Abiraterone

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Abiraterone
Systematic (IUPAC) name
(3S,8R,9S,10R,13S,14S)-10,13-Dimethyl-17-(3-pyridinyl)-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
Identifiers
CAS number 154229-19-3
ATC code  ?
PubChem 132971
Chemical data
Formula C24H31NO 
Mol. mass 349.51 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

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Legal status
Routes  ?

Abiraterone is currently a drug under investigation for use in prostate cancer. 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.

The results of two Phase II trials indicate that abiraterone may reduce prostate specific antigen (PSA) levels, as well as shrink tumors.[2] A Phase III trial is planned for 2008.

[edit] References

  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. ^ European Society for Medical Oncology. "Hormone inhibitor promising for hard-to-treat prostate cancer." News release. Published July 8, 2007. Last accessed July 10, 2007.