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

Stem definitionDrug idCAS RN
antivirals, hepatitis C Virus (HCV) NS5A inhibitors 5154 1377049-84-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • velpatasvir
  • GS-5816
  • GS5816
pan-genotypic NS5A inhibitor for the treatment of chronic genotype 1-6 hepatitis C virus (HCV) infection
  • Molecular weight: 883.02
  • Formula: C49H54N8O8
  • CLOGP: 5.70
  • LIPINSKI: 3
  • HAC: 16
  • HDO: 4
  • TPSA: 193.10
  • ALOGS: -5.21
  • ROTB: 13

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 28, 2016 FDA GILEAD SCIENCES 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 1068.25 32.16 700 5585 477652 46202125
Fatigue 1018.19 32.16 745 5540 607952 46071825
Nausea 308.83 32.16 415 5870 687039 45992738
Hepatitis C 188.01 32.16 58 6227 6260 46673517
Insomnia 150.51 32.16 145 6140 164779 46514998
Product dose omission issue 120.56 32.16 130 6155 168390 46511387
Genotype drug resistance test positive 97.71 32.16 21 6264 529 46679248
Hepatocellular carcinoma 79.95 32.16 25 6260 2814 46676963
Product use complaint 77.32 32.16 22 6263 1790 46677987
Intentional dose omission 72.31 32.16 24 6261 3266 46676511
Maternal exposure during pregnancy 62.66 32.16 73 6212 102476 46577301
Dyspepsia 59.94 32.16 59 6226 68413 46611364
Diarrhoea 58.43 32.16 186 6099 559416 46120361
Hepatitis C virus test positive 56.21 32.16 11 6274 171 46679606
Treatment failure 49.86 32.16 62 6223 93025 46586752
Irritability 35.18 32.16 30 6255 28916 46650861

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 1591.73 25.64 1048 8046 319625 29623759
Headache 1231.45 25.64 729 8365 181577 29761807
Hepatitis C 803.08 25.64 253 8841 12952 29930432
Treatment failure 428.25 25.64 209 8885 34470 29908914
Hepatocellular carcinoma 292.82 25.64 110 8984 9500 29933884
Genotype drug resistance test positive 289.17 25.64 72 9022 1517 29941867
Nausea 231.26 25.64 359 8735 296598 29646786
Product dose omission issue 221.99 25.64 199 8895 91432 29851952
Insomnia 197.49 25.64 188 8906 93148 29850236
Intentional dose omission 192.83 25.64 51 9043 1374 29942010
Dyspepsia 113.44 25.64 85 9009 30244 29913140
Diarrhoea 110.64 25.64 283 8811 333820 29609564
Hepatic cirrhosis 98.38 25.64 61 9033 15938 29927446
Drug ineffective 97.15 25.64 273 8821 340114 29603270
Liver transplant 84.98 25.64 32 9062 2770 29940614
Hepatitis C virus test positive 79.58 25.64 20 9074 437 29942947
Abdominal discomfort 76.84 25.64 84 9010 48707 29894677
Oesophageal varices haemorrhage 45.49 25.64 21 9073 3030 29940354
Hepatic cancer 42.86 25.64 26 9068 6522 29936862
Product use complaint 41.74 25.64 15 9079 1137 29942247
Ammonia abnormal 37.74 25.64 8 9086 79 29943305
Hepatic encephalopathy 36.51 25.64 32 9062 14160 29929224
Intentional product use issue 33.58 25.64 48 9046 36392 29906992
Therapy cessation 32.81 25.64 31 9063 15106 29928278
Circumstance or information capable of leading to medication error 30.08 25.64 13 9081 1606 29941778
Extra dose administered 28.49 25.64 15 9079 2871 29940513
Abdominal pain upper 28.11 25.64 60 9034 62491 29880893

Pharmacologic Action:

SourceCodeDescription
ATC J05AP55 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
ATC J05AP56 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
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 N0000190109 Organic Anion Transporting Polypeptide 2B1 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA EPC N0000191256 Hepatitis C Virus NS5A Inhibitor
CHEBI has role CHEBI:36044 anti-virus drug
CHEBI has role CHEBI:85185 ns5a inhibitor

