You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameEnzalutamide
Accession NumberDB08899
TypeSmall Molecule
GroupsApproved
Description

Enzalutamide is an androgen receptor inhibitor for the treatment of castration-resistant prostate cancer. FDA approved on August 31, 2012.

Structure
Thumb
Synonyms
MDV 3100
MDV-3100
MDV3100
XTANDI
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Xtandicapsule40 mg/1oralAstellas Pharma US, Inc.2012-08-31Not applicableUs
Xtandicapsule40 mgoralAstellas Pharma Canada Inc2013-06-07Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII93T0T9GKNU
CAS number915087-33-1
WeightAverage: 464.436
Monoisotopic: 464.093009286
Chemical FormulaC21H16F4N4O2S
InChI KeyInChIKey=WXCXUHSOUPDCQV-UHFFFAOYSA-N
InChI
InChI=1S/C21H16F4N4O2S/c1-20(2)18(31)28(12-5-4-11(10-26)15(8-12)21(23,24)25)19(32)29(20)13-6-7-14(16(22)9-13)17(30)27-3/h4-9H,1-3H3,(H,27,30)
IUPAC Name
4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl}-2-fluoro-N-methylbenzamide
SMILES
CNC(=O)C1=C(F)C=C(C=C1)N1C(=S)N(C(=O)C1(C)C)C1=CC=C(C#N)C(=C1)C(F)(F)F
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylimidazolidines. These are polycyclic compounds containing an imidazoline substituted by a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzolidines
Sub ClassImidazolidines
Direct ParentPhenylimidazolidines
Alternative Parents
Substituents
  • Phenylimidazolidine
  • Halobenzoic acid or derivatives
  • 2-halobenzoic acid or derivatives
  • N-phenylthiourea
  • Aminobenzoic acid or derivatives
  • Benzoic acid or derivatives
  • Benzamide
  • Aminobenzamide
  • Benzoyl
  • Benzonitrile
  • Halobenzene
  • Fluorobenzene
  • Benzenoid
  • Imidazolidinone
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Vinylogous halide
  • Thiourea
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Thiocarbonic acid derivative
  • Carboxamide group
  • Azacycle
  • Nitrile
  • Carbonitrile
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationEnzalutamide is indicated for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel.
PharmacodynamicsResitance to enzalutamide therapy has been observed. This may occurred due to an upregulation of NF-κB2/p52.
Mechanism of actionEnzalutamide is a competitive androgen receptor inhibitor that effects multiple stages of the signalling pathway. It is able to inhibit androgen binding to its receptor, androgen receptor nuclear translocation, and subsequent interaction with DNA. As a result, proliferation of prostate cancer cells decreases which ultimately leads to apoptosis and decreased tumour volume.
Related Articles
AbsorptionThe pharmacokinetic profile of enzalutamide and N-desmethyl enzalutamide (its major active metabolite) is described by a linear two-compartment model with first-order absorption. Enzalutamide also accumulates. Food does not affect its absorption. Tmax, prostate cancer patients = 1 hour (range of 0.5-3 hours); Cmax, steady state, enzalutamide = 16.6 μg/mL; Cmax, steady state, N-desmethyl enzalutamide = 12.7 μg/mL; Time to steady state, daily dosing = 28 days;
Volume of distribution

Apparent volume of distribution (Vd/F), single oral dose = 110 L

Protein bindingEnzalutamide is 97% to 98% bound to plasma proteins, primarily albumin. N-desmethyl enzalutamide is 95% bound to plasma proteins.
Metabolism

Enzalutamide is hepatically metabolized, primarily by CYP2C8 and CYP3A4. The enzyme that converts enzalutamide to its active metabolite, N-desmethyl enzalutamide, is CYP2C8. The activity of N-desmethyl-enzalutamide is similar to that of the parent compound.

