Identification

Name
Velpatasvir
Accession Number
DB11613
Type
Small Molecule
Groups
Approved
Description

Velpatasvir is a Direct-Acting Antiviral (DAA) medication used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients [8]. Velpatasvir acts as a defective substrate for NS5A (Non-Structural Protein 5A), a non-enzymatic viral protein that plays a key role in Hepatitis C Virus replication, assembly, and modulation of host immune responses [3]. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) such as velpatasvir. Notably, velpatasvir has a significantly higher barrier to resistance than the first generation NS5A inhibitors, such as Ledipasvir and Daclatasvir, making it a highly potent and reliable alternative for treatment of chronic Hepatitis C [6].

In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) recommend Velpatasvir as first line therapy in combination with sofosbuvir for all six genotypes of Hepatitis C [8]. Velpatasvir is currently only available within a fixed dose combination product as Epclusa with Sofosbuvir, another direct acting antiviral. Goals of therapy for Epclusa include the intent to cure, or achieve a sustained virologic response (SVR), after 12 weeks of daily therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality and risk of requiring a liver transplant [5].

Since June 2016, Velpatasvir has been available as a fixed dose combination product with Sofosbuvir, as the commercially available product Epclusa. Epclusa is the first combination HCV product indicated for the treatment of all genotypes of Hepatitis C with or without cirrhosis. It is also currently the most potent HCV antiviral medication on the market with a sustained virologic response (SVR) after 12 weeks of therapy of 93-99% depending on genotype and level of cirrhosis and a high barrier to resistance [8]. Both Canadian and American guidelines list Epclusa as a first line recommendation for all genotypes of HCV [8, 5].

Structure
Thumb
Synonyms
  • methyl {(2S)-1-[(2S,5S)-2-(9-{2-[(2S,4S)-1-{(2R)-2-[(methoxycarbonyl)amino]-2-phenylacetyl}-4-(methoxymethyl)pyrrolidin-2-yl]-1H-imidazol-4-yl}-1,11-dihydro[2]benzopyrano[4',3':6,7]naphtho[1,2-d]imidazol-2-yl)-5-methylpyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl}carbamate
External IDs
GS 5816 / GS-5816 / GS5816
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
EpclusaVelpatasvir (100 mg) + Sofosbuvir (400 mg)TabletOralGilead Sciences2016-08-02Not applicableCanada
EpclusaVelpatasvir (100 mg/1) + Sofosbuvir (400 mg/1)Tablet, film coatedOralGilead Sciences2016-06-28Not applicableUs
VoseviVelpatasvir (100 mg) + Sofosbuvir (400 mg) + Voxilaprevir (100 mg)TabletOralGilead SciencesNot applicableNot applicableCanada
VoseviVelpatasvir (100 mg/1) + Sofosbuvir (400 mg/1) + Voxilaprevir (100 mg/1)Tablet, film coatedOralGilead Sciences2017-07-18Not applicableUs
Categories
UNII
KCU0C7RS7Z
CAS number
1377049-84-7
Weight
Average: 883.019
Monoisotopic: 882.406460731
Chemical Formula
C49H54N8O8
InChI Key
FHCUMDQMBHQXKK-CDIODLITSA-N
InChI
InChI=1S/C49H54N8O8/c1-26(2)41(54-48(60)63-5)47(59)57-27(3)12-17-38(57)45-51-36-16-14-30-20-35-33-15-13-31(19-32(33)25-65-40(35)21-34(30)43(36)53-45)37-22-50-44(52-37)39-18-28(24-62-4)23-56(39)46(58)42(55-49(61)64-6)29-10-8-7-9-11-29/h7-11,13-16,19-22,26-28,38-39,41-42H,12,17-18,23-25H2,1-6H3,(H,50,52)(H,51,53)(H,54,60)(H,55,61)/t27-,28-,38-,39-,41-,42+/m0/s1
IUPAC Name
(2S)-2-{[hydroxy(methoxy)methylidene]amino}-1-[(2S,5S)-2-(17-{2-[(2S,4S)-1-[(2R)-2-{[hydroxy(methoxy)methylidene]amino}-2-phenylacetyl]-4-(methoxymethyl)pyrrolidin-2-yl]-1H-imidazol-5-yl}-21-oxa-5,7-diazapentacyclo[11.8.0.0^{3,11}.0^{4,8}.0^{14,19}]henicosa-1(13),2,4(8),6,9,11,14(19),15,17-nonaen-6-yl)-5-methylpyrrolidin-1-yl]-3-methylbutan-1-one
SMILES
[H][[email protected]](N=C(O)OC)(C(C)C)C(=O)N1[[email protected]@]([H])(C)CC[[email protected]@]1([H])C1=NC2=C(N1)C1=CC3=C(C=C1C=C2)C1=C(CO3)C=C(C=C1)C1=CN=C(N1)[[email protected]]1([H])C[[email protected]]([H])(COC)CN1C(=O)[[email protected]]([H])(N=C(O)OC)C1=CC=CC=C1

