pibrentasvir Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antivirals, hepatitis C Virus (HCV) NS5A inhibitors 5244 1353900-92-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pibrentasvir
  • ABT-530
  • A-1325912.0
Pibrentasvir is an inhibitor of HCV NS5A, which is essential for viral RNA replication and virion assembly. The mechanism of action of pibrentasvir has been characterized based on cell culture antiviral activity and drug resistance mapping studies.
  • Molecular weight: 1113.20
  • Formula: C57H65F5N10O8
  • CLOGP: 7.20
  • LIPINSKI: 3
  • HAC: 18
  • HDO: 4
  • TPSA: 199.58
  • ALOGS: -5.30
  • ROTB: 17

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 26, 2017 EMA AbbVie Deutschland GmbH & Co. KG
Aug. 3, 2017 FDA ABBVIE INC

FDA Adverse Event Reporting System (Female)

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
Headache 977.12 32.60 630 4883 477722 46202827
Fatigue 971.84 32.60 687 4826 608010 46072539
Pruritus 471.87 32.60 313 5200 242039 46438510
Nausea 317.13 32.60 393 5120 687061 45993488
Blood bilirubin increased 95.56 32.60 56 5457 34128 46646421
Product dose omission issue 86.87 32.60 103 5410 168417 46512132
Therapy cessation 47.80 32.60 33 5480 26596 46653953
Wrong schedule 46.58 32.60 9 5504 150 46680399
Jaundice 43.17 32.60 32 5481 28813 46651736
Rash 40.14 32.60 112 5401 356400 46324149
Hepatocellular carcinoma 38.60 32.60 14 5499 2825 46677724

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
Fatigue 1494.91 28.05 864 5187 319809 29626618
Headache 1448.42 28.05 704 5347 181602 29764825
Nausea 226.58 28.05 287 5764 296670 29649757
Pruritus 156.46 28.05 153 5898 118051 29828376
Hepatocellular carcinoma 95.40 28.05 44 6007 9566 29936861
Blood bilirubin increased 71.10 28.05 59 5992 36577 29909850
Product dose omission issue 64.98 28.05 86 5965 91545 29854882
Hepatic cirrhosis 63.97 28.05 40 6011 15959 29930468
Therapy cessation 58.40 28.05 37 6014 15100 29931327
Abdominal discomfort 53.07 28.05 57 5994 48734 29897693
Hepatitis C 52.75 28.05 33 6018 13172 29933255
Child-Pugh-Turcotte score increased 36.55 28.05 7 6044 62 29946365
Diarrhoea 36.24 28.05 148 5903 333955 29612472
Viral load increased 34.48 28.05 15 6036 2839 29943588
Jaundice 31.91 28.05 36 6015 32450 29913977

Pharmacologic Action:

SourceCodeDescription
ATC J05AP57 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
FDA MoA N0000182138 Cytochrome P450 1A2 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190107 Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA N0000190108 Organic Anion Transporting Polypeptide 1B3 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
FDA EPC N0000191256 Hepatitis C Virus NS5A Inhibitor
FDA MoA N0000191272 UGT1A1 Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic hepatitis C indication 128302006

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.04 acidic
pKa2 11.64 acidic
pKa3 12.69 acidic
pKa4 13.29 acidic
pKa5 5.17 Basic
pKa6 4.56 Basic
pKa7 1.2 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL Aug. 6, 2021 REVISIONS TO THE GLECAPREVIR/PIBRENTASVIR COMBINULLTION PRODUCT PRESCRIBING INFORMATION TO INCLUDE SAFETY AND EFFICACY DATA FROM THE HCV/HIV-1 COINFECTION STUDY M14-730 AND FROM THE LIVER AND RENULLL TRANSPLANT STUDY M13-596
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL April 30, 2022 NEW PATIENT POPULATION
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL Aug. 3, 2022 NEW CHEMICAL ENTITY
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL Sept. 26, 2022 EIGHT-WEEK DOSING REGIMEN FOR THE TREATMENT OF GENOTYPES 1, 2, 3, 4, 5, AND 6, CHRONIC HEPATITIS C VIRUS INFECTION IN TREATMENT-NULLIVE SUBJECTS WITH COMPENSATED CIRRHOSIS BASED ON THE RESULTS FROM THE EXPEDITION-8 STUDY
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL Oct. 30, 2022 PEDIATRIC EXCLUSIVITY
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL Feb. 3, 2023 PEDIATRIC EXCLUSIVITY
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL March 26, 2023 PEDIATRIC EXCLUSIVITY
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL April 10, 2023 INFORMATION ADDED TO THE LABELING REGARDING SAFETY AND EFFICACY IN SUBJECTS WITH HCV SUBTYPE 3B INFECTION
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL Oct. 10, 2023 PEDIATRIC EXCLUSIVITY
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL April 30, 2026 TREATMENT OF PEDIATRIC PATIENTS 12 YEARS AND OLDER OR WEIGHING AT LEAST 45 KG WITH CHRONIC HEPATITIS C VIRUS (HCV) GENOTYPE 1,2,3,4,5 OR 6 INFECTION WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS (CHILD-PUGH A)
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL April 30, 2026 TREATMENT OF PEDIATRIC PATIENTS 12 YEARS AND OLDER OR WEIGHING AT LEAST 45 KG WITH HCV GENOTYPE 1 INFECTION, WHO PREVIOUSLY HAVE BEEN TREATED WITH A REGIMEN CONTAINING AN HCV NS5A INHIBITOR OR AN NS3/4A PROTEASE INHIBITOR (PI), BUT NOT BOTH
100MG;40MG MAVYRET ABBVIE INC N209394 Aug. 3, 2017 RX TABLET ORAL Oct. 30, 2026 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

None

External reference:

IDSource
4036872 VANDF
C4310001 UMLSCUI
CHEMBL3545123 ChEMBL_ID
58031952 PUBCHEM_CID
D10816 KEGG_DRUG
DB13878 DRUGBANK_ID
C000612854 MESH_SUPPLEMENTAL_RECORD_UI
11268 IUPHAR_LIGAND_ID
C000622691 MESH_SUPPLEMENTAL_RECORD_UI
10260 INN_ID
2WU922TK3L UNII
1940636 RXNORM
33001 MMSL
d08634 MMSL
017296 NDDF
736836002 SNOMEDCT_US
816102004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Mavyret HUMAN PRESCRIPTION DRUG LABEL 2 0074-2600 PELLET 20 mg ORAL NDA 32 sections
Mavyret HUMAN PRESCRIPTION DRUG LABEL 2 0074-2625 TABLET, FILM COATED 40 mg ORAL NDA 32 sections