Identification

Name
Deutetrabenazine
Accession Number
DB12161
Type
Small Molecule
Groups
Approved, Investigational
Description

Deutetrabenazine is a vesicular monoamine transporter 2 (VMAT2) inhibitor indicated for the treatment of chorea associated with Huntington’s disease

Structure
Thumb
Synonyms
Not Available
External IDs
SD-809
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AustedoTablet, coated6 mg/1OralTeva Neuroscience, Inc.2017-04-12Not applicableUs
AustedoTablet, coated12 mg/1OralTeva Neuroscience, Inc.2017-04-12Not applicableUs
AustedoTablet, coated9 mg/1OralTeva Neuroscience, Inc.2017-04-12Not applicableUs
Categories
UNII
P341G6W9NB
CAS number
1392826-25-3
Weight
Average: 323.466
Monoisotopic: 323.236754209
Chemical Formula
C19H27NO3
InChI Key
MKJIEFSOBYUXJB-WEZHFFAMSA-N
InChI
InChI=1S/C19H27NO3/c1-12(2)7-14-11-20-6-5-13-8-18(22-3)19(23-4)9-15(13)16(20)10-17(14)21/h8-9,12,14,16H,5-7,10-11H2,1-4H3/t14-,16-/m0/s1/i3D3,4D3
IUPAC Name
(3S,11bS)-9,10-di(2H3)methoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11bH-pyrido[2,1-a]isoquinolin-2-one
SMILES
[2H]C([2H])([2H])OC1=CC2=C(C=C1OC([2H])([2H])[2H])[[email protected]@H]1CC(=O)[[email protected]@H](CC(C)C)CN1CC2

Pharmacology

Indication

Deutetrabenazine is indicated for the treatment of chorea associated with Huntington’s disease.

Structured Indications
Pharmacodynamics

Cardiac Electrophysiology The effect of a single 12-mg or 24-mg dose of deutetrabenazine on the QT interval was studied in a randomized, double-blind, placebo-controlled crossover study in healthy male and female subjects with moxifloxacin as a positive control. At 24 mg, deutetrabenazine caused an approximately 4.5 msec mean increase in QTc (90% CI: 2.4, 6.5 msec). Effects at higher exposures to deutetrabenazine or its metabolites have not been evaluated. The effect of a single 25-mg or 50-mg dose of tetrabenazine, a closely related VMAT2 inhibitor, on the QT interval was studied in a randomized, double-blind, placebo-controlled crossover study in healthy male and female subjects with moxifloxacin as a positive control. At 50 mg, tetrabenazine caused an approximately 8 msec mean increase in QTc (90% CI: 5.0, 10.4 msec). Effects at higher exposures to either tetrabenazine or its metabolites have not been evaluated . Melanin Binding Deutetrabenazine or its metabolites bind to melanin-containing tissues (i.e., eye, skin, fur) in pigmented rats. After a single oral dose of radiolabeled deutetrabenazine, radioactivity was still detected in eye and fur at 35 days following dosing.

Mechanism of action

The precise mechanism by which deutetrabenazine exerts its anti-chorea effects is unknown but is believed to be related to its effect as a reversible depletor of monoamines (such as dopamine, serotonin, norepinephrine, and histamine) from nerve terminals. The major circulating metabolites (α-dihydrotetrabenazine [HTBZ] and β-HTBZ) of deutetrabenazine, are reversible inhibitors of VMAT2, resulting in decreased uptake of monoamines into synaptic vesicles and depletion of monoamine stores.

Absorption

Following oral administration of deutetrabenazine, the extent of absorption is at least 80%. Plasma concentrations of deutetrabenazine are generally below the limit of detection after oral dosing. Peak plasma concentrations (Cmax) of deuterated α-HTBZ and β-HTBZ are reached within 3 to 4 hours after dosing. Effect of Food The effects of food on the bioavailability of deutetrabenazine were studied in subjects administered a single dose with and without food. Food had no effect on the area under the plasma concentration-time curve (AUC) of α-HTBZ or β-HTBZ, although Cmax was increased by approximately 50% in the presence of food.

Volume of distribution

The median volume of distribution (Vc/F) of the α-HTBZ, and the β-HTBZ metabolites of deutetrabenazine are approximately 500 L and 730 L, respectively.