Pharmacology

Indication

Velpatasvir is used in combination therapy with other antiviral medications to treat chronic hepatitis C virus (HCV) infected patients with HCV genoptypes 1-6, and to treat HCV and HIV co-infected patients. Depending on the level of cirrhosis or decompensation, combination therapy can also include therapy with Ribavirin.

When used in combination with Sofosbuvir as the combination product Epclusa, Velpatasvir is indicated for the treatment of adult patients with chronic hepatitis C virus (HCV) genotype 1, 2, 3, 4, 5, or 6 infection without cirrhosis or with compensated cirrhosis, or in combination with Ribavirin if associated with decompensated cirrhosis [FDA Label].

Structured Indications
Pharmacodynamics

Velpatasvir is a small molecule direct-acting antiviral used in the treatment of hepatitis C in combination with sofosbuvir. Velpatasvir prevents viral replication by inhibiting non-structural protein 5A (NS5A) [4].

At a dose 5 times the recommended dose, velpatasvir does not prolong QTc interval to any clinically relevant extent [FDA Label].

Mechanism of action

Velpatasvir's mechanism of action is likely similar to other selective NS5A inhibitors which bind domain I of NS5A consisting of amino acids 33-202 [1]. NS5A inhibitors compete with RNA for binding at this site. It is also thought that NS5A inhibitors bind the target during its action in replication when the binding site is exposed [2]. Inhibition of NS5A is also known to produce redistribution of the protein to lipid droplets. The exact role of NS5A in RNA replication is not yet understood although it is known to be an important component.

TargetActionsOrganism
ANonstructural Protein 5A (NS5A)
inhibitor
Hepatitis C Virus (HCV)
Absorption

Oral bioavailability of 25-30% [3].

Volume of distribution

1.4-1.6 L/kg [3].

Protein binding

>99.5% bound to plasma proteins [FDA Label].

Metabolism

Some metabolism by CYP2B6, CYP2C8, and CYP3A4 [3].

Route of elimination

94% excreted in feces with 77% as parent compound. 0.4% excreted in urine [FDA Label].

Half life

15h [FDA Label].

Clearance

Estimated 0.12 L/h/kg [A19175.

Toxicity

No indication of carcinogenicity or impairment of fertility/fetal viability [FDA Label].

