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Identification
NameAmprenavir
Accession NumberDB00701  (APRD00605)
TypeSmall Molecule
GroupsApproved
DescriptionAmprenavir is a protease inhibitor used to treat HIV infection.
Structure
Thumb
Synonyms
(3S)-Tetrahydro-3-furanyl ((1S,2R)-3-(((4-aminophenyl)sulfonyl)(2-methylpropyl)amino)-2-hydroxy-1-(phenylmethyl)propyl)carbamate
Agenerase
Amprenavir
Amprénavir
Amprenavirum
External Identifiers
  • 141 W 94
  • KVX 478
  • VX-478
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Agenerasecapsule50 mgoralGlaxosmithkline Inc2001-03-212008-05-27Canada
Agenerasecapsule150 mgoralGlaxosmithkline Inc2001-03-162008-05-27Canada
Ageneraseliquid15 mgoralGlaxosmithkline Inc2001-03-262008-05-27Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AgeneraseCapsule, soft50 mgOral useGlaxo Group Ltd.2000-10-20Not applicableEu
AgeneraseCapsule, soft150 mgOral useGlaxo Group Ltd.2000-10-20Not applicableEu
AgeneraseCapsule, soft150 mgOral useGlaxo Group Ltd.2000-10-20Not applicableEu
AgeneraseOral solution15 mg/mlOral useGlaxo Group Ltd.2000-10-20Not applicableEu
International Brands
NameCompany
AgemeraseGlaxoSmithKline
ProzeiKissei Pharmaceuticals Co., Ltd.
Brand mixturesNot Available
SaltsNot Available
Categories
UNII5S0W860XNR
CAS number161814-49-9
WeightAverage: 505.627
Monoisotopic: 505.224656557
Chemical FormulaC25H35N3O6S
InChI KeyInChIKey=YMARZQAQMVYCKC-OEMFJLHTSA-N
InChI
InChI=1S/C25H35N3O6S/c1-18(2)15-28(35(31,32)22-10-8-20(26)9-11-22)16-24(29)23(14-19-6-4-3-5-7-19)27-25(30)34-21-12-13-33-17-21/h3-11,18,21,23-24,29H,12-17,26H2,1-2H3,(H,27,30)/t21-,23-,24+/m0/s1
IUPAC Name
(3S)-oxolan-3-yl N-[(2S,3R)-3-hydroxy-4-[N-(2-methylpropyl)4-aminobenzenesulfonamido]-1-phenylbutan-2-yl]carbamate
SMILES
CC(C)CN(C[C@@H](O)[[email protected]](CC1=CC=CC=C1)NC(=O)O[[email protected]]1CCOC1)S(=O)(=O)C1=CC=C(N)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as aminobenzenesulfonamides. These are organic compounds containing a benzenesulfonamide moiety with an amine group attached to the benzene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzenesulfonamides
Direct ParentAminobenzenesulfonamides
Alternative Parents
Substituents
  • Phenylbutylamine
  • Aminobenzenesulfonamide
  • Sulfonylaniline
  • Amphetamine or derivatives
  • Substituted aniline
  • Aniline
  • Primary aromatic amine
  • Saccharide
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Oxolane
  • Secondary alcohol
  • Oxacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Ether
  • Dialkyl ether
  • Hydrocarbon derivative
  • Primary amine
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of HIV-1 infection in combination with other antiretroviral agents.
PharmacodynamicsAmprenavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Amprenavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.
Mechanism of actionAmprenavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
Related Articles
AbsorptionRapidly absorbed after oral administration in HIV-1-infected patients with a time to peak concentration (Tmax) typically between 1 and 2 hours after a single oral dose. The absolute oral bioavailability of amprenavir in humans has not been established.
Volume of distributionNot Available
Protein bindingVery high (90%). Amprenavir has the highest affinity for alpha(1)-acid glycoprotein.
Metabolism

Hepatic. Amprenavir is metabolized in the liver by the cytochrome P450 3A4 (CYP3A4) enzyme system. The 2 major metabolites result from oxidation of the tetrahydrofuran and aniline moieties. Glucuronide conjugates of oxidized metabolites have been identified as minor metabolites in urine and feces.