Protein binding

The in vitro protein binding of tetrabenazine, α-HTBZ, and β-HTBZ was examined in human plasma for concentrations ranging from 50 to 200 ng/mL. Tetrabenazine binding ranged from 82% to 85%, α-HTBZ binding ranged from 60% to 68%, and β-HTBZ binding ranged from 59% to 63%.

Metabolism

In vitro experiments in human liver microsomes demonstrate that deutetrabenazine is extensively biotransformed, mainly by carbonyl reductase, to its major active metabolites, α-HTBZ and β­-HTBZ, which are subsequently metabolized primarily by CYP2D6, with minor contributions of CYP1A2 and CYP3A4/5, to form several minor metabolites.

Route of elimination

75% to 86% of the deutetrabenazine dose was excreted in the urine, and fecal recovery accounted for 8% to 11% of the dose.

Half life

The half-life of total (α+β)-HTBZ from deutetrabenazine is approximately 9 to 10 hours.

Clearance

The median clearance values (CL/F) of the α-HTBZ, and the β-HTBZ metabolites of deutetrabenazine are approximately 47 L/hour and 70 L/hour, respectively, in the Huntington’s disease patient population.

Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Deutetrabenazine can be increased when it is combined with Abiraterone.Approved
AmiodaroneThe metabolism of Deutetrabenazine can be decreased when combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Deutetrabenazine can be increased when it is combined with Aprepitant.Approved, Investigational
ArtemetherThe metabolism of Deutetrabenazine can be decreased when combined with Artemether.Approved
AtazanavirThe metabolism of Deutetrabenazine can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Deutetrabenazine can be decreased when combined with Atomoxetine.Approved
AzithromycinThe metabolism of Deutetrabenazine can be decreased when combined with Azithromycin.Approved
BetaxololThe metabolism of Deutetrabenazine can be decreased when combined with Betaxolol.Approved
BoceprevirThe metabolism of Deutetrabenazine can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Deutetrabenazine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Deutetrabenazine can be decreased when it is combined with Bosentan.Approved, Investigational
BupropionThe metabolism of Deutetrabenazine can be decreased when combined with Bupropion.Approved
CaffeineThe metabolism of Deutetrabenazine can be decreased when combined with Caffeine.Approved
CarbamazepineThe metabolism of Deutetrabenazine can be increased when combined with Carbamazepine.Approved, Investigational
CelecoxibThe metabolism of Deutetrabenazine can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Deutetrabenazine can be increased when it is combined with Ceritinib.Approved
ChloroquineThe metabolism of Deutetrabenazine can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe metabolism of Deutetrabenazine can be decreased when combined with Chlorpromazine.Approved, Vet Approved
CholecalciferolThe metabolism of Deutetrabenazine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Deutetrabenazine can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Deutetrabenazine can be decreased when combined with Cinacalcet.Approved
CitalopramThe metabolism of Deutetrabenazine can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Deutetrabenazine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Deutetrabenazine can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Deutetrabenazine can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Deutetrabenazine can be decreased when combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe metabolism of Deutetrabenazine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Deutetrabenazine can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Deutetrabenazine can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Deutetrabenazine can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Deutetrabenazine can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Deutetrabenazine can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Deutetrabenazine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Deutetrabenazine can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Deutetrabenazine can be decreased when it is combined with Dabrafenib.Approved
DarifenacinThe metabolism of Deutetrabenazine can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Deutetrabenazine can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Deutetrabenazine can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Deutetrabenazine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Deutetrabenazine can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Deutetrabenazine can be decreased when combined with Desipramine.Approved
DihydroergotamineThe metabolism of Deutetrabenazine can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Deutetrabenazine can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Deutetrabenazine can be decreased when combined with Diphenhydramine.Approved
DosulepinThe metabolism of Deutetrabenazine can be decreased when combined with Dosulepin.Approved
DoxycyclineThe metabolism of Deutetrabenazine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Deutetrabenazine can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Deutetrabenazine can be decreased when combined with Duloxetine.Approved
EliglustatThe metabolism of Deutetrabenazine can be decreased when combined with Eliglustat.Approved
EnzalutamideThe serum concentration of Deutetrabenazine can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Deutetrabenazine can be decreased when combined with Erythromycin.Approved, Vet Approved
FluconazoleThe metabolism of Deutetrabenazine can be decreased when combined with Fluconazole.Approved
FluoxetineThe metabolism of Deutetrabenazine can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluvoxamineThe metabolism of Deutetrabenazine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Deutetrabenazine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Deutetrabenazine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Deutetrabenazine can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Deutetrabenazine can be increased when it is combined with Fusidic Acid.Approved
HaloperidolThe metabolism of Deutetrabenazine can be decreased when combined with Haloperidol.Approved
IdelalisibThe metabolism of Deutetrabenazine can be decreased when combined with Idelalisib.Approved
ImatinibThe metabolism of Deutetrabenazine can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Deutetrabenazine can be decreased when combined with Imipramine.Approved
IndinavirThe metabolism of Deutetrabenazine can be decreased when combined with Indinavir.Approved