Affected organisms
  • Hepatitis C Virus
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Velpatasvir can be increased when it is combined with Abiraterone.Approved
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Velpatasvir.Approved
AcetaminophenThe serum concentration of Velpatasvir can be increased when it is combined with Acetaminophen.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Velpatasvir.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Velpatasvir.Approved
AlbendazoleThe serum concentration of Velpatasvir can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Velpatasvir can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Velpatasvir can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Velpatasvir can be increased when it is combined with Alfentanil.Approved, Illicit
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Velpatasvir.Approved, Investigational
AmantadineThe serum concentration of Velpatasvir can be increased when it is combined with Amantadine.Approved
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Velpatasvir.Approved, Investigational
Aminohippuric acidThe serum concentration of Velpatasvir can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe metabolism of Velpatasvir can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Velpatasvir can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Velpatasvir can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Velpatasvir can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Velpatasvir can be increased when it is combined with Amsacrine.Approved
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Velpatasvir.Approved
AprepitantThe serum concentration of Velpatasvir can be increased when it is combined with Aprepitant.Approved, Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Velpatasvir.Approved, Investigational
AstemizoleThe serum concentration of Velpatasvir can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe metabolism of Velpatasvir can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Velpatasvir can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Velpatasvir can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Velpatasvir can be increased when it is combined with Atorvastatin.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Velpatasvir.Approved, Investigational
AzelastineThe serum concentration of Velpatasvir can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Velpatasvir can be increased when it is combined with Azithromycin.Approved
BelinostatThe serum concentration of Belinostat can be increased when it is combined with Velpatasvir.Approved, Investigational
BenzocaineThe serum concentration of Velpatasvir can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Velpatasvir can be increased when it is combined with Bepridil.Approved, Withdrawn
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Velpatasvir.Approved, Vet Approved
BiperidenThe serum concentration of Velpatasvir can be increased when it is combined with Biperiden.Approved
BoceprevirThe metabolism of Velpatasvir can be decreased when combined with Boceprevir.Withdrawn
BortezomibThe metabolism of Velpatasvir can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Velpatasvir can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Velpatasvir.Approved
BromocriptineThe serum concentration of Velpatasvir can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Velpatasvir can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Velpatasvir can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe serum concentration of Velpatasvir can be increased when it is combined with Cabazitaxel.Approved
CaffeineThe serum concentration of Velpatasvir can be increased when it is combined with Caffeine.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Velpatasvir.Experimental
CanagliflozinThe serum concentration of Velpatasvir can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Velpatasvir can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Velpatasvir can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Velpatasvir can be increased when combined with Carbamazepine.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Velpatasvir.Approved
CarvedilolThe serum concentration of Velpatasvir can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Velpatasvir can be increased when it is combined with Caspofungin.Approved
CelecoxibThe metabolism of Velpatasvir can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Velpatasvir can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Velpatasvir.Withdrawn
ChloroquineThe serum concentration of Velpatasvir can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Velpatasvir can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Velpatasvir can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Velpatasvir can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Velpatasvir can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Velpatasvir can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Velpatasvir can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Velpatasvir can be decreased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Velpatasvir can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Velpatasvir.Approved
CitalopramThe serum concentration of Velpatasvir can be increased when it is combined with Citalopram.Approved
ClarithromycinThe metabolism of Velpatasvir can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Velpatasvir can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Velpatasvir.Approved, Illicit
ClofazimineThe serum concentration of Velpatasvir can be increased when it is combined with Clofazimine.Approved, Investigational
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Velpatasvir.Approved, Investigational
ClomipramineThe serum concentration of Velpatasvir can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Velpatasvir.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Velpatasvir.Approved, Nutraceutical
ClotrimazoleThe metabolism of Velpatasvir can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Velpatasvir.Approved
CobicistatThe metabolism of Velpatasvir can be decreased when combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Velpatasvir.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Velpatasvir.Approved
ColforsinThe serum concentration of Velpatasvir can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Velpatasvir can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated estrogensThe serum concentration of Conjugated estrogens can be increased when it is combined with Velpatasvir.Approved
CopanlisibThe serum concentration of Copanlisib can be increased when it is combined with Velpatasvir.Approved
CrisaboroleThe metabolism of Velpatasvir can be decreased when combined with Crisaborole.Approved
CrizotinibThe metabolism of Velpatasvir can be decreased when combined with Crizotinib.Approved
CyclophosphamideThe serum concentration of Velpatasvir can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe metabolism of Velpatasvir can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Velpatasvir.Approved
DabrafenibThe serum concentration of Velpatasvir can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Velpatasvir can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Velpatasvir can be increased when it is combined with Dactinomycin.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Velpatasvir.Approved
DarunavirThe metabolism of Velpatasvir can be decreased when combined with Darunavir.Approved
DaunorubicinThe serum concentration of Velpatasvir can be decreased when it is combined with Daunorubicin.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Velpatasvir.Approved
DeferasiroxThe serum concentration of Velpatasvir can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Velpatasvir can be decreased when combined with Delavirdine.Approved