Route of eliminationNot Available
Half life7.1-10.6 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Human Immunodeficiency Virus
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9132
Blood Brain Barrier-0.5886
Caco-2 permeable+0.8866
P-glycoprotein substrateSubstrate0.7175
P-glycoprotein inhibitor IInhibitor0.7973
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterNon-inhibitor0.8815
CYP450 2C9 substrateNon-substrate0.5
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateSubstrate0.6176
CYP450 1A2 substrateNon-inhibitor0.7641
CYP450 2C9 inhibitorNon-inhibitor0.6591
CYP450 2D6 inhibitorNon-inhibitor0.8821
CYP450 2C19 inhibitorNon-inhibitor0.6641
CYP450 3A4 inhibitorInhibitor0.6185
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7229
Ames testNon AMES toxic0.6097
CarcinogenicityNon-carcinogens0.8218
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.4787 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9884
hERG inhibition (predictor II)Non-inhibitor0.8733
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Glaxosmithkline
Packagers
Dosage forms
FormRouteStrength
Capsuleoral150 mg
Capsuleoral50 mg
Capsule, softOral use150 mg
Capsule, softOral use50 mg
Liquidoral15 mg
Oral solutionOral use15 mg/ml
Prices
Unit descriptionCostUnit
Agenerase 50 mg capsule0.65USD capsule
Agenerase 15 mg/ml Solution0.21USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5585397 No1993-12-172013-12-17Us
US6730679 No1997-11-112017-11-11Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0491 mg/mLALOGPS
logP1.85ALOGPS
logP2.43ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)13.61ChemAxon
pKa (Strongest Basic)2.39ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area131.19 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity134.08 m3·mol-1ChemAxon
Polarizability53.6 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

DrugSyn.org

US5585397
General ReferencesNot Available
External Links
ATC CodesJ05AE05
AHFS Codes
  • 08:18.08.08
PDB Entries
FDA labelDownload (120 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Amprenavir.
AbirateroneThe serum concentration of Amprenavir can be increased when it is combined with Abiraterone.
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Amprenavir.
AcetaminophenThe serum concentration of Acetaminophen can be decreased when it is combined with Amprenavir.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be decreased when it is combined with Amprenavir.
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Amprenavir.
AldosteroneThe serum concentration of Aldosterone can be decreased when it is combined with Amprenavir.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Amprenavir.
AlitretinoinThe serum concentration of Alitretinoin can be decreased when it is combined with Amprenavir.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Amprenavir.
AmbrisentanThe serum concentration of Ambrisentan can be decreased when it is combined with Amprenavir.
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Amprenavir.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Amprenavir.
AmiodaroneThe metabolism of Amprenavir can be decreased when combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Amprenavir.
ApixabanThe serum concentration of Apixaban can be decreased when it is combined with Amprenavir.
AprepitantThe serum concentration of Amprenavir can be increased when it is combined with Aprepitant.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be decreased when it is combined with Amprenavir.
ArtemetherThe metabolism of Amprenavir can be decreased when combined with Artemether.
AtazanavirThe metabolism of Amprenavir can be decreased when combined with Atazanavir.
AtazanavirThe serum concentration of Atazanavir can be decreased when it is combined with Amprenavir.
AtenololThe serum concentration of Atenolol can be decreased when it is combined with Amprenavir.
AtomoxetineThe metabolism of Amprenavir can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Amprenavir.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Amprenavir.
BetamethasoneThe serum concentration of Betamethasone can be decreased when it is combined with Amprenavir.
BetaxololThe metabolism of Amprenavir can be decreased when combined with Betaxolol.
BexaroteneThe serum concentration of Amprenavir can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Amprenavir can be decreased when it is combined with Boceprevir.
BortezomibThe metabolism of Amprenavir can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Amprenavir can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Amprenavir.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Amprenavir.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Amprenavir.
BupropionThe metabolism of Amprenavir can be decreased when combined with Bupropion.
CabazitaxelThe serum concentration of Cabazitaxel can be decreased when it is combined with Amprenavir.
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Amprenavir.
CaffeineThe serum concentration of Caffeine can be decreased when it is combined with Amprenavir.
CamptothecinThe serum concentration of Camptothecin can be decreased when it is combined with Amprenavir.
CanagliflozinThe serum concentration of Canagliflozin can be decreased when it is combined with Amprenavir.
CapecitabineThe metabolism of Amprenavir can be decreased when combined with Capecitabine.