IsavuconazoniumThe metabolism of Deutetrabenazine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Deutetrabenazine can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Deutetrabenazine can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Deutetrabenazine can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Deutetrabenazine can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Deutetrabenazine can be decreased when combined with Ketoconazole.Approved, Investigational
LidocaineThe metabolism of Deutetrabenazine can be decreased when combined with Lidocaine.Approved, Vet Approved
LobeglitazoneThe metabolism of Deutetrabenazine can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe metabolism of Deutetrabenazine can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Deutetrabenazine can be decreased when combined with Lorcaserin.Approved
LovastatinThe metabolism of Deutetrabenazine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Deutetrabenazine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Deutetrabenazine can be increased when combined with Lumacaftor.Approved
LumefantrineThe metabolism of Deutetrabenazine can be decreased when combined with Lumefantrine.Approved
ManidipineThe metabolism of Deutetrabenazine can be decreased when combined with Manidipine.Approved, Investigational
MethadoneThe metabolism of Deutetrabenazine can be decreased when combined with Methadone.Approved
MethotrimeprazineThe metabolism of Deutetrabenazine can be decreased when combined with Methotrimeprazine.Approved
MetoprololThe metabolism of Deutetrabenazine can be decreased when combined with Metoprolol.Approved, Investigational
MexiletineThe metabolism of Deutetrabenazine can be decreased when combined with Mexiletine.Approved
MidostaurinThe metabolism of Deutetrabenazine can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Deutetrabenazine can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe metabolism of Deutetrabenazine can be decreased when combined with Mirabegron.Approved
MitotaneThe serum concentration of Deutetrabenazine can be decreased when it is combined with Mitotane.Approved
NefazodoneThe metabolism of Deutetrabenazine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Deutetrabenazine can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Deutetrabenazine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Deutetrabenazine can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Deutetrabenazine can be decreased when combined with Nicardipine.Approved
NilotinibThe metabolism of Deutetrabenazine can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Deutetrabenazine can be decreased when combined with Olaparib.Approved
OsimertinibThe serum concentration of Deutetrabenazine can be increased when it is combined with Osimertinib.Approved
PalbociclibThe serum concentration of Deutetrabenazine can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Deutetrabenazine can be increased when it is combined with Panobinostat.Approved, Investigational
ParoxetineThe metabolism of Deutetrabenazine can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Deutetrabenazine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe metabolism of Deutetrabenazine can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Deutetrabenazine can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Deutetrabenazine can be increased when combined with Phenytoin.Approved, Vet Approved
PosaconazoleThe metabolism of Deutetrabenazine can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Deutetrabenazine can be increased when combined with Primidone.Approved, Vet Approved
PromazineThe metabolism of Deutetrabenazine can be decreased when combined with Promazine.Approved, Vet Approved
QuinidineThe metabolism of Deutetrabenazine can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Deutetrabenazine can be decreased when combined with Quinine.Approved
RanolazineThe metabolism of Deutetrabenazine can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Deutetrabenazine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Deutetrabenazine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Deutetrabenazine can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Deutetrabenazine can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe metabolism of Deutetrabenazine can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Deutetrabenazine can be decreased when combined with Ropinirole.Approved, Investigational
RucaparibThe metabolism of Deutetrabenazine can be decreased when combined with Rucaparib.Approved, Investigational
SaquinavirThe metabolism of Deutetrabenazine can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Deutetrabenazine can be decreased when used in combination with Sarilumab.Approved
SertralineThe metabolism of Deutetrabenazine can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Deutetrabenazine can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Deutetrabenazine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Deutetrabenazine can be increased when it is combined with Simeprevir.Approved
St. John's WortThe serum concentration of Deutetrabenazine can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Deutetrabenazine can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Deutetrabenazine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TelaprevirThe metabolism of Deutetrabenazine can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Deutetrabenazine can be decreased when combined with Telithromycin.Approved
Tenofovir disoproxilThe metabolism of Deutetrabenazine can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerbinafineThe metabolism of Deutetrabenazine can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TeriflunomideThe serum concentration of Deutetrabenazine can be decreased when it is combined with Teriflunomide.Approved
TheophyllineThe metabolism of Deutetrabenazine can be decreased when combined with Theophylline.Approved
ThioridazineThe metabolism of Deutetrabenazine can be decreased when combined with Thioridazine.Approved, Withdrawn
TiclopidineThe metabolism of Deutetrabenazine can be decreased when combined with Ticlopidine.Approved
TipranavirThe metabolism of Deutetrabenazine can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Deutetrabenazine can be decreased when it is combined with Tocilizumab.Approved
TranylcypromineThe metabolism of Deutetrabenazine can be decreased when combined with Tranylcypromine.Approved
VemurafenibThe serum concentration of Deutetrabenazine can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Deutetrabenazine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Deutetrabenazine can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Deutetrabenazine can be decreased when combined with Voriconazole.Approved, Investigational
ZiprasidoneThe metabolism of Deutetrabenazine can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe metabolism of Deutetrabenazine can be decreased when combined with Zucapsaicin.Approved
Food Interactions
Not Available