Route of eliminationEnzalutamide is primarily eliminated by hepatic metabolism. 71% of the dose is recovered in urine (including only trace amounts of enzalutamide and N-desmethyl enzalutamide), and 14% is recovered in feces (0.4% of dose as unchanged enzalutamide and 1% as N-desmethyl enzalutamide).
Half lifeThe mean terminal half-life (t1/2) for enzalutamide in patients after a single oral dose is 5.8 days (range 2.8 to 10.2 days). Following a single 160 mg oral dose of enzalutamide in healthy volunteers, the mean terminal t1/2 for N-desmethyl enzalutamide is approximately 7.8 to 8.6 days.
Clearance

Apparent clearance (CL/F), single oral dose = 0.56 L/h (range of 0.33 – 1.02 L/h)

ToxicityThe most common adverse reactions (≥ 5%) are asthenia/fatigue, back pain, diarrhea, arthralgia, hot flush, peripheral edema, musculoskeletal pain, headache, upper respiratory infection, muscular weakness, dizziness, insomnia, lower respiratory infection, spinal cord compression and cauda equina syndrome, hematuria, paresthesia, anxiety, and hypertension.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9356
Blood Brain Barrier+0.8514
Caco-2 permeable+0.5219
P-glycoprotein substrateNon-substrate0.7609
P-glycoprotein inhibitor IInhibitor0.6464
P-glycoprotein inhibitor IIInhibitor0.5693
Renal organic cation transporterNon-inhibitor0.899
CYP450 2C9 substrateNon-substrate0.7447
CYP450 2D6 substrateNon-substrate0.8061
CYP450 3A4 substrateSubstrate0.5589
CYP450 1A2 substrateNon-inhibitor0.5613
CYP450 2C9 inhibitorInhibitor0.7126
CYP450 2D6 inhibitorNon-inhibitor0.9148
CYP450 2C19 inhibitorInhibitor0.6882
CYP450 3A4 inhibitorInhibitor0.6184
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6711
Ames testNon AMES toxic0.683
CarcinogenicityNon-carcinogens0.7232
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.4319 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9911
hERG inhibition (predictor II)Inhibitor0.7079
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Capsuleoral40 mg/1
Capsuleoral40 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7709517 No2007-08-132027-08-13Us
US8183274 No2006-05-152026-05-15Us
US9126941 No2006-05-152026-05-15Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityInsoluble FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.00136 mg/mLALOGPS
logP3.75ALOGPS
logP4.16ChemAxon
logS-5.5ALOGPS
pKa (Strongest Acidic)13.05ChemAxon
pKa (Strongest Basic)-1.7ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area76.44 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity113.48 m3·mol-1ChemAxon
Polarizability42.71 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Nadiminty N, Tummala R, Liu C, Yang J, Lou W, Evans CP, Gao AC: NF-kappaB2/p52 induces resistance to enzalutamide in prostate cancer: role of androgen receptor and its variants. Mol Cancer Ther. 2013 Aug;12(8):1629-37. doi: 10.1158/1535-7163.MCT-13-0027. Epub 2013 May 22. [PubMed:23699654 ]
External Links
ATC CodesL02BB04
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (393 KB)
MSDSDownload (89.7 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Abiraterone can be decreased when it is combined with Enzalutamide.
AlfentanilThe serum concentration of Alfentanil can be decreased when it is combined with Enzalutamide.
ApixabanThe serum concentration of Apixaban can be decreased when it is combined with Enzalutamide.
ApremilastThe serum concentration of Apremilast can be decreased when it is combined with Enzalutamide.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Enzalutamide.
ArtemetherThe serum concentration of the active metabolites of Artemether can be reduced when Artemether is used in combination with Enzalutamide resulting in a loss in efficacy.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Enzalutamide.
BedaquilineThe serum concentration of Bedaquiline can be decreased when it is combined with Enzalutamide.
BexaroteneThe serum concentration of Enzalutamide can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Boceprevir can be decreased when it is combined with Enzalutamide.
BortezomibThe serum concentration of Bortezomib can be decreased when it is combined with Enzalutamide.
BosentanThe serum concentration of Enzalutamide can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Enzalutamide.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be decreased when it is combined with Enzalutamide.
BrexpiprazoleThe serum concentration of Brexpiprazole can be decreased when it is combined with Enzalutamide.
