dasabuvir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antivirals RNA polymerase (NS5B) inhibitors 4914 1132935-63-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dasabuvir sodium monohydrate
  • dasabuvir
  • dasabuvir sodium
  • exviera
  • ABT-333
Dasabuvir is a non-nucleoside inhibitor of the HCV RNA-dependent RNA polymerase encoded by the NS5B gene, which is essential for replication of the viral genome. In a biochemical assay, dasabuvir inhibited a panel of genotype 1a and 1b NS5B polymerases. Based on drug resistance mapping studies of HCV genotypes 1a and 1b, dasabuvir targets the palm domain of the NS5B polymerase, and is therefore referred to as a non-nucleoside NS5B-palm polymerase inhibitor.
  • Molecular weight: 493.58
  • Formula: C26H27N3O5S
  • CLOGP: 4.07
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 104.81
  • ALOGS: -5.79
  • ROTB: 5

  • Status: OFM

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

Drug dosage:

DoseUnitRoute
0.50 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 2.13 L/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5.70 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 20, 2014 EMA AbbVie Ltd
Dec. 19, 2014 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
Jaundice 414.40 32.32 131 4427 29120 63455344
Hyperbilirubinaemia 344.87 32.32 92 4466 11222 63473242
Hepatic failure 262.78 32.32 98 4460 35558 63448906
Ascites 225.63 32.32 91 4467 40637 63443827
Blood bilirubin increased 195.43 32.32 80 4478 37060 63447404
Hepatocellular carcinoma 159.84 32.32 36 4522 2158 63482306
Hepatic encephalopathy 124.83 32.32 42 4516 11240 63473224
Asthenia 97.32 32.32 128 4430 383476 63100988
Renal impairment 86.03 32.32 62 4496 88293 63396171
Hepatic cirrhosis 83.41 32.32 39 4519 24695 63459769
Anaemia 79.09 32.32 101 4457 293329 63191135
Vomiting 72.28 32.32 137 4421 559480 62924984
Child-Pugh-Turcotte score increased 67.34 32.32 9 4549 17 63484447
Hepatorenal syndrome 55.42 32.32 15 4543 1917 63482547
Drug ineffective 51.92 32.32 7 4551 1044758 62439706
Varices oesophageal 48.18 32.32 15 4543 3133 63481331
Encephalopathy 46.70 32.32 31 4527 38589 63445875
Yellow skin 44.05 32.32 13 4545 2267 63482197
Acute hepatic failure 41.33 32.32 22 4536 18305 63466159
Portal vein thrombosis 38.03 32.32 12 4546 2618 63481846
Renal failure 37.21 32.32 44 4514 117608 63366856
Hepatic cancer 35.41 32.32 13 4545 4474 63479990
Nausea 33.44 32.32 135 4423 854336 62630128

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
Hepatocellular carcinoma 229.51 28.67 68 4001 7441 34945421
Ascites 206.88 28.67 103 3966 46468 34906394
Renal impairment 188.95 28.67 124 3945 94389 34858473
Hyperbilirubinaemia 158.03 28.67 63 4006 16780 34936082
Jaundice 142.82 28.67 71 3998 31811 34921051
Hepatic failure 128.86 28.67 68 4001 34463 34918399
Blood bilirubin increased 119.52 28.67 67 4002 38229 34914633
Hepatic cirrhosis 112.86 28.67 50 4019 17264 34935598
Hepatic encephalopathy 107.41 28.67 46 4023 14639 34938223
Drug interaction 61.90 28.67 101 3968 225845 34727017
Oesophageal varices haemorrhage 44.83 28.67 16 4053 3130 34949732
Gastric varices haemorrhage 42.37 28.67 9 4060 249 34952613
Anaemia 41.89 28.67 87 3982 233248 34719614
Off label use 37.72 28.67 3 4066 419521 34533341
Asthenia 33.43 28.67 82 3987 245169 34707693
Yellow skin 31.02 28.67 11 4058 2111 34950751
Encephalopathy 29.90 28.67 28 4041 35291 34917571
Gastroenteritis 28.84 28.67 19 4050 14381 34938481

