Abiraterone

Identification

Summary

Abiraterone is an antiandrogen used in the treatment of prostate cancer.

Brand Names
Yonsa, Zytiga
Generic Name
Abiraterone
DrugBank Accession Number
DB05812
Background

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.

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 349.509
Monoisotopic: 349.240564619
Chemical Formula
C24H31NO
Synonyms
  • (3β)-17-(pyridin-3-yl)androsta-5,16-dien-3-ol
  • 17-(3-Pyridyl)androsta-5,16-dien-3beta-ol
  • Abiraterona
  • Abiraterone
External IDs
  • CB 7598
  • CB-7598

Pharmacology

Indication

Abiraterone acetate is indicated in combination with methylprednisolone for the treatment of metastatic castration-resistant prostate cancer (CRPC)4 or with prednisone for the treatment of metastatic CRPC or metastatic high-risk castration-sensitive prostate cancer (CSPC).5

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Abiraterone 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 action

Abiraterone 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.

TargetActionsOrganism
ASteroid 17-alpha-hydroxylase/17,20 lyase
inhibitor
Humans
Absorption

Abiraterone 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.

Hover over products below to view reaction partners

Route of elimination

Excreted via feces (~88%) and urine (~5%)

Half-life

Terminal elimination half-life = 5-14 hours

Clearance

Not Available

Adverse Effects
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Toxicity

The human experience of overdose with abiraterone is limited, and there is no specific antidote for abiraterone overdose.4,5 Toxicity 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 hyperaldosteronism include fluid retention and hypokalemia.3 Mineralocorticoid receptor antagonists may be used to treat signs and symptoms.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Abiraterone can be increased when it is combined with Abametapir.
AcebutololThe metabolism of Acebutolol can be decreased when combined with Abiraterone.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Abiraterone.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Abiraterone.
AcyclovirThe serum concentration of Acyclovir can be increased when it is combined with Abiraterone.
AgomelatineThe serum concentration of Agomelatine can be increased when it is combined with Abiraterone.
AlbendazoleThe serum concentration of Albendazole can be increased when it is combined with Abiraterone.
AlfuzosinThe metabolism of Alfuzosin can be decreased when combined with Abiraterone.
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Abiraterone.
AlogliptinThe metabolism of Alogliptin can be decreased when combined with Abiraterone.
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Food Interactions
  • Exercise caution with St. John's Wort. This herb induces CYP3A4 and may increase the serum levels of abiraterone.
  • Take on an empty stomach. Take at least 1 hour before or 2 hours after eating as food may increase exposure to abiraterone by 4-fold.

Products

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dosage, form, labeller, route of administration, and marketing period.
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Product Ingredients
IngredientUNIICASInChI Key
Abiraterone acetateEM5OCB9YJ6154229-18-2UVIQSJCZCSLXRZ-UBUQANBQSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AbirateroneTablet500 mgOralJamp Pharma Corporation2022-07-12Not applicableCanada flag
AbirateroneTablet250 mgOralJamp Pharma CorporationNot applicableNot applicableCanada flag
Abiraterone AccordTablet, film coated500 mgOralAccord Healthcare S.L.U.2022-06-06Not applicableEU flag
Abiraterone AccordTablet250 mgOralAccord Healthcare S.L.U.2022-06-06Not applicableEU flag
Abiraterone AccordTablet, film coated500 mgOralAccord Healthcare S.L.U.2022-06-06Not applicableEU flag
Abiraterone acetateTablet, film coated500 mg/1OralJanssen Biotech, Inc.2018-03-052018-03-06US flag
Abiraterone KrkaTablet, film coated500 mgOralKrka, D.D., Novo Mesto2022-01-18Not applicableEU flag
Abiraterone KrkaTablet, film coated500 mgOralKrka, D.D., Novo Mesto2022-01-18Not applicableEU flag
Abiraterone KrkaTablet, film coated500 mgOralKrka, D.D., Novo Mesto2022-01-18Not applicableEU flag
Abiraterone MylanTablet, film coated1000 mgOralMylan Ireland Limited2021-10-06Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AbirateroneTablet250 mg/1OralPD-Rx Pharmaceuticals, Inc.2018-11-23Not applicableUS flag
AbirateroneTablet250 mg/1OralCivicaScript, LLC2018-11-23Not applicableUS flag
AbirateroneTablet250 mg/1OralMsn Laboratories Private Limited2019-07-10Not applicableUS flag
AbirateroneTablet250 mg/1OralBluePoint Laboratories2019-07-10Not applicableUS flag
AbirateroneTablet250 mg/1OralHikma Pharmaceuticals USA Inc.2018-11-23Not applicableUS flag
AbirateroneTablet250 mg/1OralNovadoz Pharmaceuticals Llc2019-07-10Not applicableUS flag
Abiraterone AcetateTablet, film coated250 mg/1Oralbryant ranch prepack2022-01-05Not applicableUS flag
Abiraterone acetateTablet250 mg/1OralRising Pharmaceuticals, Inc.2019-02-25Not applicableUS flag
Abiraterone AcetateTablet500 mg/1OralAvKARE2021-04-29Not applicableUS flag
Abiraterone AcetateTablet250 mg/1OralGolden State Medical Supply, Inc.2018-10-31Not applicableUS flag

