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Identification
NameAbiraterone
Accession NumberDB05812
TypeSmall Molecule
GroupsApproved
Description

Abiraterone is a derivative of steroidal progesterone and is an innovative drug that offers clinical benefit to patients with hormone refractory prostate cancer. Abiraterone is administered as an acetate salt prodrug because it has a higher bioavailability and less susceptible to hydrolysis than abiraterone itself. FDA approved on April 28, 2011.

Structure
Thumb
Synonyms
(3beta)-17-(Pyridin-3-yl)androsta-5,16-dien-3-ol
17-(3-Pyridyl)androsta-5,16-dien-3beta-ol
External Identifiers
  • CB7630
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Zytigatablet250 mg/1oralJanssen Biotech, Inc.2011-04-28Not applicableUs
Zytigatablet250 mgoralJanssen Inc2011-07-28Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Abiraterone acetate
ThumbNot applicableDBSALT001173
Categories
UNIIG819A456D0
CAS number154229-19-3
WeightAverage: 349.509
Monoisotopic: 349.240564619
Chemical FormulaC24H31NO
InChI KeyInChIKey=GZOSMCIZMLWJML-VJLLXTKPSA-N
InChI
InChI=1S/C24H31NO/c1-23-11-9-18(26)14-17(23)5-6-19-21-8-7-20(16-4-3-13-25-15-16)24(21,2)12-10-22(19)23/h3-5,7,13,15,18-19,21-22,26H,6,8-12,14H2,1-2H3/t18-,19-,21-,22-,23-,24+/m0/s1
IUPAC Name
(1S,2R,5S,10R,11S,15S)-2,15-dimethyl-14-(pyridin-3-yl)tetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-7,13-dien-5-ol
SMILES
[H][C@@]12CC=C(C3=CC=CN=C3)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC=C2C[C@@H](O)CC[C@]12C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as androgens and derivatives. These are 3-hydroxylated C19 steroid hormones. They are known to favor the development of masculine characteristics. They also show profound effects on scalp and body hair in humans.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassAndrostane steroids
Direct ParentAndrogens and derivatives
Alternative Parents
Substituents
  • Androgen-skeleton
  • 3-beta-hydroxysteroid
  • 3-beta-hydroxy-delta-5-steroid
  • Hydroxysteroid
  • 3-hydroxysteroid
  • 3-hydroxy-delta-5-steroid
  • Delta-5-steroid
  • Pyridine
  • Heteroaromatic compound
  • Cyclic alcohol
  • Secondary alcohol
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed in combination with prednisone for the treatment of metastatic, castration-resistant prostate cancer.
PharmacodynamicsAbiraterone is associated with decreases in PSA levels, tumor shrinkage (as evaluated by RECIST criteria), radiographic regression of bone metastases and improvement in pain. Levels of adrenocorticotropic hormones increased up to 6-fold but this can be suppressed by dexamethasone.
Mechanism of actionAbiraterone is an orally active inhibitor of the steroidal enzyme CYP17A1 (17 alpha-hydroxylase/C17,20 lyase). It inhibits CYP17A1 in a selective and irreversible manner via covalent binding mechanism. CYP17A1 is an enzyme that catalyzes the biosynthesis of androgen and is highly expressed in testicular, adrenal, and prostatic tumor tissue. More specifically, abiraterone inhibits the conversion of 17-hydroxyprognenolone to dehydroepiandrosterone (DHEA) by the enzyme CYP17A1 to decrease serum levels of testosterone and other androgens.
Related Articles
AbsorptionAbiraterone itself is poorly absorbed and is susceptible to hydrolysis by esterases. The salt form, abiraterone acetate, is a prodrug which has a much higher oral bioavailability and is also esterase resistant. Peak drug concentrations of abiraterone were reached in 1.5 - 4 hours. Abiraterone acetate was rapidly and completely deacetylated into abiraterone-the parent salt form was not detectable in early pharmacokinetic studies. Food and high fat meals increases absorption 4.4-fold.
Volume of distribution

Vdss= 19,669 ± 13,358 L

Protein binding>99% protein bound to alpha-1-acid glycoprotein and albumin.
Metabolism

Abiraterone acetate is hydrolyzed into active metabolite abiraterone via esterases. CYP3A4 and SULT2A1 further metabolizes abiraterone into two inactive metabolites called abiraterone sulfate and N-oxide abiraterone sulfate.