DesipramineThe serum concentration of Velpatasvir can be increased when it is combined with Desipramine.Approved
DesloratadineThe serum concentration of Velpatasvir can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Velpatasvir can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Velpatasvir can be increased when it is combined with Dextromethorphan.Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Velpatasvir.Approved, Illicit, Vet Approved
DiclofenacThe serum concentration of Velpatasvir can be increased when it is combined with Diclofenac.Approved, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Velpatasvir.Approved
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Velpatasvir.Approved
DigoxinThe serum concentration of Velpatasvir can be decreased when it is combined with Digoxin.Approved
DihydroergotamineThe metabolism of Velpatasvir can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Velpatasvir.Illicit
DiltiazemThe metabolism of Velpatasvir can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Velpatasvir can be increased when it is combined with Dipyridamole.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Velpatasvir.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Velpatasvir.Approved, Investigational, Vet Approved
DoxazosinThe serum concentration of Velpatasvir can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Velpatasvir can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Velpatasvir.Approved, Investigational
DoxorubicinThe serum concentration of Velpatasvir can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Velpatasvir can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Velpatasvir can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Velpatasvir can be decreased when combined with Dronedarone.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Velpatasvir.Approved
EfavirenzThe metabolism of Velpatasvir can be decreased when combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Velpatasvir can be increased when it is combined with Elbasvir.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Velpatasvir.Approved, Investigational
EltrombopagThe serum concentration of Velpatasvir can be increased when it is combined with Eltrombopag.Approved
EnalaprilThe serum concentration of Velpatasvir can be increased when it is combined with Enalapril.Approved, Vet Approved
EnasidenibThe serum concentration of Enasidenib can be increased when it is combined with Velpatasvir.Approved
EnzalutamideThe serum concentration of Velpatasvir can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Velpatasvir.Approved, Investigational
ErgonovineThe serum concentration of Velpatasvir can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Velpatasvir can be increased when it is combined with Ergotamine.Approved
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Velpatasvir.Approved, Investigational
ErythromycinThe metabolism of Velpatasvir can be decreased when combined with Erythromycin.Approved, Vet Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Velpatasvir.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Velpatasvir can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Velpatasvir can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Velpatasvir can be decreased when it is combined with Estrone.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Velpatasvir.Approved
EtoposideThe serum concentration of Velpatasvir can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Velpatasvir can be increased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Velpatasvir.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Velpatasvir.Approved
FelodipineThe serum concentration of Velpatasvir can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Velpatasvir can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Velpatasvir.Approved
FexofenadineThe serum concentration of Velpatasvir can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Velpatasvir can be increased when it is combined with Fidaxomicin.Approved
FluconazoleThe metabolism of Velpatasvir can be decreased when combined with Fluconazole.Approved
FluoxetineThe serum concentration of Velpatasvir can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Velpatasvir can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Velpatasvir can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Velpatasvir can be increased when it is combined with Flurazepam.Approved, Illicit
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Velpatasvir.Approved
FluvoxamineThe metabolism of Velpatasvir can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Velpatasvir can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Velpatasvir can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Velpatasvir can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Velpatasvir can be increased when it is combined with Fusidic Acid.Approved
GefitinibThe serum concentration of Velpatasvir can be increased when it is combined with Gefitinib.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Velpatasvir.Approved
GenisteinThe serum concentration of Velpatasvir can be increased when it is combined with Genistein.Investigational
GlecaprevirThe serum concentration of Glecaprevir can be increased when it is combined with Velpatasvir.Approved
GlyburideThe serum concentration of Velpatasvir can be increased when it is combined with Glyburide.Approved
GlycerinThe serum concentration of Velpatasvir can be increased when it is combined with Glycerin.Approved, Investigational
Gramicidin DThe serum concentration of Velpatasvir can be increased when it is combined with Gramicidin D.Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Velpatasvir.Approved
GrepafloxacinThe serum concentration of Velpatasvir can be increased when it is combined with Grepafloxacin.Withdrawn
HaloperidolThe serum concentration of Velpatasvir can be increased when it is combined with Haloperidol.Approved
HydrocortisoneThe serum concentration of Velpatasvir can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Velpatasvir.Approved
IdelalisibThe serum concentration of Velpatasvir can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Velpatasvir can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Velpatasvir can be increased when it is combined with Imipramine.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Velpatasvir.Approved
IndinavirThe metabolism of Velpatasvir can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Velpatasvir can be increased when it is combined with Indomethacin.Approved, Investigational
Inotuzumab ozogamicinThe serum concentration of Inotuzumab ozogamicin can be increased when it is combined with Velpatasvir.Approved
IrbesartanThe metabolism of Velpatasvir can be decreased when combined with Irbesartan.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Velpatasvir.Approved, Investigational
IsavuconazoniumThe metabolism of Velpatasvir can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Velpatasvir can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Velpatasvir can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Velpatasvir can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Velpatasvir can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Velpatasvir can be increased when it is combined with Ketamine.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Velpatasvir.Approved
KetoconazoleThe metabolism of Velpatasvir can be decreased when combined with Ketoconazole.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Velpatasvir.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Velpatasvir.Approved, Investigational
