Description

Simple

An anti-tumor hormone therapy used for the treatment of certain types of prostate cancer.

Clinical

An antiandrogen used in the treatment of prostate cancer.

Overview

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.

Pharmacology

Indication

Used in combination with prednisone for the treatment of metastatic, castration-resistant prostate cancer.

Pharmacodynamic

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 testic... Read more

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 acetat... Read more

Protein binding

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

Volume of distribution

Vdss= 19,669 ± 13,358 L

Clearance

Information currently not available.

Half life

Terminal elimination half-life = 5-14 hours

Route of elimination

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

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 an... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Pregnancy
      • Drugbank Id: DBCOND0018394

Food Interactions

  • Take on an empty stomach. Giving this medication with food may increase exposure to abiraterone by 4-fold.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The serum concentration of (R)-warfarin can be increased when it is combined with Abiraterone.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Abiraterone.
3-isobutyl-1-methyl-7H-xanthine
The serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Abiraterone.
4-Methoxyamphetamine
The metabolism of 4-Methoxyamphetamine can be decreased when combined with Abiraterone.
5-methoxy-N,N-dimethyltryptamine
The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Abiraterone.
6-O-benzylguanine
The serum concentration of 6-O-benzylguanine can be increased when it is combined with Abiraterone.
7-Deazaguanine
The serum concentration of 7-Deazaguanine can be increased when it is combined with Abiraterone.
7,9-Dimethylguanine
The serum concentration of 7,9-Dimethylguanine can be increased when it is combined with Abiraterone.
8-azaguanine
The serum concentration of 8-azaguanine can be increased when it is combined with Abiraterone.
8-chlorotheophylline
The serum concentration of 8-chlorotheophylline can be increased when it is combined with Abiraterone.
9-Deazaguanine
The serum concentration of 9-Deazaguanine can be increased when it is combined with Abiraterone.
9-Methylguanine
The serum concentration of 9-Methylguanine can be increased when it is combined with Abiraterone.
Acebutolol
The metabolism of Acebutolol can be decreased when combined with Abiraterone.
Acefylline
The serum concentration of Acefylline can be increased when it is 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.
Acetohexamide
The metabolism of Acetohexamide can be decreased when combined with Abiraterone.
Acetylsalicylic acid
The metabolism of Acetylsalicylic acid can be decreased when 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.
2 References
  1. 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. 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