CabozantinibThe serum concentration of Cabozantinib can be decreased when it is combined with Enzalutamide.
CannabidiolThe serum concentration of Cannabidiol can be decreased when it is combined with Enzalutamide.
CapromabEnzalutamide may decrease effectiveness of Capromab as a diagnostic agent.
CarbamazepineThe serum concentration of Enzalutamide can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Ceritinib can be decreased when it is combined with Enzalutamide.
Choline C 11The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Enzalutamide.
ClarithromycinThe serum concentration of the active metabolites of Clarithromycin can be increased when Clarithromycin is used in combination with Enzalutamide.
ClopidogrelThe serum concentration of Enzalutamide can be increased when it is combined with Clopidogrel.
ClozapineThe serum concentration of Clozapine can be decreased when it is combined with Enzalutamide.
CrizotinibThe serum concentration of Crizotinib can be decreased when it is combined with Enzalutamide.
CyclosporineThe serum concentration of Cyclosporine can be decreased when it is combined with Enzalutamide.
DabrafenibThe serum concentration of Enzalutamide can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Daclatasvir can be decreased when it is combined with Enzalutamide.
DasatinibThe serum concentration of Dasatinib can be decreased when it is combined with Enzalutamide.
DeferasiroxThe serum concentration of Enzalutamide can be decreased when it is combined with Deferasirox.
DexamethasoneThe serum concentration of Enzalutamide can be decreased when it is combined with Dexamethasone.
DienogestThe serum concentration of Dienogest can be decreased when it is combined with Enzalutamide.
DihydroergotamineThe serum concentration of Dihydroergotamine can be decreased when it is combined with Enzalutamide.
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Enzalutamide.
DronabinolThe serum concentration of Dronabinol can be decreased when it is combined with Enzalutamide.
DronedaroneThe serum concentration of Dronedarone can be decreased when it is combined with Enzalutamide.
EfavirenzThe serum concentration of Enzalutamide can be decreased when it is combined with Efavirenz.
EliglustatThe serum concentration of Eliglustat can be decreased when it is combined with Enzalutamide.
ErgotamineThe serum concentration of Ergotamine can be decreased when it is combined with Enzalutamide.
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Enzalutamide.
Eslicarbazepine acetateThe serum concentration of Enzalutamide can be decreased when it is combined with Eslicarbazepine acetate.
EtoposideThe serum concentration of Etoposide can be decreased when it is combined with Enzalutamide.
EtravirineThe serum concentration of Enzalutamide can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be decreased when it is combined with Enzalutamide.
ExemestaneThe serum concentration of Exemestane can be decreased when it is combined with Enzalutamide.
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Enzalutamide.
FlibanserinThe serum concentration of Flibanserin can be decreased when it is combined with Enzalutamide.
FludrocortisoneThe serum concentration of Fludrocortisone can be decreased when it is combined with Enzalutamide.
FlunisolideThe metabolism of Flunisolide can be increased when combined with Enzalutamide.
FosphenytoinThe serum concentration of Enzalutamide can be decreased when it is combined with Fosphenytoin.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Enzalutamide.
GemfibrozilThe serum concentration of Enzalutamide can be increased when it is combined with Gemfibrozil.
GuanfacineThe serum concentration of Guanfacine can be decreased when it is combined with Enzalutamide.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Enzalutamide.
HydrocortisoneThe serum concentration of Hydrocortisone can be decreased when it is combined with Enzalutamide.
IbrutinibThe serum concentration of Ibrutinib can be decreased when it is combined with Enzalutamide.
IdelalisibThe serum concentration of Idelalisib can be decreased when it is combined with Enzalutamide.
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be increased when Ifosfamide is used in combination with Enzalutamide.
ImatinibThe serum concentration of Imatinib can be decreased when it is combined with Enzalutamide.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Enzalutamide resulting in a loss in efficacy.