LansoprazoleThe serum concentration of Velpatasvir can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Velpatasvir can be increased when it is combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Velpatasvir.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Velpatasvir.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Velpatasvir.Approved
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Velpatasvir.Approved, Investigational
LevofloxacinThe serum concentration of Velpatasvir can be increased when it is combined with Levofloxacin.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Velpatasvir.Approved
LevothyroxineThe serum concentration of Velpatasvir can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Velpatasvir can be increased when it is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Velpatasvir.Approved
LiothyronineThe serum concentration of Velpatasvir can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Velpatasvir can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Velpatasvir can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Velpatasvir can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Velpatasvir can be increased when it is combined with Loperamide.Approved
LopinavirThe metabolism of Velpatasvir can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Velpatasvir can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Velpatasvir can be increased when it is combined with Losartan.Approved
LovastatinThe metabolism of Velpatasvir can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Velpatasvir can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Velpatasvir can be increased when it is combined with Lumacaftor.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Velpatasvir.Approved, Investigational
MaprotilineThe serum concentration of Velpatasvir can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Velpatasvir can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Velpatasvir can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Velpatasvir can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Velpatasvir can be increased when it is combined with Meprobamate.Approved, Illicit
MethadoneThe serum concentration of Velpatasvir can be increased when it is combined with Methadone.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Velpatasvir.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Velpatasvir.Approved, Vet Approved
MetoprololThe serum concentration of Velpatasvir can be increased when it is combined with Metoprolol.Approved, Investigational
MibefradilThe serum concentration of Velpatasvir can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Velpatasvir can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Velpatasvir can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Velpatasvir can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Velpatasvir.Approved
MitomycinThe serum concentration of Velpatasvir can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Velpatasvir can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Velpatasvir can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MorphineThe serum concentration of Velpatasvir can be increased when it is combined with Morphine.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Velpatasvir.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Velpatasvir.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Velpatasvir.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Velpatasvir.Approved, Vet Approved
NaltrexoneThe serum concentration of Velpatasvir can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Velpatasvir can be increased when it is combined with Naringenin.Experimental
NefazodoneThe metabolism of Velpatasvir can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Velpatasvir can be decreased when combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Velpatasvir can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Velpatasvir can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Velpatasvir can be increased when combined with Nevirapine.Approved
NicardipineThe serum concentration of Velpatasvir can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Velpatasvir can be decreased when it is combined with Nifedipine.Approved
NilotinibThe metabolism of Velpatasvir can be decreased when combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Velpatasvir.Approved
NisoldipineThe serum concentration of Velpatasvir can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Velpatasvir can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Velpatasvir can be increased when it is combined with Nitrendipine.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Velpatasvir.Approved
NorethisteroneThe serum concentration of Velpatasvir can be decreased when it is combined with Norethisterone.Approved
OdanacatibThe serum concentration of Odanacatib can be increased when it is combined with Velpatasvir.Investigational
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Velpatasvir.Approved, Investigational
OlaparibThe metabolism of Velpatasvir can be decreased when combined with Olaparib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Velpatasvir.Approved
OmeprazoleThe serum concentration of Velpatasvir can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Velpatasvir can be increased when it is combined with Osimertinib.Approved
P-NitrophenolThe serum concentration of Velpatasvir can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Velpatasvir can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Velpatasvir can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Velpatasvir can be increased when it is combined with Palmitic Acid.Experimental
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Velpatasvir.Approved, Investigational
PantoprazoleThe serum concentration of Velpatasvir can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe serum concentration of Velpatasvir can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Velpatasvir.Approved
PentobarbitalThe metabolism of Velpatasvir can be increased when combined with Pentobarbital.Approved, Vet Approved
PerindoprilThe serum concentration of Velpatasvir can be increased when it is combined with Perindopril.Approved
PhenobarbitalThe metabolism of Velpatasvir can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Velpatasvir can be increased when combined with Phenytoin.Approved, Vet Approved
PibrentasvirThe serum concentration of Pibrentasvir can be increased when it is combined with Velpatasvir.Approved
PimozideThe serum concentration of Velpatasvir can be increased when it is combined with Pimozide.Approved
PioglitazoneThe metabolism of Velpatasvir can be decreased when combined with Pioglitazone.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Velpatasvir.Approved
Platelet Activating FactorThe serum concentration of Velpatasvir can be decreased when it is combined with Platelet Activating Factor.Experimental
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Velpatasvir.Approved
PonatinibThe serum concentration of Velpatasvir can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe metabolism of Velpatasvir can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Velpatasvir can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Velpatasvir can be increased when it is combined with Prazosin.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Velpatasvir.Approved, Vet Approved
PrednisoneThe serum concentration of Velpatasvir can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Velpatasvir can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Velpatasvir can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Velpatasvir can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Velpatasvir can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Velpatasvir can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Velpatasvir can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Velpatasvir can be increased when it is combined with Protriptyline.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Velpatasvir.Approved