Categories

ATC Codes
L02BX03 — Abiraterone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This 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.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Androstane steroids
Direct Parent
Androgens and derivatives
Alternative Parents
3-beta-hydroxysteroids / 3-beta-hydroxy delta-5-steroids / Delta-5-steroids / Pyridines and derivatives / Heteroaromatic compounds / Secondary alcohols / Cyclic alcohols and derivatives / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds
show 1 more
Substituents
3-beta-hydroxy-delta-5-steroid / 3-beta-hydroxysteroid / 3-hydroxy-delta-5-steroid / 3-hydroxysteroid / Alcohol / Androgen-skeleton / Aromatic heteropolycyclic compound / Azacycle / Cyclic alcohol / Delta-5-steroid
show 11 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
pyridines, 3beta-sterol (CHEBI:68642)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
G819A456D0
CAS number
154229-19-3
InChI Key
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
(3aS,3bR,7S,9aR,9bS,11aS)-9a,11a-dimethyl-1-(pyridin-3-yl)-3H,3aH,3bH,4H,6H,7H,8H,9H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-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

References

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. [Article]
  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. [Article]
  3. Gill D, Gaston D, Bailey E, Hahn A, Gupta S, Batten J, Alex A, Boucher K, Stenehjem D, Agarwal N: Efficacy of Eplerenone in the Management of Mineralocorticoid Excess in Men With Metastatic Castration-resistant Prostate Cancer Treated With Abiraterone Without Prednisone. Clin Genitourin Cancer. 2017 Aug;15(4):e599-e602. doi: 10.1016/j.clgc.2016.12.008. Epub 2017 Jan 5. [Article]
  4. FDA Approved Drug Products: Yonsa (abiraterone acetate) tablets for oral use [Link]
  5. FDA Approved Drug Products: Zytiga (abiraterone acetate) tablets for oral use [Link]
KEGG Drug
D09701
PubChem Compound
132971
PubChem Substance
175427038
ChemSpider
117349
BindingDB
25458
RxNav
1100072
ChEBI
68642
ChEMBL
CHEMBL254328
ZINC
ZINC000003797541
PharmGKB
PA166123407
PDBe Ligand
AER
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Abiraterone_acetate
PDB Entries
3ruk / 4nkv / 4r1z / 4r20 / 6b82 / 6wr1
FDA label
Download (418 KB)
MSDS
Download (480 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentMetastatic Castration-Resistant Prostate Cancer (mCRPC)1
4CompletedTreatmentMetastatic Prostate Cancer1
4CompletedTreatmentProstate Cancer1
4RecruitingSupportive CareCastration Resistant Prostate Cancer / Hormone-Refractory Prostate Cancer / Metastatic Carcinoma of the Prostate / Recurrent Prostate Carcinoma / Stage IV Prostate Cancer1
4RecruitingTreatmentMetastatic Castration-Resistant Prostate Cancer (mCRPC)1
3Active Not RecruitingTreatmentAdenocarcinoma of Prostate / Hormone Resistant Prostate Cancer / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
3Active Not RecruitingTreatmentCastration Resistant Prostate Cancer1
3Active Not RecruitingTreatmentMetastatic Castration-Resistant Prostate Cancer (mCRPC)3
3Active Not RecruitingTreatmentMetastatic Castration-resistent Prostate Cancer1
3Active Not RecruitingTreatmentMetastatic Prostate Cancer2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral1000 mg
TabletOral250 mg/1
TabletOral500 mg/1
Tablet, film coatedOral500 mg/1
Tablet, coatedOral250 mg
TabletOral250.000 mg
TabletOral250 mg
Tablet, film coatedOral250 MG
TabletOral250.00 mg
TabletOral1000 mg
Tablet, film coatedOral1000.00 mg
Tablet, film coatedOral250.00 mg
Tablet, film coatedOral500.00 mg
TabletOral125 mg/1
TabletOral
Tablet, film coatedOral
Tablet, film coatedOral250 mg/1
Tablet, coatedOral500 mg
TabletOral500 mg
Tablet, film coatedOral500 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5604213No1997-02-182016-12-13US flag
US8822438No2014-09-022027-08-24US flag
US9889144No2018-02-132034-03-17US flag
US10292990No2019-05-212034-05-20US flag

