE COMBINATION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Genome polyprotein Polyprotein INHIBITOR EC50 11.30 SCIENTIFIC LITERATURE DRUG LABEL
Genome polyprotein Polyprotein INHIBITOR EC50 10.85 SCIENTIFIC LITERATURE DRUG LABEL
Nonstructural protein 5A Unclassified EC50 10.85 CHEMBL
Genome polyprotein [Cleaved into: Core protein p21 Enzyme EC50 10.92 CHEMBL

External reference:

IDSource
D10576 KEGG_DRUG
1456607-70-7 SECONDARY_CAS_RN
4034026 VANDF
CHEBI:85183 CHEBI
CHEMBL3127326 ChEMBL_ID
C586094 MESH_SUPPLEMENTAL_RECORD_UI
11272 IUPHAR_LIGAND_ID
DB09296 DRUGBANK_ID
1597371 RXNORM
30776 MMSL
d08320 MMSL
015825 NDDF
713479007 SNOMEDCT_US
714429000 SNOMEDCT_US
C3852670 UMLSCUI
9740 INN_ID
54767916 PUBCHEM_CID
2302768XJ8 UNII

Pharmaceutical products:

None