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

Stem definition	Drug id	CAS RN
Hepatitis Virus C (HVC) protease inhibitors	5242	1535212-07-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: voxilaprevir GS-9857	Voxilaprevir is a noncovalent, reversible inhibitor of the NS3/4A protease, which is necessary for the proteolytic cleavage of the HCV encoded polyprotein (into mature forms of the NS3, NS4A, NS4B, NS5A, and NS5B proteins) and is essential for viral replication. In a biochemical inhibition assay, voxilaprevir inhibited the proteolytic activity of recombinant NS3/4A enzymes from clinical isolates of HCV genotypes 1b and 3a with Ki values of 38 and 66 pM, respectively. Molecular weight: 868.94 Formula: C40H52F4N6O9S CLOGP: 6.79 LIPINSKI: 3 HAC: 15 HDO: 3 TPSA: 195.22 ALOGS: -4.23 ROTB: 8 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

voxilaprevir
GS-9857

Voxilaprevir is a noncovalent, reversible inhibitor of the NS3/4A protease, which is necessary for the proteolytic cleavage of the HCV encoded polyprotein (into mature forms of the NS3, NS4A, NS4B, NS5A, and NS5B proteins) and is essential for viral replication. In a biochemical inhibition assay, voxilaprevir inhibited the proteolytic activity of recombinant NS3/4A enzymes from clinical isolates of HCV genotypes 1b and 3a with Ki values of 38 and 66 pM, respectively.

Molecular weight: 868.94
Formula: C40H52F4N6O9S
CLOGP: 6.79
LIPINSKI: 3
HAC: 15
HDO: 3
TPSA: 195.22
ALOGS: -4.23
ROTB: 8

Status: ONP

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

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	4	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
July 18, 2017	FDA	GILEAD SCIENCES INC
July 26, 2017	EMA	GILEAD SCIENCES IRELAND UC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J05AP56	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HCV infections
FDA EPC	N0000182639	Hepatitis C Virus NS3/4A Protease Inhibitor
FDA MoA	N0000182638	HCV NS3/4A Protease 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

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

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Disease	Relation	SNOMED_ID
Chronic hepatitis C	indication	128302006
Product containing ethinylestradiol	contraindication	15432003
Pglycoprotein (Pgp) and/or strong cytochrome P450 (CYP) inducers	contraindication	422728003
Dabigatran etexilate	contraindication	700029008
Rosuvastatin	contraindication	700067006