CarbamazepineThe metabolism of Amprenavir can be increased when combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be decreased when it is combined with Amprenavir.
CarfilzomibThe serum concentration of Carfilzomib can be decreased when it is combined with Amprenavir.
CelecoxibThe metabolism of Amprenavir can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Amprenavir can be increased when it is combined with Ceritinib.
CeritinibThe serum concentration of Ceritinib can be decreased when it is combined with Amprenavir.
CerivastatinThe serum concentration of Cerivastatin can be decreased when it is combined with Amprenavir.
ChloroquineThe metabolism of Amprenavir can be decreased when combined with Chloroquine.
ChlorpromazineThe serum concentration of Chlorpromazine can be decreased when it is combined with Amprenavir.
ChlorpromazineThe metabolism of Amprenavir can be decreased when combined with Chlorpromazine.
CholecalciferolThe metabolism of Amprenavir can be decreased when combined with Cholecalciferol.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Amprenavir.
CimetidineThe serum concentration of Cimetidine can be decreased when it is combined with Amprenavir.
CimetidineThe metabolism of Amprenavir can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Amprenavir can be decreased when combined with Cinacalcet.
CiprofloxacinThe serum concentration of Ciprofloxacin can be decreased when it is combined with Amprenavir.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Amprenavir.
CisplatinThe serum concentration of Cisplatin can be decreased when it is combined with Amprenavir.
CitalopramThe serum concentration of Citalopram can be decreased when it is combined with Amprenavir.
CitalopramThe metabolism of Amprenavir can be decreased when combined with Citalopram.
ClarithromycinThe metabolism of Amprenavir can be decreased when combined with Clarithromycin.
ClarithromycinThe serum concentration of Clarithromycin can be decreased when it is combined with Amprenavir.
ClemastineThe metabolism of Amprenavir can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be decreased when it is combined with Amprenavir.
ClobazamThe metabolism of Amprenavir can be decreased when combined with Clobazam.
ClomifeneThe serum concentration of Clomifene can be decreased when it is combined with Amprenavir.
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Amprenavir.
ClomipramineThe metabolism of Amprenavir can be decreased when combined with Clomipramine.
ClonidineThe serum concentration of Clonidine can be decreased when it is combined with Amprenavir.
ClopidogrelThe serum concentration of Clopidogrel can be decreased when it is combined with Amprenavir.
ClopidogrelThe metabolism of Amprenavir can be decreased when combined with Clopidogrel.
ClotrimazoleThe metabolism of Amprenavir can be decreased when combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be decreased when it is combined with Amprenavir.
ClozapineThe metabolism of Amprenavir can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Amprenavir can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be decreased when it is combined with Amprenavir.
CocaineThe metabolism of Amprenavir can be decreased when combined with Cocaine.
ColchicineThe serum concentration of Colchicine can be decreased when it is combined with Amprenavir.
ConivaptanThe serum concentration of Amprenavir can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Amprenavir.
CrizotinibThe metabolism of Amprenavir can be decreased when combined with Crizotinib.
CrizotinibThe serum concentration of Crizotinib can be decreased when it is combined with Amprenavir.
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Amprenavir.
CyclophosphamideThe risk or severity of adverse effects can be increased when Amprenavir is combined with Cyclophosphamide.
CyclosporineThe metabolism of Amprenavir can be decreased when combined with Cyclosporine.
CyclosporineThe serum concentration of Cyclosporine can be decreased when it is combined with Amprenavir.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Amprenavir.
DabrafenibThe serum concentration of Amprenavir can be decreased when it is combined with Dabrafenib.
DactinomycinThe serum concentration of Dactinomycin can be decreased when it is combined with Amprenavir.
DapagliflozinThe serum concentration of Dapagliflozin can be decreased when it is combined with Amprenavir.
DarifenacinThe metabolism of Amprenavir can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Amprenavir can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Amprenavir can be increased when it is combined with Dasatinib.
DasatinibThe serum concentration of Dasatinib can be decreased when it is combined with Amprenavir.
DaunorubicinThe serum concentration of Daunorubicin can be decreased when it is combined with Amprenavir.
DebrisoquinThe serum concentration of Debrisoquin can be decreased when it is combined with Amprenavir.
DeferasiroxThe serum concentration of Amprenavir can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Amprenavir.
