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Systematic (IUPAC) name
(3S,8R,9S,10R,13 S,14S)-10,13-dimethyl-17-(pyridin-3-yl)-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1 H-cyclopenta[a]phenanthren-3-ol
CAS number 154229-19-3
ATC code none
PubChem 132971
ChemSpider 117349
Chemical data
Formula C 24H31NO 
Mol. mass 349.509 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?
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Abiraterone is a drug currently under investigation for use in hormone-refractory prostate cancer (prostate cancer not responding to treatment with antiandrogens). It blocks the formation of testosterone by inhibiting CYP17A1 (CYP450c17), an enzyme also known as 17α-hydroxylase/17,20 lyase.[1] This enzyme is involved in the formation of DHEA and androstenedione, which may ultimately be metabolized into testosterone. This drug was initially discovered and developed at the Institute of Cancer Research in London. Cougar Biotechnology is the biotechnology company conducting the research.[2 ] It has been announced that Cougar will be acquired by Johnson & Johnson in 2009. Subsequent to merger, J&J will conduct trials.[3]


Clinical studies

The first study run at the Royal Marsden Hospital, London, in patients who had not received chemotherapy reported that abiraterone acetate induced decline in prostate specific antigen in up to 70% of patients as well as radiological shrinkage of tumors, symptom improvement, normalization of lactate dehydrogenase.[4] However others have cautioned that it is too early to know whether abiraterone treatment will have long term benefit.[5][6]

Results of two Phase II trials indicate that abiraterone may reduce prostate specific antigen (PSA) levels, as well as shrink tumors.[7] Many of the 21 men in the Phase II trial reported significant improvements in their quality of life and several were able to stop taking morphine, used to control the pain caused after the cancer spread into their bones.[8] On average, progression-free survival was prolonged by 161 days in patients which had been treated with chemotherapy, and by 236 days in chemotherapy naive patients.[9]

A Phase III trial in subjects previously treated with docetaxel started in 2008 and is now closed to accrual.[10 ] A placebo-randomized phase III clincal trial in patients with castration-refractory prostate cancer who are chemotherapy-naive opened to accrual in April 2009.[11 ]


  1. ^ Attard G, Belldegrun AS, de Bono JS (2005). "Selective blockade of androgenic steroid synthesis by novel lyase inhibitors as a therapeutic strategy for treating metastatic prostate cancer". BJU Int. 96 (9): 1241–6. doi:10.1111/j.1464-410X.2005.05821.x. PMID 16287438.  
  2. ^ "Abiraterone Acetate (CB7630)". Research and Development Pipeline. Cougar Biotechnology, Inc.. Retrieved 2008-08-20.  
  3. ^ "Johnson & Johnson Announces Definitive Agreement to Acquire Cougar Biotechnology, Inc.". Press Release. Cougar Biotechnology, Inc.. 2009-05-11. Retrieved 2009-06-03.  
  4. ^ Attard G, Reid AHM, Yap TA, Raynaud F, Dowsett M, Settatree S, Barrett M, Parker C, Martins V, Folkerd E, Clark J, Cooper CS, Kaye SB, Dearnaley D, Lee G, de Bono JS (2008). "Phase I Clinical Trial of a Selective Inhibitor of CYP17, Abiraterone Acetate, Confirms That Castration-Resistant Prostate Cancer Commonly Remains Hormone Driven". Journal of Clinical Oncology 26: 4563. doi:10.1200/JCO.2007.15.9749. PMID 18645193.  
  5. ^ Cole A (2008). "Cancer expert doubts claims about prostate cancer trial". BMJ 337: a979. doi:10.1136/bmj.a979. PMID 18653636.  
  6. ^ Attard G, Reid AH, Dearnaley D, De Bono JS (2008). "New prostate cancer drug: Prostate cancer's day in the sun". BMJ 337: a1249. doi:10.1136/bmj.a979. PMID 18694888.  
  7. ^ "Hormone inhibitor promising for hard-to-treat prostate cancer". Press release. European Society for Medical Oncology. 2007-07-08. Retrieved 2008-07-22.  
  8. ^ "Drug for deadly prostate cancer". Health. BBC NEWS. 2008-07-21. Retrieved 2008-08-20.  
  9. ^ Ang, J. E.; Olmos, D.; Bono, J. S. D. (March 2009). "CYP17 blockade by abiraterone: further evidence for frequent continued hormone-dependence in castration-resistant prostate cancer". Br. J. Cancer 100 (5): 671–675. doi:10.1038/sj.bjc.6604904. PMID 19223900.   edit
  10. ^ "NCT00638690". Retrieved 2008-08-22. "Abiraterone Acetate in Castration-Resistant Prostate Cancer Previously Treated With Docetaxel-Based Chemotherapy"  
  11. ^ "NCT00887198". Retrieved 2009-12-29. "Abiraterone Acetate in Asymptomatic or Mildly Symptomatic Patients With Metastatic Castration-Resistant Prostate Cancer"  

News reports

See also

  • MDV3100, another drug against hormone-refractory prostate cancer


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