Properties

State
Solid
Experimental Properties
Not 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
Polarizability42.03 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
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)

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

Targets

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Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
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Kind
Protein
Organism
Humans
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 ...
Gene Name
CYP17A1
Uniprot ID
P05093
Uniprot Name
Steroid 17-alpha-hydroxylase/17,20 lyase
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. [Article]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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. [Article]
  2. Flockhart Table of Drug Interactions [Link]
  3. FDA Approved Drug Products: Yonsa (abiraterone acetate) tablets for oral use [Link]
Kind
Protein
Organism
Humans
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
Uniprot Name
Bile salt sulfotransferase
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. [Article]
Kind
Protein
Organism
Humans
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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. [Article]
  2. Flockhart Table of Drug Interactions [Link]
  3. FDA Approved Drug Products: Yonsa (abiraterone acetate) tablets for oral use [Link]
Kind
Protein
Organism
Humans
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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [Article]
  2. Monbaliu J, Gonzalez M, Bernard A, Jiao J, Sensenhauser C, Snoeys J, Stieltjes H, Wynant I, Smit JW, Chien C: In Vitro and In Vivo Drug-Drug Interaction Studies to Assess the Effect of Abiraterone Acetate, Abiraterone, and Metabolites of Abiraterone on CYP2C8 Activity. Drug Metab Dispos. 2016 Oct;44(10):1682-91. doi: 10.1124/dmd.116.070672. Epub 2016 Aug 8. [Article]
  3. Flockhart Table of Drug Interactions [Link]
  4. FDA Approved Drug Products: Yonsa (abiraterone acetate) tablets for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Malikova J, Brixius-Anderko S, Udhane SS, Parween S, Dick B, Bernhardt R, Pandey AV: CYP17A1 inhibitor abiraterone, an anti-prostate cancer drug, also inhibits the 21-hydroxylase activity of CYP21A2. J Steroid Biochem Mol Biol. 2017 Nov;174:192-200. doi: 10.1016/j.jsbmb.2017.09.007. Epub 2017 Sep 8. [Article]
  2. Benoist GE, Hendriks RJ, Mulders PF, Gerritsen WR, Somford DM, Schalken JA, van Oort IM, Burger DM, van Erp NP: Pharmacokinetic Aspects of the Two Novel Oral Drugs Used for Metastatic Castration-Resistant Prostate Cancer: Abiraterone Acetate and Enzalutamide. Clin Pharmacokinet. 2016 Nov;55(11):1369-1380. doi: 10.1007/s40262-016-0403-6. [Article]
  3. 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. [Article]
  4. Abiraterone FDA label [File]
Kind
Protein
Organism
Humans
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Goldberg T, Berrios-Colon E: Abiraterone (zytiga), a novel agent for the management of castration-resistant prostate cancer. P T. 2013 Jan;38(1):23-6. [Article]
  2. 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. [Article]
  3. Zytiga product monograph [File]
Kind
Protein
Organism
Humans
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 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. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
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 colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
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...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
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. [Article]

Transporters

Kind
Protein
Organism
Humans
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, methotre...
Gene Name
ABCC1
Uniprot ID
P33527
Uniprot Name
Multidrug resistance-associated protein 1
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. [Article]
  2. Benoist GE, Hendriks RJ, Mulders PF, Gerritsen WR, Somford DM, Schalken JA, van Oort IM, Burger DM, van Erp NP: Pharmacokinetic Aspects of the Two Novel Oral Drugs Used for Metastatic Castration-Resistant Prostate Cancer: Abiraterone Acetate and Enzalutamide. Clin Pharmacokinet. 2016 Nov;55(11):1369-1380. doi: 10.1007/s40262-016-0403-6. [Article]

Drug created at November 18, 2007 18:28 / Updated at March 19, 2023 23:50