Identification

Name
Glecaprevir
Accession Number
DB13879
Type
Small Molecule
Groups
Approved
Description

Glecaprevir is a direct acting antiviral agent and Hepatitis C virus (HCV) NS3/4A protease inhibitor that targets the the viral RNA replication. In combination with Pibrentasvir, glecaprevir is a useful therapy for patients who experienced therapeutic failure from other NS3/4A protease inhibitors. It demonstrates a high genetic barrier against resistance mutations of the virus. In cell cultures, the emergence of amino acid substitutions at NS3 resistance-associated positions A156 or D/Q168 in HCV genotype 1a, 2a or 3a replicons led to reduced susceptibility to glecaprevir [FDA Label]. The combinations of amino acid substitutions at NS3 position Y65H and D/Q168 also results in greater reductions in glecaprevir susceptibility, and NS3 Q80R in genotype 3a patients also leads to glecaprevir resistance [FDA Label].

Glecaprevir is available as an oral combination therapy with Pibrentasvir under the brand name Mavyret. This fixed-dose combination therapy was FDA-approved in August 2017 to treat adults with chronic hepatitis C virus (HCV) genotypes 1-6 without cirrhosis (liver disease) or with mild cirrhosis, including patients with moderate to severe kidney disease and those who are on dialysis [2]. Mavyret is also indicated for HCV genotype 1-infected patients who have been previously treated with regimens either containing an NS5A inhibitor or an NS3/4A protease inhibitor, but not both [2]. Hepatitis C viral infection often leads to decreased liver function and subsequent liver failure, causing a significantly negative impact on the patients' quality of life. The ultimate goal of the combination treatment is to achieve sustained virologic response (SVR) and cure the patients from the infection. In clinical trials, this combination therapy achieved SVR12 rate, or undetectable Hepatitis C for twelve or more weeks after the end of treatment, of ≥93% across genotypes 1a, 2a, 3a, 4, 5 and 6 [FDA Label].

Structure
Thumb
Synonyms
  • (3aR,7S,10S,12R,21E,24aR)-7-tert-butyl-N-{(1R,2R)-2­ (difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl}-20,20-difluoro­ 5,8-dioxo-2,3,3a,5,6,7,8,11,12,20,23,24a-dodecahydro-1H,10H-9,12­ methanocyclopenta[18,19][1,10,17,3,6]trioxadiazacyclononadecino[11,12-b]quinoxaline-10­ carboxamide hydrate
  • Glécaprévir
  • glecaprevirum
External IDs
A-1282576 / A-1282576.0 / A-12825760 / ABT-493
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
MaviretGlecaprevir (100 mg) + Pibrentasvir (40 mg)TabletOralAbbvieNot applicableNot applicableCanada
MavyretGlecaprevir (100 mg/1) + Pibrentasvir (40 mg/1)Tablet, film coatedOralAbbvie2017-08-03Not applicableUs
Categories
UNII
K6BUU8J72P
CAS number
1365970-03-1
Weight
Average: 838.87
Monoisotopic: 838.298310911
Chemical Formula
C38H46F4N6O9S
InChI Key
MLSQGNCUYAMAHD-ITNVBOSISA-N
InChI
InChI=1S/C38H46F4N6O9S/c1-35(2,3)28-32(50)48-19-20(17-24(48)30(49)46-37(18-21(37)29(39)40)33(51)47-58(53,54)36(4)14-15-36)56-31-27(43-22-9-5-6-10-23(22)44-31)38(41,42)13-8-16-55-25-11-7-12-26(25)57-34(52)45-28/h5-6,8-10,13,20-21,24-26,28-29H,7,11-12,14-19H2,1-4H3,(H,45,52)(H,46,49)(H,47,51)/b13-8+/t20-,21+,24+,25-,26-,28-,37-/m1/s1
IUPAC Name
(1R,14E,18R,22R,26S,29S)-26-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-13,13-difluoro-24,27-dioxo-2,17,23-trioxa-4,11,25,28-tetraazapentacyclo[26.2.1.0^{3,12}.0^{5,10}.0^{18,22}]hentriaconta-3,5(10),6,8,11,14-hexaene-29-carboxamide
SMILES
CC(C)(C)[[email protected]@H]1NC(=O)O[[email protected]@H]2CCC[[email protected]]2OC\C=C\C(F)(F)C2=NC3=C(C=CC=C3)N=C2O[[email protected]@H]2C[[email protected]](N(C2)C1=O)C(=O)N[[email protected]@]1(C[[email protected]]1C(F)F)C(=O)NS(=O)(=O)C1(C)CC1