DelavirdineThe metabolism of Amprenavir can be decreased when combined with Delavirdine.
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Amprenavir.
DesipramineThe metabolism of Amprenavir can be decreased when combined with Desipramine.
DexamethasoneThe serum concentration of Amprenavir can be decreased when it is combined with Dexamethasone.
DiazepamThe serum concentration of Diazepam can be decreased when it is combined with Amprenavir.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Amprenavir.
DigitoxinThe serum concentration of Digitoxin can be decreased when it is combined with Amprenavir.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Amprenavir.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Amprenavir.
DihydroergotamineThe metabolism of Amprenavir can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be decreased when it is combined with Amprenavir.
DiltiazemThe metabolism of Amprenavir can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be decreased when it is combined with Amprenavir.
DiphenhydramineThe metabolism of Amprenavir can be decreased when combined with Diphenhydramine.
DipyridamoleThe serum concentration of Dipyridamole can be decreased when it is combined with Amprenavir.
DocetaxelThe serum concentration of Docetaxel can be decreased when it is combined with Amprenavir.
DomperidoneThe serum concentration of Domperidone can be decreased when it is combined with Amprenavir.
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Amprenavir.
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Amprenavir.
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Amprenavir.
DoxycyclineThe metabolism of Amprenavir can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Amprenavir can be decreased when combined with Dronedarone.
DuloxetineThe metabolism of Amprenavir can be decreased when combined with Duloxetine.
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Amprenavir.
EdoxabanThe serum concentration of Edoxaban can be decreased when it is combined with Amprenavir.
EfavirenzThe serum concentration of Amprenavir can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Eletriptan can be decreased when it is combined with Amprenavir.
EliglustatThe metabolism of Amprenavir can be decreased when combined with Eliglustat.
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Amprenavir.
EnzalutamideThe serum concentration of Amprenavir can be decreased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Epinastine can be decreased when it is combined with Amprenavir.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Amprenavir.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Amprenavir.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Amprenavir.
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Amprenavir.
ErythromycinThe metabolism of Amprenavir can be decreased when combined with Erythromycin.
ErythromycinThe serum concentration of Erythromycin can be decreased when it is combined with Amprenavir.
Eslicarbazepine acetateThe serum concentration of Amprenavir can be decreased when it is combined with Eslicarbazepine acetate.
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Amprenavir.
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Amprenavir.
EstriolThe serum concentration of Estriol can be decreased when it is combined with Amprenavir.
EstroneThe serum concentration of Estrone can be decreased when it is combined with Amprenavir.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Amprenavir.
EtoposideThe serum concentration of Etoposide can be decreased when it is combined with Amprenavir.
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Amprenavir.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Amprenavir.
EzetimibeThe serum concentration of Ezetimibe can be decreased when it is combined with Amprenavir.
FelodipineThe metabolism of Amprenavir can be decreased when combined with Felodipine.
FesoterodineThe serum concentration of Fesoterodine can be decreased when it is combined with Amprenavir.
FexofenadineThe serum concentration of Fexofenadine can be decreased when it is combined with Amprenavir.
FidaxomicinThe serum concentration of Fidaxomicin can be decreased when it is combined with Amprenavir.
FloxuridineThe metabolism of Amprenavir can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Amprenavir can be decreased when combined with Fluconazole.
FluorouracilThe metabolism of Amprenavir can be decreased when combined with Fluorouracil.
FluoxetineThe metabolism of Amprenavir can be decreased when combined with Fluoxetine.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be decreased when it is combined with Amprenavir.
FluvastatinThe metabolism of Amprenavir can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Amprenavir can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Amprenavir can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Amprenavir can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Amprenavir can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Amprenavir can be increased when it is combined with Fusidic Acid.
GarlicThe serum concentration of Amprenavir can be decreased when it is combined with Garlic.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Amprenavir.
GemcitabineThe serum concentration of Gemcitabine can be decreased when it is combined with Amprenavir.
GemfibrozilThe metabolism of Amprenavir can be decreased when combined with Gemfibrozil.
GrazoprevirThe serum concentration of Grazoprevir can be decreased when it is combined with Amprenavir.
GrepafloxacinThe serum concentration of Grepafloxacin can be decreased when it is combined with Amprenavir.
HaloperidolThe serum concentration of Haloperidol can be decreased when it is combined with Amprenavir.