IsavuconazoniumThe serum concentration of the active metabolites of Isavuconazonium can be reduced when Isavuconazonium is used in combination with Enzalutamide resulting in a loss in efficacy.
IsosorbideThe serum concentration of Isosorbide can be decreased when it is combined with Enzalutamide.
ItraconazoleThe serum concentration of Itraconazole can be decreased when it is combined with Enzalutamide.
IvabradineThe serum concentration of Ivabradine can be decreased when it is combined with Enzalutamide.
IvacaftorThe serum concentration of Ivacaftor can be decreased when it is combined with Enzalutamide.
IxabepiloneThe serum concentration of Ixabepilone can be decreased when it is combined with Enzalutamide.
LapatinibThe serum concentration of Lapatinib can be decreased when it is combined with Enzalutamide.
LinagliptinThe serum concentration of Linagliptin can be decreased when it is combined with Enzalutamide.
LumefantrineThe serum concentration of Lumefantrine can be decreased when it is combined with Enzalutamide.
LurasidoneThe serum concentration of Lurasidone can be decreased when it is combined with Enzalutamide.
MacitentanThe serum concentration of MACITENTAN can be decreased when it is combined with Enzalutamide.
MaravirocThe serum concentration of Maraviroc can be decreased when it is combined with Enzalutamide.
MethylprednisoloneThe serum concentration of Methylprednisolone can be decreased when it is combined with Enzalutamide.
MifepristoneThe serum concentration of Mifepristone can be decreased when it is combined with Enzalutamide.
MitotaneThe serum concentration of Enzalutamide can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Enzalutamide can be decreased when it is combined with Modafinil.
NafcillinThe serum concentration of Enzalutamide can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be decreased when it is combined with Enzalutamide.
NelfinavirThe serum concentration of Enzalutamide can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Netupitant can be decreased when it is combined with Enzalutamide.
NifedipineThe serum concentration of Nifedipine can be decreased when it is combined with Enzalutamide.
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Enzalutamide.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Enzalutamide.
NisoldipineThe serum concentration of Nisoldipine can be decreased when it is combined with Enzalutamide.
OlaparibThe serum concentration of Olaparib can be decreased when it is combined with Enzalutamide.
PalbociclibThe serum concentration of Palbociclib can be decreased when it is combined with Enzalutamide.
PanobinostatThe serum concentration of Panobinostat can be decreased when it is combined with Enzalutamide.
PazopanibThe serum concentration of Pazopanib can be decreased when it is combined with Enzalutamide.
PerampanelThe serum concentration of Perampanel can be decreased when it is combined with Enzalutamide.
PhenobarbitalThe serum concentration of Enzalutamide can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Enzalutamide can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be decreased when it is combined with Enzalutamide.
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Enzalutamide.
PosaconazoleThe serum concentration of Enzalutamide can be increased when it is combined with Posaconazole.
PraziquantelThe serum concentration of Praziquantel can be decreased when it is combined with Enzalutamide.
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Enzalutamide.
PrednisoneThe serum concentration of Prednisone can be decreased when it is combined with Enzalutamide.
PrimidoneThe serum concentration of Enzalutamide can be decreased when it is combined with Primidone.
PropafenoneThe serum concentration of Propafenone can be decreased when it is combined with Enzalutamide.
QuetiapineThe serum concentration of Quetiapine can be decreased when it is combined with Enzalutamide.
QuinidineThe serum concentration of Quinidine can be decreased when it is combined with Enzalutamide.
RanolazineThe serum concentration of Ranolazine can be decreased when it is combined with Enzalutamide.
RegorafenibThe serum concentration of Regorafenib can be decreased when it is combined with Enzalutamide.
RifabutinThe serum concentration of Enzalutamide can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Enzalutamide can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Enzalutamide can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Enzalutamide can be increased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Rivaroxaban can be decreased when it is combined with Enzalutamide.
