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

Stem definition	Drug id	CAS RN
antivirals RNA polymerase (NS5B) inhibitors	4914	1132935-63-7

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.50	g	O

ADMET properties:

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

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Approvals:

Date	Agency	Company	Orphan
Dec. 19, 2014	FDA	ABBVIE INC
Nov. 20, 2014	EMA	AbbVie Ltd

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
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
CHEBI has role	CHEBI:36044	antiviral drugs
CHEBI has role	CHEBI:85180	nonnucleoside hepatitis C virus polymerase inhibitors
FDA EPC	N0000191257	Hepatitis C Virus Non-Nucleoside NS5B Palm Polymerase Inhibitor
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
FDA MoA	N0000191258	RNA Replicase Inhibitors
FDA MoA	N0000191272	UGT1A1 Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Chronic hepatitis C	indication	128302006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.38	acidic
pKa2	9.01	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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.
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 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 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.

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Protein cereblon	Cytosolic other	Q96SW2	CRBN_HUMAN		Ki	5.33		CHEMBL
NS5B protein	Enzyme		Q8JXU8_9HEPC		EC50	8.74		CHEMBL

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External reference:

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ID	Source
015829	NDDF
015830	NDDF
11270	IUPHAR_LIGAND_ID
1456607-55-8	SECONDARY_CAS_RN
1597381	RXNORM
30778	MMSL
31899	MMSL
4034028	VANDF
56640146	PUBCHEM_CID
714104000	SNOMEDCT_US

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Pharmaceutical products:

None