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 11.48 acidic
pKa2 12.26 acidic
pKa3 12.93 acidic
pKa4 13.17 acidic
pKa5 6.49 Basic
pKa6 5.8 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL June 28, 2021 NEW CHEMICAL ENTITY
400MG;100MG;100MG VOSEVI GILEAD SCIENCES INC N209195 July 18, 2017 RX TABLET ORAL July 18, 2022 NEW CHEMICAL ENTITY
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL Nov. 15, 2022 INFORMATION ADDED TO THE DOSING SECTION IN REGARD TO THE TREATMENT OF CHRONIC HEPATITIS C VIRUS INFECTION IN PATIENTS WITH SEVERE RENULLL IMPAIRMENT INCLUDING PATIENTS WITH END STAGE RENULLL DISEASE ON DIALYSIS
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL March 19, 2023 NEW STRENGTH
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL March 19, 2023 NEW PATIENT POPULATION
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL May 15, 2023 PEDIATRIC EXCLUSIVITY
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL July 14, 2023 INFORMATION ADDED TO THE LABELING DESCRIBING A PHASE 2, MULTICENTER, OPEN-LABEL STUDY TO EVALUATE THE SAFETY/EFFICACY OF SOFOSBUVIR/VELPATASVIR IN SUBJECTS WITH CHRONIC HCV INFECTION WHO HAVE RECEIVED A LIVER TRANSPLANT
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL July 14, 2023 INFORMATION ADDED TO THE LABELING DESCRIBING A PHASE 2, MULTICENTER, OPEN-LABEL STUDY TO EVALUATE THE SAFETY/EFFICACY OF SOFOSBUVIR/VELPATASVIR IN SUBJECTS WITH CHRONIC HCV INFECTION WHO HAVE RECEIVED A LIVER TRANSPLANT
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL Sept. 19, 2023 PEDIATRIC EXCLUSIVITY
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL Sept. 19, 2023 PEDIATRIC EXCLUSIVITY
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL Jan. 14, 2024 PEDIATRIC EXCLUSIVITY
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL Jan. 14, 2024 PEDIATRIC EXCLUSIVITY
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL March 19, 2027 TX OF PED PTS 6 YRS OF AGE & OLDER OR WEIGHING AT LEAST 17 KG WITH CHRONIC HEPATITIS C VIRUS GENOTYPE 1, 2, 3, 4, 5, OR 6 INFECTION: WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS; OR WITH DECOMPENSATED CIRRHOSIS FOR USE IN COMBINULLTION WITH RIBAVIRIN
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL March 19, 2027 TX OF PED PTS 6 YRS OF AGE & OLDER OR WEIGHING AT LEAST 17 KG WITH CHRONIC HEPATITIS C VIRUS GENOTYPE 1, 2, 3, 4, 5, OR 6 INFECTION: WITHOUT CIRRHOSIS OR WITH COMPENSATED CIRRHOSIS; OR WITH DECOMPENSATED CIRRHOSIS FOR USE IN COMBINULLTION WITH RIBAVIRIN
200MG;50MG EPCLUSA GILEAD SCIENCES INC N208341 March 19, 2020 RX TABLET ORAL Sept. 19, 2027 PEDIATRIC EXCLUSIVITY
400MG;100MG EPCLUSA GILEAD SCIENCES INC N208341 June 28, 2016 RX TABLET ORAL Sept. 19, 2027 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Genome polyprotein Polyprotein INHIBITOR EC50 10.85 DRUG LABEL DRUG LABEL
Genome polyprotein Polyprotein INHIBITOR EC50 10.80 DRUG LABEL DRUG LABEL
Genome polyprotein Polyprotein INHIBITOR EC50 10.98 DRUG LABEL DRUG LABEL
Genome polyprotein Polyprotein INHIBITOR EC50 11.05 DRUG LABEL DRUG LABEL
Genome polyprotein Polyprotein INHIBITOR EC50 11.40 DRUG LABEL DRUG LABEL
Genome polyprotein Polyprotein INHIBITOR EC50 11.40 DRUG LABEL DRUG LABEL
Genome polyprotein Polyprotein INHIBITOR EC50 10.43 DRUG LABEL DRUG LABEL
Genome polyprotein Polyprotein INHIBITOR EC50 11.10 DRUG LABEL DRUG LABEL

External reference:

IDSource
4035867 VANDF
C4080094 UMLSCUI
CHEBI:133009 CHEBI
CHEMBL3545062 ChEMBL_ID
C000604171 MESH_SUPPLEMENTAL_RECORD_UI
9960 INN_ID
DB11613 DRUGBANK_ID
KCU0C7RS7Z UNII
67683363 PUBCHEM_CID
11269 IUPHAR_LIGAND_ID
1799206 RXNORM
31777 MMSL
d08455 MMSL
016909 NDDF
719641001 SNOMEDCT_US
816105002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Epclusa HUMAN PRESCRIPTION DRUG LABEL 2 61958-2201 TABLET, FILM COATED 100 mg ORAL NDA 36 sections
Epclusa Access HUMAN PRESCRIPTION DRUG LABEL 2 61958-2202 TABLET, FILM COATED 100 mg ORAL Export only 31 sections
Epclusa HUMAN PRESCRIPTION DRUG LABEL 2 61958-2203 TABLET, FILM COATED 50 mg ORAL NDA 36 sections
Epclusa HUMAN PRESCRIPTION DRUG LABEL 2 61958-2204 PELLET 50 mg ORAL NDA 36 sections
Epclusa HUMAN PRESCRIPTION DRUG LABEL 2 61958-2205 PELLET 37.50 mg ORAL NDA 36 sections
Vosevi HUMAN PRESCRIPTION DRUG LABEL 3 61958-2401 TABLET, FILM COATED 100 mg ORAL NDA 34 sections
Sofosbuvir and Velpatasvir HUMAN PRESCRIPTION DRUG LABEL 2 72626-2701 TABLET, FILM COATED 100 mg ORAL NDA AUTHORIZED GENERIC 35 sections