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
Structure for Abiraterone (DB05812)
- 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)3 or with prednisone for the treatment of metastatic CRPC or metastatic high-risk castration-sensitive prostate cancer (CSPC).4
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- 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.
Target Actions Organism ASteroid 17-alpha-hydroxylase/17,20 lyase inhibitorHumans - 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
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 hydroaldosteronism include fluid retention and hypokalemia. 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Abiraterone can be increased when it is combined with Abametapir. Acebutolol The metabolism of Acebutolol can be decreased when combined with Abiraterone. Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Abiraterone. Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Abiraterone. Acyclovir The serum concentration of Acyclovir can be increased when it is combined with Abiraterone. Agomelatine The serum concentration of Agomelatine can be increased when it is combined with Abiraterone. Albendazole The serum concentration of Albendazole can be increased when it is combined with Abiraterone. Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Abiraterone. Almotriptan The metabolism of Almotriptan can be decreased when combined with Abiraterone. Alogliptin The metabolism of Alogliptin can be decreased when combined with Abiraterone. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - 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
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Abiraterone acetate EM5OCB9YJ6 154229-18-2 UVIQSJCZCSLXRZ-UBUQANBQSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Abiraterone Tablet 500 mg Oral Jamp Pharma Corporation 2022-07-12 Not applicable Canada 
Abiraterone Tablet 250 mg Oral Jamp Pharma Corporation Not applicable Not applicable Canada Abiraterone Accord Tablet, film coated 500 mg Oral Accord Healthcare S.L.U. 2022-06-06 Not applicable EU 
Abiraterone Accord Tablet 250 mg Oral Accord Healthcare S.L.U. 2022-06-06 Not applicable EU Abiraterone Accord Tablet, film coated 500 mg Oral Accord Healthcare S.L.U. 2022-06-06 Not applicable EU Abiraterone acetate Tablet, film coated 500 mg/1 Oral Janssen Biotech, Inc. 2018-03-05 2018-03-06 US 
Abiraterone Krka Tablet, film coated 500 mg Oral Krka, D.D., Novo Mesto 2022-01-18 Not applicable EU Abiraterone Krka Tablet, film coated 500 mg Oral Krka, D.D., Novo Mesto 2022-01-18 Not applicable EU Abiraterone Krka Tablet, film coated 500 mg Oral Krka, D.D., Novo Mesto 2022-01-18 Not applicable EU Abiraterone Mylan Tablet, film coated 1000 mg Oral Mylan Ireland Limited 2021-10-06 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Abiraterone Tablet 250 mg/1 Oral Msn Laboratories Private Limited 2019-07-10 Not applicable US Abiraterone Tablet 250 mg/1 Oral PD-Rx Pharmaceuticals, Inc. 2018-11-23 Not applicable US Abiraterone Tablet 250 mg/1 Oral CivicaScript, LLC 2018-11-23 Not applicable US Abiraterone Tablet 250 mg/1 Oral Hikma Pharmaceuticals USA Inc. 2018-11-23 Not applicable US Abiraterone Tablet 250 mg/1 Oral BluePoint Laboratories 2019-07-10 Not applicable US Abiraterone Tablet 250 mg/1 Oral Novadoz Pharmaceuticals Llc 2019-07-10 Not applicable US Abiraterone acetate Tablet 250 mg/1 Oral Rising Pharmaceuticals, Inc. 2019-02-25 Not applicable US Abiraterone acetate Tablet 250 mg/1 Oral Janssen Biotech, Inc. 2018-02-09 Not applicable US Abiraterone Acetate Tablet, film coated 500 mg/1 Oral Apotex Corp. 2021-07-16 Not applicable US Abiraterone Acetate Tablet 250 mg/1 Oral Florida Pharmaceutical Products, LLC. 2022-08-15 Not applicable US
Categories
- ATC Codes
- L02BX03 — Abiraterone
- Drug Categories
- Androstanes
- Androstenes
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP1A2 Inhibitors (strong)
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors (moderate)
- Cytochrome P-450 CYP2C19 inhibitors (strength unknown)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (moderate)
- Cytochrome P-450 CYP2C8 Inhibitors (weak)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (moderate)
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (moderate)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (moderate)
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Cytochrome P450 17A1 Inhibitors
- Endocrine Therapy
- Enzyme Inhibitors
- Fused-Ring Compounds
- Hormone Antagonists
- Hormone Antagonists and Related Agents
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Steroid Synthesis Inhibitors
- Steroids
- 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