Pharmacology

Indication

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 (Child-Pugh A). MAVYRET is also indicated for the treatment of adult patients with HCV genotype 1 infection, who previously have been treated with a regimen containing an HCV NS5A inhibitor or an NS3/4A protease inhibitor (PI), but not both [FDA Label].

Structured Indications
Not Available
Pharmacodynamics

In a biochemical assay studying clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a, glecaprevir displayed IC50 values ranging from 3.5 to 11.3 nM that resulted in inhibition of the proteolytic activity of recombinant NS3/4A enzymes. In HCV replicon assays, glecaprevir had median EC50 values of 0.08-4.6 nM against laboratory and clinical isolates from subtypes 1a, 1b, 2a, 2b, 3a, 4a, 4d, 5a, and 6a [FDA Label]. In a QT study, glecaprevir is not shown to prolong the QTc interval.

Mechanism of action

Glecaprevir is an inhibitor of the HCV NS3/4A protease, which is a viral enzyme necessary for the proteolytic cleavage of the HCV encoded polyprotein into mature forms of the NS3, NS4A, NS4B, NS5A, and NS5B proteins [FDA Label]. These multifunctional proteins, including NS3, are essential for viral replication. The N-terminal of NS3 protein confers serine protease activity, whileThe C-terminus of NS3 encodes a DExH/D-box RNA helicase which hydyolyzes NTP as an energy source to unwind double-stranded RNA in a 3′ to 5′ direction during replication of viral genomic RNA [1]. NS4A is a cofactor for NS3 that directs the localization of NS3 and modulates its enzymatic activities [1]. Glecaprevir disrupts the intracellular processes of the viral life cycle through inhibiting the NS3/4A protease activity of cleaving downstream junctions of HCV polypeptide and proteolytic processing of mature structural proteins [1].

TargetActionsOrganism
ANS3 protease
inhibitor
Hepatitis C virus
Absorption

In healthy subjects, the time it takes to reach the peak plasma concentration (Tmax) is approximately 5 hours. The mean peak plasma concentration (Cmax) is 597ng/mL in non-cirrhotic HCV-infected subjects. Relative to fasting conditions, the consumption of meals increases the absorption of glecaprevir by 83-163% [FDA Label].

Volume of distribution
Not Available
Protein binding

Pibrentasvir is 97.5% bound to human plasma proteins. The Blood-to-plasma ratio is approximately 0.57 [FDA Label].

Metabolism

Glecaprevir undergoes limited secondary metabolism in vitro, predominantly by CYP3A [FDA Label].

Route of elimination

The predominant route of elimination of the drug is biliary-fecal, where 92.1% of administered drug is excreted in feces and 0.7% of the drug is excreted in the urine [FDA Label].

Half life

The elimination half life (t1/2) is approximately 6 hours [FDA Label].

Clearance
Not Available
Toxicity

Glecaprevir is not shown to be genotoxic according to in vitro or in vivo studies. It also shows to have no effect on mating, female or male fertility, or early embryonic development in rodent studies. Carcinogenicity studies with glecaprevir have not been conducted [FDA Label].