References

General References
  1. FDA label [Link]
External Links
PubChem Compound
73442840
PubChem Substance
347828453
ChemSpider
32700662

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentGilles de la Tourette's Syndrome1
2, 3CompletedTreatmentTardive Dyskinesia1
3Active Not RecruitingTreatmentTardive Dyskinesia1
3CompletedTreatmentChorea1
3CompletedTreatmentChorea Associated With Huntington Disease1
3CompletedTreatmentTardive Dyskinesia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, coatedOral12 mg/1
Tablet, coatedOral6 mg/1
Tablet, coatedOral9 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8524733No2011-03-272031-03-27Us
US9296739No2013-09-182033-09-18Us
US9233959No2013-09-182033-09-18Us
US9550780No2013-09-182033-09-18Us

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.361 mg/mLALOGPS
logP3.23ALOGPS
logP3.4ChemAxon
logS-2.9ALOGPS
pKa (Strongest Acidic)18.26ChemAxon
pKa (Strongest Basic)7.33ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area38.77 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity91.31 m3·mol-1ChemAxon
Polarizability36.83 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

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

Taxonomy

Description
This compound belongs to the class of organic compounds known as tetrahydroisoquinolines. These are tetrahydrogenated isoquinoline derivatives.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Tetrahydroisoquinolines
Sub Class
Not Available
Direct Parent
Tetrahydroisoquinolines
Alternative Parents
Anisoles / Piperidinones / Aralkylamines / Alkyl aryl ethers / Trialkylamines / Cyclic ketones / Azacyclic compounds / Organic oxides / Hydrocarbon derivatives
Substituents
Tetrahydroisoquinoline / Anisole / Phenol ether / Alkyl aryl ether / Piperidinone / Aralkylamine / Piperidine / Benzenoid / Tertiary aliphatic amine / Tertiary amine
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Prostaglandin-e2 9-reductase activity
Specific Function
NADPH-dependent reductase with broad substrate specificity. Catalyzes the reduction of a wide variety of carbonyl compounds including quinones, prostaglandins, menadione, plus various xenobiotics. ...
Gene Name
CBR1
Uniprot ID
P16152
Uniprot Name
Carbonyl reductase [NADPH] 1
Molecular Weight
30374.73 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Nadph binding
Specific Function
Has low NADPH-dependent oxidoreductase activity towards 4-benzoylpyridine and menadione (in vitro).
Gene Name
CBR3
Uniprot ID
O75828
Uniprot Name
Carbonyl reductase [NADPH] 3
Molecular Weight
30849.97 Da
Kind
Protein
Organism
Human
Pharmacological action
Yes
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Substrate
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
Yes
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Not Available
Specific Function
Not Available
Gene Name
VMAT2
Uniprot ID
Q99870
Uniprot Name
Vesicle monoamine transporter type 2
Molecular Weight
17291.525 Da

Drug created on October 20, 2016 15:30 / Updated on December 01, 2017 16:27