- 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]
- 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]
- FDA Approved Drug Products: Yonsa (abiraterone acetate) tablets for oral use [Link]
- FDA Approved Drug Products: Zytiga (abiraterone acetate) tablets for oral use [Link]
- External Links
- KEGG Drug
- D09701
- PubChem Compound
- 132971
- PubChem Substance
- 175427038
- ChemSpider
- 117349
- BindingDB
- 25458
- 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
Phase Status Purpose Conditions Count 4 Completed Treatment Metastatic Castration Resistant Prostate Cancer (CRPC) 1 4 Completed Treatment Prostate Cancer 1 4 Completed Treatment Refractory, metastatic hormone-refractory Prostate cancer 1 4 Recruiting Supportive Care Castration Resistant Prostatic Cancer / Hormone Refractory Prostate Cancer / Recurrent Prostate Carcinoma / Refractory, metastatic hormone-refractory Prostate cancer / Stage IV Prostate Cancer 1 4 Recruiting Treatment Metastatic Castration Resistant Prostate Cancer (CRPC) 1 3 Active Not Recruiting Treatment Adenocarcinoma of the Prostate / Hormone Resistant Prostate Cancer / Prostate Cancer - Recurrent / Stage IV Prostate Cancer 1 3 Active Not Recruiting Treatment Castration Resistant Prostatic Cancer 1 3 Active Not Recruiting Treatment Metastatic Castration Resistant Prostate Cancer (CRPC) 4 3 Active Not Recruiting Treatment Metastatic Castration-resistent Prostate Cancer 1 3 Active Not Recruiting Treatment Prostate Cancer 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral 1000 mg Tablet Oral 250 mg/1 Tablet Oral 500 mg/1 Tablet, film coated Oral 500 mg/1 Tablet, coated Oral 250 mg Tablet Oral 250.000 mg Tablet Oral 250 mg Tablet Oral 250.00 mg Tablet Oral 1000 mg Tablet 250 MG Tablet, film coated Oral 1000.00 mg Tablet, film coated Oral 250.00 mg Tablet, film coated Oral 500.00 mg Tablet Oral 125 mg/1 Tablet, film coated Oral 250 mg Tablet Oral Tablet, film coated Oral Tablet, film coated Oral 250 mg/1 Tablet, coated Oral 500 mg Tablet Oral 500 mg Tablet, film coated Oral 500 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5604213 No 1997-02-18 2016-12-13 US US8822438 No 2014-09-02 2027-08-24 US US9889144 No 2018-02-13 2034-03-17 US US10292990 No 2019-05-21 2034-05-20 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00305 mg/mL ALOGPS logP 5.1 ALOGPS logP 3.97 Chemaxon logS -5.1 ALOGPS pKa (Strongest Acidic) 18.2 Chemaxon pKa (Strongest Basic) 4.81 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 33.12 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 107.3 m3·mol-1 Chemaxon Polarizability 42.03 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.98 Caco-2 permeable + 0.7245 P-glycoprotein substrate Substrate 0.6583 P-glycoprotein inhibitor I Inhibitor 0.5 P-glycoprotein inhibitor II Non-inhibitor 0.8831 Renal organic cation transporter Non-inhibitor 0.7453 CYP450 2C9 substrate Non-substrate 0.854 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.6478 CYP450 1A2 substrate Inhibitor 0.5124 CYP450 2C9 inhibitor Non-inhibitor 0.8046 CYP450 2D6 inhibitor Non-inhibitor 0.8693 CYP450 2C19 inhibitor Non-inhibitor 0.5349 CYP450 3A4 inhibitor Inhibitor 0.7176 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.5363 Ames test Non AMES toxic 0.8499 Carcinogenicity Non-carcinogens 0.9616 Biodegradation Not ready biodegradable 0.9565 Rat acute toxicity 2.4407 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8318 hERG inhibition (predictor II) Non-inhibitor 0.7059
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
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Use our structured and evidence-based datasets to unlock newinsights 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
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- 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]
- Flockhart Table of Drug Interactions [Link]
- 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
- 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
- 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]
- Flockhart Table of Drug Interactions [Link]
- 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
- 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]
- 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]
- Flockhart Table of Drug Interactions [Link]
- 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
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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
- 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
- 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
- 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
- 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]
- 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 December 03, 2022 06:43