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

Interactions

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

References

General References
  1. Salam KA, Akimitsu N: Hepatitis C virus NS3 inhibitors: current and future perspectives. Biomed Res Int. 2013;2013:467869. doi: 10.1155/2013/467869. Epub 2013 Oct 27. [PubMed:24282816]
  2. FDA Press Announcements: FDA approves Mavyret for Hepatitis C [Link]
External Links
KEGG Drug
D10814
ChemSpider
35013015
ChEMBL
CHEMBL3545363
Wikipedia
Glecaprevir
AHFS Codes
  • 08:18.40.20 — HCV Protease Inhibitors
  • 08:18.40.24 — HCV Replication Complex Inhibitors
FDA label
Download (925 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceHepatic Impairment1
1CompletedBasic ScienceImpaired Renal Function1
2CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / HCV / Hepatitis C Virus (HCV)2
2CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Compensated liver disease / Hepatitis C Virus (HCV)1
2Enrolling by InvitationDiagnosticChronic Hepatitis C Infection1
2, 3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Hepatitis C Virus (HCV)1
3Active Not RecruitingTreatmentChronic Hepatitis C Virus (HCV) Infection / Compensated Cirrhosis and Non-cirrhotics / Hepatitis C Virus Infection / Human Immunodeficiency Virus (HIV) Infections1
3Active Not RecruitingTreatmentChronic Hepatitis C Virus / Hepatitis C Virus (HCV)1
3Active Not RecruitingTreatmentHepatitis C, Acute1
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection2
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Genotype 3 Hepatitis C Virus / Hepatitis C Virus (HCV)1
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / HCV / Hepatitis C Virus (HCV)2
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Compensated liver disease / Hepatitis C Virus Infection1
3CompletedTreatmentChronic Hepatitis C Virus / Hepatitis C Virus (HCV)1
3CompletedTreatmentHepatitis C Virus (HCV)1
3Enrolling by InvitationTreatmentHepatitis C Virus Infection1
3Not Yet RecruitingTreatmentHepatitis C Virus (HCV)2
3RecruitingTreatmentChronic Hepatitis C Infection / HCV1
3RecruitingTreatmentChronic Hepatitis C Virus (HCV)1
3RecruitingTreatmentChronic Hepatitis C Virus (HCV) Genotype 5 or 6 Infection1
3RecruitingTreatmentHepatitis C Virus (HCV)4
Not AvailableAvailableNot AvailableHepatitis C Virus Infection1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral
Tablet, film coatedOral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility<0.1 to 0.3 mg/mLFDA Label
Predicted Properties
PropertyValueSource
Water Solubility0.0463 mg/mLALOGPS
logP4.26ALOGPS
logP3.95ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)3.74ChemAxon
pKa (Strongest Basic)-1.2ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count10ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area195.22 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity194.55 m3·mol-1ChemAxon
Polarizability80.16 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as cyclic peptides. These are compounds containing a cyclic moiety bearing a peptide backbone.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Cyclic peptides
Alternative Parents
Macrolactams / N-acyl-alpha amino acids and derivatives / Alpha amino acid amides / Quinoxalines / Pyrrolidinecarboxamides / Alkyl aryl ethers / Pyrazines / Benzenoids / Cyclopropanecarboxylic acids and derivatives / Tertiary carboxylic acid amides
show 16 more
Substituents
Cyclic alpha peptide / Macrolactam / N-acyl-alpha amino acid or derivatives / Alpha-amino acid amide / Diazanaphthalene / Alpha-amino acid or derivatives / Quinoxaline / Pyrrolidine carboxylic acid or derivatives / Pyrrolidine-2-carboxamide / Alkyl aryl ether
show 33 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Hepatitis C virus
Pharmacological action
Yes
Actions
Inhibitor
General Function
Serine-type peptidase activity
Specific Function
Not Available
Gene Name
Not Available
Uniprot ID
Q91RS4
Uniprot Name
NS3 protease
Molecular Weight
19113.77 Da

Enzymes

Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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...

Components:
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
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
Unknown
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
Unknown
Actions
Substrate
Inhibitor
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
Unknown
Actions
Substrate
Inhibitor
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

Drug created on August 31, 2017 09:33 / Updated on October 21, 2017 19:35