QuazepamThe serum concentration of Velpatasvir can be increased when it is combined with Quazepam.Approved, Illicit
QuercetinThe serum concentration of Velpatasvir can be increased when it is combined with Quercetin.Experimental
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Velpatasvir.Approved
QuinacrineThe serum concentration of Velpatasvir can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Velpatasvir can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Velpatasvir can be increased when it is combined with Quinine.Approved
RabeprazoleThe metabolism of Velpatasvir can be decreased when combined with Rabeprazole.Approved, Investigational
RanitidineThe serum concentration of Velpatasvir can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Velpatasvir.Approved, Investigational
ReboxetineThe serum concentration of Velpatasvir can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Velpatasvir can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Velpatasvir can be decreased when it is combined with Reserpine.Approved
RifabutinThe metabolism of Velpatasvir can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Velpatasvir can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Velpatasvir can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Velpatasvir.Approved, Investigational
RilpivirineThe serum concentration of Velpatasvir can be increased when it is combined with Rilpivirine.Approved
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Velpatasvir.Approved, Investigational
RitonavirThe metabolism of Velpatasvir can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Velpatasvir.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Velpatasvir.Approved, Investigational
RosiglitazoneThe metabolism of Velpatasvir can be decreased when combined with Rosiglitazone.Approved, Investigational
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Velpatasvir.Approved, Vet Approved
SaquinavirThe metabolism of Velpatasvir can be decreased when combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Velpatasvir can be increased when it is combined with Scopolamine.Approved
SecobarbitalThe metabolism of Velpatasvir can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe serum concentration of Velpatasvir can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Velpatasvir.Approved
SertralineThe serum concentration of Velpatasvir can be increased when it is combined with Sertraline.Approved
SildenafilThe metabolism of Velpatasvir can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Velpatasvir.Approved
SiltuximabThe serum concentration of Velpatasvir can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Velpatasvir can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Velpatasvir can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Velpatasvir can be decreased when it is combined with Sirolimus.Approved, Investigational
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Velpatasvir.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Velpatasvir.Approved
SorafenibThe serum concentration of Velpatasvir can be increased when it is combined with Sorafenib.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Velpatasvir.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Velpatasvir.Experimental
SpironolactoneThe serum concentration of Velpatasvir can be increased when it is combined with Spironolactone.Approved
St. John's WortThe serum concentration of Velpatasvir can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Velpatasvir can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Velpatasvir can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Velpatasvir can be decreased when it is combined with Streptozocin.Approved
SulfamethoxazoleThe metabolism of Velpatasvir can be decreased when combined with Sulfamethoxazole.Approved
SulfinpyrazoneThe serum concentration of Velpatasvir can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Velpatasvir can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Velpatasvir can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Velpatasvir can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Velpatasvir can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Velpatasvir can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Velpatasvir can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Velpatasvir can be increased when it is combined with Taurocholic Acid.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Velpatasvir.Approved
TelaprevirThe metabolism of Velpatasvir can be decreased when combined with Telaprevir.Withdrawn
TelithromycinThe metabolism of Velpatasvir can be decreased when combined with Telithromycin.Approved
TelmisartanThe serum concentration of Velpatasvir can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Velpatasvir can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Velpatasvir can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Velpatasvir can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Velpatasvir can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Velpatasvir can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Velpatasvir can be increased when it is combined with Testosterone.Approved, Investigational
ThiotepaThe metabolism of Velpatasvir can be decreased when combined with Thiotepa.Approved
TicagrelorThe serum concentration of Velpatasvir can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Velpatasvir can be decreased when combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Velpatasvir.Approved
TocilizumabThe serum concentration of Velpatasvir can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Velpatasvir can be increased when it is combined with Tolvaptan.Approved
TopiroxostatThe metabolism of Velpatasvir can be decreased when combined with Topiroxostat.Approved
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Velpatasvir.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Velpatasvir.Approved
TrazodoneThe serum concentration of Velpatasvir can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Velpatasvir can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Velpatasvir can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Velpatasvir can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Velpatasvir can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Velpatasvir can be increased when it is combined with Troleandomycin.Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Velpatasvir.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Velpatasvir.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Velpatasvir.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Velpatasvir.Approved
VenlafaxineThe metabolism of Velpatasvir can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Velpatasvir can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Velpatasvir can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Velpatasvir.Approved, Investigational
VincristineThe serum concentration of Velpatasvir can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Velpatasvir can be increased when it is combined with Vinorelbine.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Velpatasvir.Approved
VoriconazoleThe metabolism of Velpatasvir can be decreased when combined with Voriconazole.Approved, Investigational
VoxilaprevirThe serum concentration of Voxilaprevir can be increased when it is combined with Velpatasvir.Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Velpatasvir.Approved
ZimelidineThe serum concentration of Velpatasvir can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Velpatasvir can be decreased when combined with Ziprasidone.Approved
Food Interactions
Not Available