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.64	acidic
pKa2	1.22	Basic

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
400MG;100MG;100MG	VOSEVI	GILEAD SCIENCES INC	N209195	July 18, 2017	RX	TABLET	ORAL	8334270	March 21, 2028	TREATMENT OF ADULT PATIENTS WITH CHRONIC HCV INFECTION WHO HAVE GENOTYPE 1, 2, 3, 4, 5, OR 6 INFECTION AND HAVE PREVIOUSLY BEEN TREATED WITH AN HCV REGIMEN CONTAINING AN NS5A INHIBITOR
400MG;100MG;100MG	VOSEVI	GILEAD SCIENCES INC	N209195	July 18, 2017	RX	TABLET	ORAL	8334270	March 21, 2028	TREATMENT OF ADULT PATIENTS WITH CHRONIC HCV INFECTION WHO HAVE GENOTYPE 1A OR 3 INFECTION AND HAVE PREVIOUSLY BEEN TREATED WITH AN HCV REGIMEN CONTAINING SOFOSBUVIR WITHOUT AN NS5A INHIBITOR
400MG;100MG;100MG	VOSEVI	GILEAD SCIENCES INC	N209195	July 18, 2017	RX	TABLET	ORAL	8580765	March 21, 2028	TREATMENT OF ADULT PATIENTS WITH CHRONIC HCV INFECTION WHO HAVE GENOTYPE 1, 2, 3, 4, 5, OR 6 INFECTION AND HAVE PREVIOUSLY BEEN TREATED WITH AN HCV REGIMEN CONTAINING AN NS5A INHIBITOR
400MG;100MG;100MG	VOSEVI	GILEAD SCIENCES INC	N209195	July 18, 2017	RX	TABLET	ORAL	8580765	March 21, 2028	TREATMENT OF ADULT PATIENTS WITH CHRONIC HCV INFECTION WHO HAVE GENOTYPE 1A OR 3 INFECTION AND HAVE PREVIOUSLY BEEN TREATED WITH AN HCV REGIMEN CONTAINING SOFOSBUVIR WITHOUT AN NS5A INHIBITOR
400MG;100MG;100MG	VOSEVI	GILEAD SCIENCES INC	N209195	July 18, 2017	RX	TABLET	ORAL	8735372	March 21, 2028	TREATMENT OF ADULT PATIENTS WITH CHRONIC HCV INFECTION WHO HAVE GENOTYPE 1, 2, 3, 4, 5, OR 6 INFECTION AND HAVE PREVIOUSLY BEEN TREATED WITH AN HCV REGIMEN CONTAINING AN NS5A INHIBITOR
400MG;100MG;100MG	VOSEVI	GILEAD SCIENCES INC	N209195	July 18, 2017	RX	TABLET	ORAL	8735372	March 21, 2028	TREATMENT OF ADULT PATIENTS WITH CHRONIC HCV INFECTION WHO HAVE GENOTYPE 1A OR 3 INFECTION AND HAVE PREVIOUSLY BEEN TREATED WITH AN HCV REGIMEN CONTAINING SOFOSBUVIR WITHOUT AN NS5A INHIBITOR
400MG;100MG;100MG	VOSEVI	GILEAD SCIENCES INC	N209195	July 18, 2017	RX	TABLET	ORAL	8957046	March 21, 2028	TREATMENT OF ADULT PATIENTS WITH CHRONIC HCV INFECTION WHO HAVE GENOTYPE 1, 2, 3, 4, 5, OR 6 INFECTION AND HAVE PREVIOUSLY BEEN TREATED WITH AN HCV REGIMEN CONTAINING AN NS5A INHIBITOR
400MG;100MG;100MG	VOSEVI	GILEAD SCIENCES INC	N209195	July 18, 2017	RX	TABLET	ORAL	8957046	March 21, 2028	TREATMENT OF ADULT PATIENTS WITH CHRONIC HCV INFECTION WHO HAVE GENOTYPE 1A OR 3 INFECTION AND HAVE PREVIOUSLY BEEN TREATED WITH AN HCV REGIMEN CONTAINING SOFOSBUVIR WITHOUT AN NS5A INHIBITOR
400MG;100MG;100MG	VOSEVI	GILEAD SCIENCES INC	N209195	July 18, 2017	RX	TABLET	ORAL	9085573	March 21, 2028	TREATMENT OF ADULT PATIENTS WITH CHRONIC HCV INFECTION WHO HAVE GENOTYPE 1, 2, 3, 4, 5, OR 6 INFECTION AND HAVE PREVIOUSLY BEEN TREATED WITH AN HCV REGIMEN CONTAINING AN NS5A INHIBITOR
400MG;100MG;100MG	VOSEVI	GILEAD SCIENCES INC	N209195	July 18, 2017	RX	TABLET	ORAL	9085573	March 21, 2028	TREATMENT OF ADULT PATIENTS WITH CHRONIC HCV INFECTION WHO HAVE GENOTYPE 1A OR 3 INFECTION AND HAVE PREVIOUSLY BEEN TREATED WITH AN HCV REGIMEN CONTAINING SOFOSBUVIR WITHOUT AN NS5A INHIBITOR

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Genome polyprotein	Polyprotein		POLG_HCVBK	INHIBITOR	Ki	10.42		DRUG LABEL	DRUG LABEL
Genome polyprotein	Polyprotein		POLG_HCVK3	INHIBITOR	Ki	10.18		DRUG LABEL	DRUG LABEL

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External reference:

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ID	Source
L9P	PDB_CHEM_ID
017285	NDDF
0570F37359	UNII
10143	INN_ID
1939323	RXNORM
32914	MMSL
4036863	VANDF
736536005	SNOMEDCT_US
816106001	SNOMEDCT_US
89921642	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Vosevi	HUMAN PRESCRIPTION DRUG LABEL	3	61958-2401	TABLET, FILM COATED	100 mg	ORAL	NDA	34 sections

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