RoflumilastThe serum concentration of Roflumilast can be decreased when it is combined with Enzalutamide.
RolapitantThe serum concentration of Rolapitant can be decreased when it is combined with Enzalutamide.
RomidepsinThe serum concentration of Romidepsin can be decreased when it is combined with Enzalutamide.
RosiglitazoneThe metabolism of Enzalutamide can be decreased when combined with Rosiglitazone.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Enzalutamide.
SecobarbitalThe serum concentration of Enzalutamide can be decreased when it is combined with Secobarbital.
SiltuximabThe serum concentration of Enzalutamide can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Simeprevir can be decreased when it is combined with Enzalutamide.
SirolimusThe serum concentration of Sirolimus can be decreased when it is combined with Enzalutamide.
SonidegibThe serum concentration of Sonidegib can be decreased when it is combined with Enzalutamide.
SorafenibThe serum concentration of Sorafenib can be decreased when it is combined with Enzalutamide.
St. John's WortThe serum concentration of Enzalutamide can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Enzalutamide can be increased when it is combined with Stiripentol.
SunitinibThe serum concentration of Sunitinib can be decreased when it is combined with Enzalutamide.
SuvorexantThe serum concentration of Suvorexant can be decreased when it is combined with Enzalutamide.
TacrolimusThe serum concentration of Tacrolimus can be decreased when it is combined with Enzalutamide.
TadalafilThe serum concentration of Tadalafil can be decreased when it is combined with Enzalutamide.
TasimelteonThe serum concentration of Tasimelteon can be decreased when it is combined with Enzalutamide.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Enzalutamide.
TicagrelorThe serum concentration of the active metabolites of Ticagrelor can be reduced when Ticagrelor is used in combination with Enzalutamide resulting in a loss in efficacy.
TocilizumabThe serum concentration of Enzalutamide can be decreased when it is combined with Tocilizumab.
TofacitinibThe serum concentration of Tofacitinib can be decreased when it is combined with Enzalutamide.
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Enzalutamide.
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Enzalutamide.
TrabectedinThe serum concentration of Trabectedin can be decreased when it is combined with Enzalutamide.
TrimethoprimThe metabolism of Enzalutamide can be decreased when combined with Trimethoprim.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Enzalutamide.
VandetanibThe serum concentration of Vandetanib can be decreased when it is combined with Enzalutamide.
VemurafenibThe serum concentration of Vemurafenib can be decreased when it is combined with Enzalutamide.
VilazodoneThe serum concentration of Vilazodone can be decreased when it is combined with Enzalutamide.
VincristineThe serum concentration of Vincristine can be decreased when it is combined with Enzalutamide.
VorapaxarThe serum concentration of Vorapaxar can be decreased when it is combined with Enzalutamide.
VoriconazoleThe serum concentration of Enzalutamide can be increased when it is combined with Voriconazole.
VortioxetineThe serum concentration of Vortioxetine can be decreased when it is combined with Enzalutamide.
WarfarinThe serum concentration of Warfarin can be decreased when it is combined with Enzalutamide.
ZaleplonThe serum concentration of Zaleplon can be decreased when it is combined with Enzalutamide.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be decreased when it is combined with Enzalutamide.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins. Transcription activation is down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3.
Gene Name:
AR
Uniprot ID:
P10275
Molecular Weight:
98987.9 Da

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
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
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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
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
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
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
Molecular Weight:
141477.255 Da
Comments
comments powered by Disqus
Drug created on June 04, 2013 23:12 / Updated on August 24, 2016 01:53