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
Jaundice 474.89 25.52 187 8264 53162 79682775
Hyperbilirubinaemia 458.19 25.52 149 8302 24369 79711568
Ascites 393.17 25.52 181 8270 75381 79660556
Hepatocellular carcinoma 338.77 25.52 94 8357 8927 79727010
Hepatic failure 338.34 25.52 153 8298 61059 79674878
Renal impairment 266.04 25.52 180 8271 157603 79578334
Blood bilirubin increased 248.61 25.52 127 8324 66105 79669832
Hepatic encephalopathy 205.17 25.52 82 8369 24084 79711853
Hepatic cirrhosis 166.88 25.52 79 8372 34827 79701110
Anaemia 109.31 25.52 180 8271 444835 79291102
Asthenia 106.11 25.52 192 8259 511497 79224440
Hepatorenal syndrome 84.02 25.52 27 8424 4222 79731715
Child-Pugh-Turcotte score increased 82.25 25.52 12 8439 32 79735905
Drug interaction 81.13 25.52 152 8299 415031 79320906
Yellow skin 80.64 25.52 25 8426 3480 79732457
Oesophageal varices haemorrhage 68.02 25.52 23 8428 4213 79731724
Drug ineffective 67.64 25.52 16 8435 1080897 78655040
Off label use 57.54 25.52 13 8438 907202 78828735
Encephalopathy 56.51 25.52 51 8400 67346 79668591
Portal vein thrombosis 50.20 25.52 20 8431 5807 79730130
Vomiting 47.99 25.52 167 8284 665661 79070276
Varices oesophageal 46.23 25.52 19 8432 5972 79729965
Acute hepatic failure 42.72 25.52 31 8420 30082 79705855
Renal failure 42.16 25.52 76 8375 200892 79535045
Alanine aminotransferase increased 41.37 25.52 67 8384 162503 79573434
Gastric varices haemorrhage 38.34 25.52 9 8442 435 79735502
Ocular icterus 34.31 25.52 15 8436 5485 79730452
Hepatic neoplasm 33.89 25.52 13 8438 3413 79732524
Upper gastrointestinal haemorrhage 32.11 25.52 30 8421 41350 79694587
Haematemesis 31.48 25.52 33 8418 52231 79683706
Decreased appetite 31.00 25.52 93 8358 342325 79393612
Bilirubin conjugated increased 27.87 25.52 13 8438 5526 79730411
Hepatic cancer 27.74 25.52 16 8435 10513 79725424
Procalcitonin 27.07 25.52 4 8447 12 79735925

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AP09 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
ATC J05AP52 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Antivirals for treatment of HCV infections
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA EPC N0000191257 Hepatitis C Virus Non-Nucleoside NS5B Palm Polymerase Inhibitor
FDA MoA N0000191258 RNA Replicase Inhibitors
FDA MoA N0000191272 UGT1A1 Inhibitors
CHEBI has role CHEBI:36044 antiviral drugs
CHEBI has role CHEBI:85180 nonnucleoside hepatitis C virus polymerase inhibitors

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 8.38 acidic
pKa2 9.01 acidic

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 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 DISCN TABLET 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 9139536 Nov. 9, 2028 TREATMENT OF HCV INFECTION USING DASABUVIR
EQ 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 DISCN TABLET ORAL 8501238 Dec. 19, 2028 USE OF DASABUVIR TO INHIBIT VIRAL REPLICATION FOR THE TREATMENT OF HCV INFECTION.
EQ 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 DISCN TABLET ORAL 8188104 May 17, 2029 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 8188104 May 17, 2029 USE OF DASABUVIR TO INHIBIT VIRAL REPLICATION FOR THE TREATMENT OF HCV INFECTION.
EQ 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 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
EQ 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 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
EQ 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 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 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 DISCN TABLET ORAL 8466159 Sept. 4, 2032 TREATMENT OF HCV INFECTION USING PARITAPREVIR, OMBITASVIR, RITONAVIR, AND DASABUVIR WITH RIBAVIRIN.
EQ 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 DISCN TABLET ORAL 8492386 Sept. 4, 2032 TREATMENT OF HCV INFECTION USING PARITAPREVIR, OMBITASVIR, RITONAVIR, AND DASABUVIR, WITHOUT RIBAVIRIN
EQ 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 DISCN TABLET ORAL 8680106 Sept. 4, 2032 TREATMENT OF HCV INFECTION USING PARITAPREVIR, OMBITASVIR, RITONAVIR, AND DASABUVIR WITH RIBAVIRIN.
EQ 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 DISCN TABLET 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 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 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 DISCN TABLET ORAL 10201542 Oct. 18, 2033 TREATMENT OF HCV INFECTION USING DASABUVIR
EQ 250MG BASE;12.5MG, 75MG, 50MG VIEKIRA PAK (COPACKAGED) ABBVIE N206619 Dec. 19, 2014 DISCN TABLET ORAL 9629841 Oct. 18, 2033 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 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
Protein cereblon Cytosolic other Ki 5.33 CHEMBL
NS5B protein Enzyme EC50 8.74 CHEMBL

External reference:

IDSource
D10553 KEGG_DRUG
1456607-55-8 SECONDARY_CAS_RN
4034028 VANDF
CHEBI:85182 CHEBI
CHEMBL3137312 ChEMBL_ID
C588260 MESH_SUPPLEMENTAL_RECORD_UI
11270 IUPHAR_LIGAND_ID
DB09183 DRUGBANK_ID
1597381 RXNORM
30778 MMSL
31899 MMSL
d08322 MMSL
015829 NDDF
015830 NDDF
714104000 SNOMEDCT_US
714105004 SNOMEDCT_US
716018007 SNOMEDCT_US
725851005 SNOMEDCT_US
C3852512 UMLSCUI
CHEMBL3544985 ChEMBL_ID
9741 INN_ID
56640146 PUBCHEM_CID
DE54EQW8T1 UNII

Pharmaceutical products:

None