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http://linked.open...gbank/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. (en)
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http://linked.open...y/drugbank/dosage
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http://linked.open...generalReferences
| - # 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":http://www.ncbi.nlm.nih.gov/pubmed/15150570 # 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":http://www.ncbi.nlm.nih.gov/pubmed/23199349 (en)
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http://linked.open...gy/drugbank/group
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http://linked.open...drugbank/halfLife
| - Terminal elimination half-life = 5-14 hours (en)
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http://linked.open...ugbank/indication
| - Used in combination with prednisone for the treatment of metastatic, castration-resistant prostate cancer. (en)
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sameAs
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Title
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adms:identifier
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http://linked.open...mechanismOfAction
| - 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. (en)
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http://linked.open...y/drugbank/patent
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http://linked.open...outeOfElimination
| - Excreted via feces (~88%) and urine (~5%) (en)
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http://linked.open.../drugbank/synonym
| - (3beta)-17-(Pyridin-3-yl)androsta-5,16-dien-3-ol (en)
- 17-(3-Pyridyl)androsta-5,16-dien-3beta-ol (en)
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http://linked.open...drugbank/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. (en)
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http://linked.open...umeOfDistribution
| - Vdss= 19,669 ± 13,358 L (en)
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http://linked.open.../drug/hasAHFSCode
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http://linked.open...k/foodInteraction
| - Food and high fat meals increases the drug exposure 4.4-fold. It is suggested that abiraterone is taken on an empty stomach. (en)
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http://linked.open...nk/proteinBinding
| - >99% protein bound to alpha-1-acid glycoprotein and albumin. (en)
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foaf:page
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http://linked.open...ugbank/IUPAC-Name
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http://linked.open...gy/drugbank/InChI
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http://linked.open...Molecular-Formula
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http://linked.open.../Molecular-Weight
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http://linked.open...noisotopic-Weight
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http://linked.open...y/drugbank/SMILES
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http://linked.open.../Water-Solubility
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http://linked.open...ogy/drugbank/logP
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http://linked.open...ogy/drugbank/logS
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http://linked.open...l/drug/hasATCCode
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http://linked.open...nd-Acceptor-Count
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http://linked.open...-Bond-Donor-Count
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http://linked.open...drugbank/InChIKey
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http://linked.open...urface-Area--PSA-
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http://linked.open...nk/Polarizability
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http://linked.open...bank/Refractivity
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http://linked.open...atable-Bond-Count
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http://linked.open...ugbank/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. (en)
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http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
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http://linked.open...casRegistryNumber
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http://linked.open...k/Bioavailability
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http://linked.open...bank/Ghose-Filter
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http://linked.open...nk/MDDR-Like-Rule
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http://linked.open...k/Number-of-Rings
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http://linked.open...siological-Charge
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http://linked.open...bank/Rule-of-Five
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http://linked.open...tional-IUPAC-Name
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http://linked.open...strongest-acidic-
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http://linked.open...-strongest-basic-
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