HaloperidolThe metabolism of Amprenavir can be decreased when combined with Haloperidol.
HydrocortisoneThe serum concentration of Hydrocortisone can be decreased when it is combined with Amprenavir.
IbuprofenThe serum concentration of Ibuprofen can be decreased when it is combined with Amprenavir.
IdelalisibThe serum concentration of Amprenavir can be increased when it is combined with Idelalisib.
IdelalisibThe serum concentration of Idelalisib can be decreased when it is combined with Amprenavir.
ImatinibThe metabolism of Amprenavir can be decreased when combined with Imatinib.
ImatinibThe serum concentration of Imatinib can be decreased when it is combined with Amprenavir.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Amprenavir.
ImipramineThe metabolism of Amprenavir can be decreased when combined with Imipramine.
IndacaterolThe serum concentration of Indacaterol can be decreased when it is combined with Amprenavir.
IndinavirThe serum concentration of Indinavir can be decreased when it is combined with Amprenavir.
IndinavirThe metabolism of Amprenavir can be decreased when combined with Indinavir.
IndomethacinThe serum concentration of Indomethacin can be decreased when it is combined with Amprenavir.
IrbesartanThe metabolism of Amprenavir can be decreased when combined with Irbesartan.
IrinotecanThe serum concentration of Irinotecan can be decreased when it is combined with Amprenavir.
IsavuconazoniumThe metabolism of Amprenavir can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Amprenavir can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Amprenavir can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Amprenavir can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Amprenavir can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be decreased when it is combined with Amprenavir.
KetazolamThe serum concentration of Ketazolam can be decreased when it is combined with Amprenavir.
KetoconazoleThe serum concentration of Ketoconazole can be decreased when it is combined with Amprenavir.
KetoconazoleThe metabolism of Amprenavir can be decreased when combined with Ketoconazole.
LamivudineThe serum concentration of Lamivudine can be decreased when it is combined with Amprenavir.
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Amprenavir.
LansoprazoleThe serum concentration of Lansoprazole can be decreased when it is combined with Amprenavir.
LapatinibThe metabolism of Amprenavir can be decreased when combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Amprenavir.
LeflunomideThe metabolism of Amprenavir can be decreased when combined with Leflunomide.
LenalidomideThe serum concentration of Lenalidomide can be decreased when it is combined with Amprenavir.
LenvatinibThe serum concentration of Lenvatinib can be decreased when it is combined with Amprenavir.
LevetiracetamThe serum concentration of Levetiracetam can be decreased when it is combined with Amprenavir.
LevofloxacinThe serum concentration of Levofloxacin can be decreased when it is combined with Amprenavir.
LevomilnacipranThe serum concentration of Levomilnacipran can be decreased when it is combined with Amprenavir.
LinagliptinThe serum concentration of Linagliptin can be decreased when it is combined with Amprenavir.
LoperamideThe serum concentration of Loperamide can be decreased when it is combined with Amprenavir.
LopinavirThe metabolism of Amprenavir can be decreased when combined with Lopinavir.
LorcaserinThe metabolism of Amprenavir can be decreased when combined with Lorcaserin.
LosartanThe serum concentration of Losartan can be decreased when it is combined with Amprenavir.
LosartanThe metabolism of Amprenavir can be decreased when combined with Losartan.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Amprenavir.
LovastatinThe metabolism of Amprenavir can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Amprenavir can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Amprenavir can be decreased when it is combined with Lumacaftor.
LumefantrineThe metabolism of Amprenavir can be decreased when combined with Lumefantrine.
MannitolThe serum concentration of Mannitol can be decreased when it is combined with Amprenavir.
MethadoneThe metabolism of Amprenavir can be decreased when combined with Methadone.
MethotrexateThe serum concentration of Methotrexate can be decreased when it is combined with Amprenavir.
MethotrimeprazineThe metabolism of Amprenavir can be decreased when combined with Methotrimeprazine.
MethylprednisoloneThe serum concentration of Methylprednisolone can be decreased when it is combined with Amprenavir.
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Amprenavir.
MetoprololThe metabolism of Amprenavir can be decreased when combined with Metoprolol.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Amprenavir.
MifepristoneThe metabolism of Amprenavir can be decreased when combined with Mifepristone.
MirabegronThe serum concentration of Mirabegron can be decreased when it is combined with Amprenavir.