References

Synthesis Reference
Not Available
General References
  1. Ascher DB, Wielens J, Nero TL, Doughty L, Morton CJ, Parker MW: Potent hepatitis C inhibitors bind directly to NS5A and reduce its affinity for RNA. Sci Rep. 2014 Apr 23;4:4765. doi: 10.1038/srep04765. [PubMed:24755925 ]
  2. Targett-Adams P, Graham EJ, Middleton J, Palmer A, Shaw SM, Lavender H, Brain P, Tran TD, Jones LH, Wakenhut F, Stammen B, Pryde D, Pickford C, Westby M: Small molecules targeting hepatitis C virus-encoded NS5A cause subcellular redistribution of their target: insights into compound modes of action. J Virol. 2011 Jul;85(13):6353-68. doi: 10.1128/JVI.00215-11. Epub 2011 Apr 20. [PubMed:21507963 ]
  3. Mogalian E, German P, Kearney BP, Yang CY, Brainard D, Link J, McNally J, Han L, Ling J, Mathias A: Preclinical Pharmacokinetics and First-in-Human Pharmacokinetics, Safety, and Tolerability of Velpatasvir, a Pangenotypic Hepatitis C Virus NS5A Inhibitor, in Healthy Subjects. Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02084-16. doi: 10.1128/AAC.02084-16. Print 2017 May. [PubMed:28193657 ]
  4. Lawitz E, Freilich B, Link J, German P, Mo H, Han L, Brainard DM, McNally J, Marbury T, Rodriguez-Torres M: A phase 1, randomized, dose-ranging study of GS-5816, a once-daily NS5A inhibitor, in patients with genotype 1-4 hepatitis C virus. J Viral Hepat. 2015 Dec;22(12):1011-9. doi: 10.1111/jvh.12435. Epub 2015 Jul 16. [PubMed:26183611 ]
  5. Myers RP, Shah H, Burak KW, Cooper C, Feld JJ: An update on the management of chronic hepatitis C: 2015 Consensus guidelines from the Canadian Association for the Study of the Liver. Can J Gastroenterol Hepatol. 2015 Jan-Feb;29(1):19-34. Epub 2015 Jan 13. [PubMed:25585348 ]
  6. Lawitz EJ, Dvory-Sobol H, Doehle BP, Worth AS, McNally J, Brainard DM, Link JO, Miller MD, Mo H: Clinical Resistance to Velpatasvir (GS-5816), a Novel Pan-Genotypic Inhibitor of the Hepatitis C Virus NS5A Protein. Antimicrob Agents Chemother. 2016 Aug 22;60(9):5368-78. doi: 10.1128/AAC.00763-16. Print 2016 Sep. [PubMed:27353271 ]
  7. Epclusa FDA Approval Announcement [Link]
  8. American Association for the Study of Liver Diseases; Infectious Diseases Society of America. HCV guidance. http://hcvguidelines.org. Accessed June 12, 2017. [Link]
External Links
KEGG Drug
D10806
ChemSpider
34501056
ChEBI
133009
ChEMBL
CHEMBL3545062
PharmGKB
PA166163415
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Velpatasvir
ATC Codes
Not Available
AHFS Codes
Not Available
PDB Entries
Not Available
FDA label
Download (338 KB)
MSDS
Download (243 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingTreatmentChronic Hepatitis C Infection / Lung Transplant Infection1
0RecruitingTreatmentChronic Hepatitis C Infection / Transplant, Kidney1
1CompletedTreatmentChronic Hepatitis C Virus1
1CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection1
1CompletedTreatmentHepatitis C Virus (HCV)1
1CompletedTreatmentHepatitis C Virus Infection1
2Active Not RecruitingTreatmentHepatitis C Virus Infection1
2CompletedTreatmentChronic Hepatitis C Infection2
2CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection2
2CompletedTreatmentHepatitis C Virus Infection5
2RecruitingTreatmentChronic Hepatitis C Infection1
2RecruitingTreatmentChronic Hepatitis C Virus (HCV) Infection3
2RecruitingTreatmentHepatitis C Virus Infection3
3Active Not RecruitingTreatmentChronic Hepatitis C Infection1
3Active Not RecruitingTreatmentHepatitis C Virus Infection3
3CompletedTreatmentChronic Hepatitis C Infection1
3CompletedTreatmentHepatitis C Virus Infection10
3Enrolling by InvitationTreatmentHepatitis C Virus Infection1