SubstrateEnzymesProduct
Abiraterone
Not Available
abiraterone sulfateDetails
Abiraterone
Not Available
N-oxide abiraterone sulfateDetails
Route of eliminationExcreted via feces (~88%) and urine (~5%)
Half lifeTerminal elimination half-life = 5-14 hours
ClearanceNot Available
ToxicityToxicity is related to the blockade of 17α-hydroxylase activity. Blockade results in the accumulation of upstream mineralocorticoids like 11-deoxycorticosterone leading to secondary hyperaldosteronism. Signs of hydroaldosteronism include fluid retention and hypokalemia. Mineralocorticoid receptor antagonists may be used to treat signs and symptoms.
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+1.0
Blood Brain Barrier+0.98
Caco-2 permeable+0.7245
P-glycoprotein substrateSubstrate0.6583
P-glycoprotein inhibitor IInhibitor0.5
P-glycoprotein inhibitor IINon-inhibitor0.8831
Renal organic cation transporterNon-inhibitor0.7453
CYP450 2C9 substrateNon-substrate0.854
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6478
CYP450 1A2 substrateInhibitor0.5124
CYP450 2C9 inhibitorNon-inhibitor0.8046
CYP450 2D6 inhibitorNon-inhibitor0.8693
CYP450 2C19 inhibitorNon-inhibitor0.5349
CYP450 3A4 inhibitorInhibitor0.7176
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5363
Ames testNon AMES toxic0.8499
CarcinogenicityNon-carcinogens0.9616
BiodegradationNot ready biodegradable0.9565
Rat acute toxicity2.4407 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8318
hERG inhibition (predictor II)Non-inhibitor0.7059
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral250 mg/1
Tabletoral250 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5604213 No1996-12-132016-12-13Us
US8822438 No2007-08-242027-08-24Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.00305 mg/mLALOGPS
logP5.1ALOGPS
logP3.97ChemAxon
logS-5.1ALOGPS
pKa (Strongest Acidic)18.2ChemAxon
pKa (Strongest Basic)4.81ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area33.12 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity107.3 m3·mol-1ChemAxon
Polarizability42.04 Å3ChemAxon
Number of Rings5ChemAxon
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. O'Donnell A, Judson I, Dowsett M, Raynaud F, Dearnaley D, Mason M, Harland S, Robbins A, Halbert G, Nutley B, Jarman M: Hormonal impact of the 17alpha-hydroxylase/C(17,20)-lyase inhibitor abiraterone acetate (CB7630) in patients with prostate cancer. Br J Cancer. 2004 Jun 14;90(12):2317-25. [PubMed:15150570 ]
  2. Ryan CJ, Cheng ML: Abiraterone acetate for the treatment of prostate cancer. Expert Opin Pharmacother. 2013 Jan;14(1):91-6. doi: 10.1517/14656566.2013.745852. Epub 2012 Nov 30. [PubMed:23199349 ]
External Links
ATC CodesL02BX03
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (418 KB)
MSDSDownload (480 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Abiraterone.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Abiraterone.
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Abiraterone.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Abiraterone.
AmiodaroneThe serum concentration of Amiodarone can be increased when it is combined with Abiraterone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Abiraterone.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Abiraterone.
AmoxapineThe serum concentration of Amoxapine can be increased when it is combined with Abiraterone.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Abiraterone.
AsenapineThe serum concentration of Asenapine can be increased when it is combined with Abiraterone.
AtomoxetineThe serum concentration of Atomoxetine can be increased when it is combined with Abiraterone.
BetaxololThe serum concentration of Betaxolol can be increased when it is combined with Abiraterone.
BexaroteneThe serum concentration of Abiraterone can be decreased when it is combined with Bexarotene.
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Abiraterone.
BosentanThe serum concentration of Abiraterone can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Abiraterone.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Abiraterone.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Abiraterone.
BromazepamThe serum concentration of Bromazepam can be increased when it is combined with Abiraterone.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Abiraterone.
CapromabAbiraterone may decrease effectiveness of Capromab as a diagnostic agent.
CaptoprilThe serum concentration of Captopril can be increased when it is combined with Abiraterone.
CarbamazepineThe serum concentration of Abiraterone can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Abiraterone.
ChloroquineThe serum concentration of Chloroquine can be increased when it is combined with Abiraterone.
ChlorphenamineThe serum concentration of Chlorphenamine can be increased when it is combined with Abiraterone.
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Abiraterone.
Choline C 11The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Abiraterone.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Abiraterone.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Abiraterone.
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Abiraterone.
ClopidogrelThe serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Abiraterone resulting in a loss in efficacy.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Abiraterone.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Abiraterone.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Abiraterone.
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Abiraterone.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Abiraterone.
DabrafenibThe serum concentration of Abiraterone can be decreased when it is combined with Dabrafenib.