MirabegronThe metabolism of Amprenavir can be decreased when combined with Mirabegron.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Amprenavir.
MitotaneThe serum concentration of Amprenavir can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Mitoxantrone can be decreased when it is combined with Amprenavir.
ModafinilThe serum concentration of Amprenavir can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Morphine can be decreased when it is combined with Amprenavir.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be decreased when it is combined with Amprenavir.
NadololThe serum concentration of Nadolol can be decreased when it is combined with Amprenavir.
NafcillinThe serum concentration of Amprenavir can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Amprenavir.
NaloxoneThe serum concentration of Naloxone can be decreased when it is combined with Amprenavir.
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Amprenavir.
NefazodoneThe metabolism of Amprenavir can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Amprenavir can be decreased when combined with Nelfinavir.
NelfinavirThe serum concentration of Nelfinavir can be decreased when it is combined with Amprenavir.
NetupitantThe serum concentration of Amprenavir can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Amprenavir can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Nicardipine can be decreased when it is combined with Amprenavir.
NicardipineThe metabolism of Amprenavir can be decreased when combined with Nicardipine.
NifedipineThe serum concentration of Nifedipine can be decreased when it is combined with Amprenavir.
NilotinibThe metabolism of Amprenavir can be decreased when combined with Nilotinib.
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Amprenavir.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Amprenavir.
NizatidineThe serum concentration of Nizatidine can be decreased when it is combined with Amprenavir.
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Amprenavir.
OlanzapineThe serum concentration of Olanzapine can be decreased when it is combined with Amprenavir.
OlaparibThe metabolism of Amprenavir can be decreased when combined with Olaparib.
OmbitasvirThe serum concentration of Ombitasvir can be decreased when it is combined with Amprenavir.
OmeprazoleThe metabolism of Amprenavir can be decreased when combined with Omeprazole.
OsimertinibThe serum concentration of Amprenavir can be increased when it is combined with Osimertinib.
OsimertinibThe serum concentration of Osimertinib can be decreased when it is combined with Amprenavir.
PaclitaxelThe serum concentration of Paclitaxel can be decreased when it is combined with Amprenavir.
PalbociclibThe serum concentration of Amprenavir can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Panobinostat can be decreased when it is combined with Amprenavir.
PanobinostatThe metabolism of Amprenavir can be decreased when combined with Panobinostat.
ParoxetineThe metabolism of Amprenavir can be decreased when combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Amprenavir.
Peginterferon alfa-2bThe serum concentration of Amprenavir can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Amprenavir can be increased when combined with Pentobarbital.
PethidineThe risk or severity of adverse effects can be increased when Amprenavir is combined with Pethidine.
PhenobarbitalThe metabolism of Amprenavir can be increased when combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be decreased when it is combined with Amprenavir.
PhenytoinThe metabolism of Amprenavir can be increased when combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be decreased when it is combined with Amprenavir.
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Amprenavir.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Amprenavir.
PioglitazoneThe metabolism of Amprenavir can be decreased when combined with Pioglitazone.
PitavastatinThe serum concentration of Pitavastatin can be decreased when it is combined with Amprenavir.
PomalidomideThe serum concentration of Pomalidomide can be decreased when it is combined with Amprenavir.
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Amprenavir.
PosaconazoleThe metabolism of Amprenavir can be decreased when combined with Posaconazole.
PravastatinThe serum concentration of Pravastatin can be decreased when it is combined with Amprenavir.
PrazosinThe serum concentration of Prazosin can be decreased when it is combined with Amprenavir.
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Amprenavir.
PrednisoneThe serum concentration of Prednisone can be decreased when it is combined with Amprenavir.
PrimidoneThe metabolism of Amprenavir can be increased when combined with Primidone.
ProgesteroneThe serum concentration of Progesterone can be decreased when it is combined with Amprenavir.
PromazineThe metabolism of Amprenavir can be decreased when combined with Promazine.
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Amprenavir.
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Amprenavir.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Amprenavir.
PyrimethamineThe metabolism of Amprenavir can be decreased when combined with Pyrimethamine.
QuetiapineThe serum concentration of Quetiapine can be decreased when it is combined with Amprenavir.
QuinidineThe serum concentration of Quinidine can be decreased when it is combined with Amprenavir.
