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Abiraterone acetate

Abiraterone acetate
Abiraterone acetate.svg
Clinical data
Trade names Zytiga
AHFS/Drugs.com Monograph
MedlinePlus a611046
License data
Pregnancy
category
  • AU: D
  • US: X (Contraindicated)
Routes of
administration
Oral (tablets)
ATC code L02BX03 (WHO)
Legal status
Legal status
Pharmacokinetic data
Protein binding >99%
Metabolism Esterases, CYP3A4, SULT2A1
Biological half-life 12 ± 5 hours
Excretion Feces (88%), urine (5%)
Identifiers
CAS Number 154229-19-3 N
PubChem (CID) 132971
IUPHAR/BPS 6745
ChemSpider 117349 YesY
UNII G819A456D0 YesY
ChEMBL CHEMBL254328 YesY
Chemical and physical data
Formula C24H31NO
Molar mass 349.509 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  

Abiraterone acetate (INN, USAN, BAN, JAN) (brand names Zytiga, Abiratas, Abretone, Abirapro) is a steroidal CYP17A1 inhibitor and by extension androgen synthesis inhibitor which is used in combination with prednisone in metastatic castration-resistant prostate cancer (previously called hormone-resistant or hormone-refractory prostate cancer) – i.e., prostate cancer not responding to androgen deprivation or treatment with androgen receptor antagonists. It is a prodrug to the active agent abiraterone, and is marketed by Janssen Biotech under the trade name Zytiga. In addition, Intas Pharmaceuticals markets the drug under the trade name Abiratas, Cadila Pharmaceuticals markets the drug as Abretone, and Glenmark Pharmaceuticals as Abirapro.

Abiraterone acetate was approved by the United States Food and Drug Administration on April 28, 2011. The FDA press release made reference to a phase III clinical trial in which abiraterone use was associated with a median survival of 14.8 months versus 10.9 months with placebo; the study was stopped early because of the successful outcome.


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