DacarbazineThe serum concentration of Dacarbazine can be increased when it is combined with Abiraterone.
DeferasiroxThe serum concentration of Abiraterone can be decreased when it is combined with Deferasirox.
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Abiraterone.
DextromethorphanThe serum concentration of Dextromethorphan can be increased when it is combined with Abiraterone.
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Abiraterone.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Abiraterone.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Abiraterone.
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Abiraterone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Abiraterone.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Abiraterone.
EnzalutamideThe serum concentration of Abiraterone can be decreased when it is combined with Enzalutamide.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Abiraterone.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Abiraterone.
FlecainideThe serum concentration of Flecainide can be increased when it is combined with Abiraterone.
FluoxetineThe serum concentration of Fluoxetine can be increased when it is combined with Abiraterone.
FluphenazineThe serum concentration of Fluphenazine can be increased when it is combined with Abiraterone.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Abiraterone.
FluvoxamineThe serum concentration of Fluvoxamine can be increased when it is combined with Abiraterone.
FosphenytoinThe serum concentration of Abiraterone can be decreased when it is combined with Fosphenytoin.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Abiraterone.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Abiraterone.
IloperidoneThe serum concentration of Iloperidone can be increased when it is combined with Abiraterone.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Abiraterone.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Abiraterone.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Abiraterone.
MaprotilineThe serum concentration of Maprotiline can be increased when it is combined with Abiraterone.
MethamphetamineThe serum concentration of Methamphetamine can be increased when it is combined with Abiraterone.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Abiraterone.
MexiletineThe serum concentration of Mexiletine can be increased when it is combined with Abiraterone.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Abiraterone.
MitotaneThe serum concentration of Abiraterone can be decreased when it is combined with Mitotane.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Abiraterone.
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Abiraterone.
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Abiraterone.
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Abiraterone.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Abiraterone.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Abiraterone.
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Abiraterone.
ParoxetineThe serum concentration of Paroxetine can be increased when it is combined with Abiraterone.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Abiraterone.
PerphenazineThe serum concentration of Perphenazine can be increased when it is combined with Abiraterone.
PhenobarbitalThe serum concentration of Abiraterone can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Abiraterone can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Abiraterone.
PioglitazoneThe serum concentration of Pioglitazone can be increased when it is combined with Abiraterone.
PipotiazineThe serum concentration of Pipotiazine can be increased when it is combined with Abiraterone.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Abiraterone.
PrimaquineThe serum concentration of Primaquine can be increased when it is combined with Abiraterone.
PrimidoneThe serum concentration of Abiraterone can be decreased when it is combined with Primidone.
ProcainamideThe serum concentration of Procainamide can be increased when it is combined with Abiraterone.
PromazineThe serum concentration of Promazine can be increased when it is combined with Abiraterone.
PromethazineThe serum concentration of Promethazine can be increased when it is combined with Abiraterone.
PropafenoneThe serum concentration of Abiraterone can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Abiraterone.
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Abiraterone.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Abiraterone.
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Abiraterone.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Abiraterone.
RasagilineThe serum concentration of Rasagiline can be increased when it is combined with Abiraterone.
RepaglinideThe serum concentration of Repaglinide can be increased when it is combined with Abiraterone.
RifabutinThe serum concentration of Abiraterone can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Abiraterone can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Abiraterone can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Abiraterone.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Abiraterone.
RopiniroleThe serum concentration of Ropinirole can be increased when it is combined with Abiraterone.
RopivacaineThe serum concentration of Ropivacaine can be increased when it is combined with Abiraterone.
RosiglitazoneThe serum concentration of Rosiglitazone can be increased when it is combined with Abiraterone.
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Abiraterone.