QuinidineThe metabolism of Amprenavir can be decreased when combined with Quinidine.
QuinineThe serum concentration of Quinine can be decreased when it is combined with Amprenavir.
QuinineThe metabolism of Amprenavir can be decreased when combined with Quinine.
RabeprazoleThe metabolism of Amprenavir can be decreased when combined with Rabeprazole.
RanitidineThe serum concentration of Ranitidine can be decreased when it is combined with Amprenavir.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Amprenavir.
RanolazineThe metabolism of Amprenavir can be decreased when combined with Ranolazine.
ReserpineThe serum concentration of Reserpine can be decreased when it is combined with Amprenavir.
RifabutinThe metabolism of Amprenavir can be increased when combined with Rifabutin.
RifampicinThe metabolism of Amprenavir can be increased when combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be decreased when it is combined with Amprenavir.
RifapentineThe metabolism of Amprenavir can be increased when combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Amprenavir.
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Amprenavir.
RisperidoneThe serum concentration of Risperidone can be decreased when it is combined with Amprenavir.
RitonavirThe metabolism of Amprenavir can be decreased when combined with Ritonavir.
RitonavirThe serum concentration of Ritonavir can be decreased when it is combined with Amprenavir.
RivaroxabanThe serum concentration of Rivaroxaban can be decreased when it is combined with Amprenavir.
RolapitantThe metabolism of Amprenavir can be decreased when combined with Rolapitant.
RomidepsinThe serum concentration of Romidepsin can be decreased when it is combined with Amprenavir.
RopiniroleThe metabolism of Amprenavir can be decreased when combined with Ropinirole.
RosiglitazoneThe metabolism of Amprenavir can be decreased when combined with Rosiglitazone.
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Amprenavir.
Salicylic acidThe serum concentration of Salicylic acid can be decreased when it is combined with Amprenavir.
SaquinavirThe metabolism of Amprenavir can be decreased when combined with Saquinavir.
SaquinavirThe serum concentration of Saquinavir can be decreased when it is combined with Amprenavir.
SecobarbitalThe metabolism of Amprenavir can be increased when combined with Secobarbital.
SelexipagThe serum concentration of Selexipag can be decreased when it is combined with Amprenavir.
SertralineThe metabolism of Amprenavir can be decreased when combined with Sertraline.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Amprenavir.
SildenafilThe metabolism of Amprenavir can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Amprenavir.
SiltuximabThe serum concentration of Amprenavir can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Amprenavir can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Amprenavir.
SitagliptinThe serum concentration of Sitagliptin can be decreased when it is combined with Amprenavir.
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Amprenavir.
SorafenibThe serum concentration of Sorafenib can be decreased when it is combined with Amprenavir.
SorafenibThe metabolism of Amprenavir can be decreased when combined with Sorafenib.
SparfloxacinThe serum concentration of Sparfloxacin can be decreased when it is combined with Amprenavir.
SphingosineThe serum concentration of Sphingosine can be decreased when it is combined with Amprenavir.
St. John's WortThe metabolism of Amprenavir can be increased when combined with St. John's Wort.
StiripentolThe serum concentration of Amprenavir can be increased when it is combined with Stiripentol.
SulfadiazineThe metabolism of Amprenavir can be decreased when combined with Sulfadiazine.
SulfamethoxazoleThe metabolism of Amprenavir can be decreased when combined with Sulfamethoxazole.
SulfisoxazoleThe metabolism of Amprenavir can be decreased when combined with Sulfisoxazole.
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Amprenavir.
TamoxifenThe serum concentration of Tamoxifen can be decreased when it is combined with Amprenavir.
TamoxifenThe metabolism of Amprenavir can be decreased when combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be decreased when it is combined with Amprenavir.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be decreased when it is combined with Amprenavir.
TelaprevirThe metabolism of Amprenavir can be decreased when combined with Telaprevir.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Amprenavir.
TelithromycinThe metabolism of Amprenavir can be decreased when combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be decreased when it is combined with Amprenavir.
TerbinafineThe metabolism of Amprenavir can be decreased when combined with Terbinafine.
TeriflunomideThe metabolism of Amprenavir can be decreased when combined with Teriflunomide.
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Amprenavir.
ThioridazineThe metabolism of Amprenavir can be decreased when combined with Thioridazine.
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Amprenavir.