4CompletedTreatmentHepatitis C Virus Infection, Response to Therapy of / Human Immunodeficiency Virus (HIV)1
4Enrolling by InvitationTreatmentHepatitis C, Chronic1
4Not Yet RecruitingHealth Services ResearchHepatitis C, Chronic / Opioid-use Disorder1
4Not Yet RecruitingPreventionChronic Hepatitis C Infection / End Stage Liver Diseases1
4Not Yet RecruitingTreatmentChronic Hepatitis C Infection / Hepatitis C, Chronic / Opiate Dependence1
4Not Yet RecruitingTreatmentHepatitis C, Chronic / Lung Transplant1
4RecruitingTreatmentAwaiting Organ Transplant / Chronic Hepatitis C Infection1
4RecruitingTreatmentChronic Hepatitis C Infection1
4RecruitingTreatmentChronic Hepatitis C Infection / Thalassaemic disorders1
4RecruitingTreatmentHCV Coinfection / Human Immunodeficiency Virus (HIV) / Liver Diseases1
Not AvailableEnrolling by InvitationNot AvailableChronic Hepatitis C Infection1
Not AvailableNot Yet RecruitingTreatmentCardiac Transplant / Chronic Hepatitis C Infection1
Not AvailableRecruitingNot AvailableChronic Hepatitis C Infection1
Not AvailableRecruitingNot AvailableHepatitis C, Chronic / Human Immunodeficiency Virus (HIV)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral
Tablet, film coatedOral
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7964580 No2009-03-262029-03-26Us
US8334270 No2008-03-212028-03-21Us
US8633309 No2009-03-262029-03-26Us
US8618076 No2010-12-112030-12-11Us
US8735372 No2008-03-212028-03-21Us
US8580765 No2008-03-212028-03-21Us
US8889159 No2009-03-262029-03-26Us
US9085573 No2008-03-212028-03-21Us
US9284342 No2010-09-132030-09-13Us
US8940718 No2012-11-162032-11-16Us
US8575135 No2012-11-162032-11-16Us
US8921341 No2012-11-162032-11-16Us
US9585906 No2008-03-212028-03-21Us
US9296782 No2014-07-172034-07-17Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00153 mg/mLALOGPS
logP5.65ALOGPS
logP4.26ChemAxon
logS-5.8ALOGPS
pKa (Strongest Acidic)3.74ChemAxon
pKa (Strongest Basic)5.98ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count12ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area200.08 Å2ChemAxon
Rotatable Bond Count13ChemAxon
Refractivity242.15 m3·mol-1ChemAxon
Polarizability97.91 Å3ChemAxon
Number of Rings9ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as naphthopyrans. These are compounds containing a pyran ring fused to a naphthalene moiety. Furan is a 6 membered-ring non-aromatic ring with five carbon and one oxygen atoms. Naphthalene is a polycyclic aromatic hydrocarbon made up of two fused benzene rings.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Naphthopyrans
Sub Class
Not Available
Direct Parent
Naphthopyrans
Alternative Parents
Dibenzopyrans / Valine and derivatives / Alpha amino acid amides / Phenylacetamides / 2-benzopyrans / Naphthalenes / Benzimidazoles / N-acylpyrrolidines / Alkyl aryl ethers / Pyrans
show 12 more
Substituents
Naphthopyran / Dibenzopyran / Valine or derivatives / Alpha-amino acid amide / Naphthalene / Phenylacetamide / 1-benzopyran / 2-benzopyran / Benzopyran / Alpha-amino acid or derivatives
show 28 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

1. Nonstructural Protein 5A (NS5A)
Kind
Protein
Organism
Hepatitis C Virus (HCV)
Pharmacological action
Yes
Actions
Inhibitor

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
Transporter
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
Transporter
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
Transporter
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name
SLCO2B1
Uniprot ID
O94956
Uniprot Name
Solute carrier organic anion transporter family member 2B1
Molecular Weight
76709.98 Da

Drug created on August 05, 2016 17:48 / Updated on October 02, 2017 06:20