SildenafilThe metabolism of Sildenafil can be decreased when combined with Abiraterone.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Abiraterone.
SiltuximabThe serum concentration of Abiraterone can be decreased when it is combined with Siltuximab.
SpironolactoneThe therapeutic efficacy of Abiraterone can be decreased when used in combination with Spironolactone.
St. John's WortThe serum concentration of Abiraterone can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Stiripentol can be increased when it is combined with Abiraterone.
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Abiraterone resulting in a loss in efficacy.
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Abiraterone.
TetrabenazineThe serum concentration of Tetrabenazine can be increased when it is combined with Abiraterone.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Abiraterone.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Abiraterone.
ThiothixeneThe serum concentration of Thiothixene can be increased when it is combined with Abiraterone.
TimololThe serum concentration of Timolol can be increased when it is combined with Abiraterone.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Abiraterone.
TocilizumabThe serum concentration of Abiraterone can be decreased when it is combined with Tocilizumab.
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Abiraterone.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Abiraterone.
TorasemideThe serum concentration of Torasemide can be increased when it is combined with Abiraterone.
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Abiraterone.
TretinoinThe serum concentration of Tretinoin can be increased when it is combined with Abiraterone.
TrifluoperazineThe serum concentration of Trifluoperazine can be increased when it is combined with Abiraterone.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Abiraterone.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Abiraterone.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Abiraterone.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Abiraterone.
VortioxetineThe serum concentration of Vortioxetine can be increased when it is combined with Abiraterone.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be increased when it is combined with Abiraterone.
Food Interactions
  • Food and high fat meals increases the drug exposure 4.4-fold. It is suggested that abiraterone is taken on an empty stomach.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Steroid 17-alpha-monooxygenase activity
Specific Function:
Conversion of pregnenolone and progesterone to their 17-alpha-hydroxylated products and subsequently to dehydroepiandrosterone (DHEA) and androstenedione. Catalyzes both the 17-alpha-hydroxylation and the 17,20-lyase reaction. Involved in sexual development during fetal life and at puberty.
Gene Name:
CYP17A1
Uniprot ID:
P05093
Molecular Weight:
57369.995 Da
References
  1. Vogiatzi P, Claudio PP: Efficacy of abiraterone acetate in post-docetaxel castration-resistant prostate cancer. Expert Rev Anticancer Ther. 2010 Jul;10(7):1027-30. doi: 10.1586/era.10.84. [PubMed:20645691 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
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 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. Beckett RD, Rodeffer KM, Snodgrass R: Abiraterone for the treatment of metastatic castrate-resistant prostate cancer. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1016-24. doi: 10.1345/aph.1Q758. Epub 2012 Jun 19. [PubMed:22714819 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sulfotransferase activity
Specific Function:
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfonation of steroids and bile acids in the liver and adrenal glands.
Gene Name:
SULT2A1
Uniprot ID:
Q06520
Molecular Weight:
33779.57 Da
References
  1. Beckett RD, Rodeffer KM, Snodgrass R: Abiraterone for the treatment of metastatic castrate-resistant prostate cancer. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1016-24. doi: 10.1345/aph.1Q758. Epub 2012 Jun 19. [PubMed:22714819 ]
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
References
  1. Chi KN, Tolcher A, Lee P, Rosen PJ, Kollmannsberger CK, Papadopoulos KP, Patnaik A, Molina A, Jiao J, Pankras C, Kaiser B, Bernard A, Tran N, Acharya M: Effect of abiraterone acetate plus prednisone on the pharmacokinetics of dextromethorphan and theophylline in patients with metastatic castration-resistant prostate cancer. Cancer Chemother Pharmacol. 2013 Jan;71(1):237-44. doi: 10.1007/s00280-012-2001-0. Epub 2012 Oct 12. [PubMed:23064959 ]
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. 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
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 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
References
  1. Ryan CJ, Cheng ML: Abiraterone acetate for the treatment of prostate cancer. Expert Opin Pharmacother. 2013 Jan;14(1):91-6. doi: 10.1517/14656566.2013.745852. Epub 2012 Nov 30. [PubMed:23199349 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da
References
  1. Ryan CJ, Cheng ML: Abiraterone acetate for the treatment of prostate cancer. Expert Opin Pharmacother. 2013 Jan;14(1):91-6. doi: 10.1517/14656566.2013.745852. Epub 2012 Nov 30. [PubMed:23199349 ]

Transporters

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. Beckett RD, Rodeffer KM, Snodgrass R: Abiraterone for the treatment of metastatic castrate-resistant prostate cancer. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1016-24. doi: 10.1345/aph.1Q758. Epub 2012 Jun 19. [PubMed:22714819 ]
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Drug created on November 18, 2007 11:28 / Updated on June 26, 2016 01:53