TicagrelorThe serum concentration of Ticagrelor can be decreased when it is combined with Amprenavir.
TicagrelorThe metabolism of Amprenavir can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Amprenavir can be decreased when combined with Ticlopidine.
TimololThe serum concentration of Timolol can be decreased when it is combined with Amprenavir.
TipranavirThe serum concentration of Amprenavir can be decreased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Amprenavir can be decreased when it is combined with Tocilizumab.
TolbutamideThe metabolism of Amprenavir can be decreased when combined with Tolbutamide.
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Amprenavir.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Amprenavir.
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Amprenavir.
TranylcypromineThe metabolism of Amprenavir can be decreased when combined with Tranylcypromine.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Amprenavir.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Amprenavir.
TrimethoprimThe metabolism of Amprenavir can be decreased when combined with Trimethoprim.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Amprenavir.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Amprenavir.
UmeclidiniumThe serum concentration of Umeclidinium can be decreased when it is combined with Amprenavir.
Valproic AcidThe metabolism of Amprenavir can be decreased when combined with Valproic Acid.
ValsartanThe metabolism of Amprenavir can be decreased when combined with Valsartan.
VecuroniumThe serum concentration of Vecuronium can be decreased when it is combined with Amprenavir.
VenlafaxineThe metabolism of Amprenavir can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be decreased when it is combined with Amprenavir.
VerapamilThe metabolism of Amprenavir can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be decreased when it is combined with Amprenavir.
VinblastineThe serum concentration of Vinblastine can be decreased when it is combined with Amprenavir.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Amprenavir.
VismodegibThe serum concentration of Vismodegib can be decreased when it is combined with Amprenavir.
VoriconazoleThe metabolism of Amprenavir can be decreased when combined with Voriconazole.
ZafirlukastThe metabolism of Amprenavir can be decreased when combined with Zafirlukast.
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Amprenavir.
ZiprasidoneThe metabolism of Amprenavir can be decreased when combined with Ziprasidone.
Food Interactions
  • Avoid alcohol, especially with the oral solution since it contains propylene glycol which competes with alcohol for alcohol dehydrogenase metabolism.
  • Take with or without food, however avoid lipid-rich meals.
  • Vitamin E increases amprenavir bioavailability.

Targets

Kind
Protein
Organism
Human immunodeficiency virus 1
Pharmacological action
yes
Actions
inhibitor
General Function:
Aspartic-type endopeptidase activity
Specific Function:
Not Available
Gene Name:
pol
Uniprot ID:
Q72874
Molecular Weight:
10778.7 Da
References
  1. Wittayanarakul K, Hannongbua S, Feig M: Accurate prediction of protonation state as a prerequisite for reliable MM-PB(GB)SA binding free energy calculations of HIV-1 protease inhibitors. J Comput Chem. 2008 Apr 15;29(5):673-85. [PubMed:17849388 ]
  2. Dandache S, Sevigny G, Yelle J, Stranix BR, Parkin N, Schapiro JM, Wainberg MA, Wu JJ: In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2007 Nov;51(11):4036-43. Epub 2007 Jul 16. [PubMed:17638694 ]
  3. Sadler BM, Hanson CD, Chittick GE, Symonds WT, Roskell NS: Safety and pharmacokinetics of amprenavir (141W94), a human immunodeficiency virus (HIV) type 1 protease inhibitor, following oral administration of single doses to HIV-infected adults. Antimicrob Agents Chemother. 1999 Jul;43(7):1686-92. [PubMed:10390223 ]
  4. Authors unspecified: Amprenavir: a new HIV protease inhibitor. Med Lett Drugs Ther. 1999 Jul 16;41(1057):64-6. [PubMed:10436772 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
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
Molecular Weight:
141477.255 Da
References
  1. Perloff MD, von Moltke LL, Fahey JM, Daily JP, Greenblatt DJ: Induction of P-glycoprotein expression by HIV protease inhibitors in cell culture. AIDS. 2000 Jun 16;14(9):1287-9. [PubMed:10894301 ]
  2. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Olson DP, Scadden DT, D'Aquila RT, De Pasquale MP: The protease inhibitor ritonavir inhibits the functional activity of the multidrug resistance related-protein 1 (MRP-1). AIDS. 2002 Sep 6;16(13):1743-7. [PubMed:12218384 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on September 28, 2016 02:25