Abiraterone

Drugbox
IUPAC_name = (3"S",8"R",9"S",10"R",13"S", 14"S")-10,13-Dimethyl-17-(3-pyridinyl)-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro- 1"H"-cyclopenta ["a"] phenanthren-3-ol

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CAS_number = 154229-19-3
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PubChem = 132971
DrugBank =
C=24|H=31|N=1|O=1
molecular_weight = 349.51 g/mol
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Abiraterone is a drug currently 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. [cite journal |author=Attard G, Belldegrun AS, de Bono JS |title=Selective blockade of androgenic steroid synthesis by novel lyase inhibitors as a therapeutic strategy for treating metastatic prostate cancer |journal=BJU Int. |volume=96 |issue=9 |pages=1241–6 |year=2005 |pmid=16287438 |doi=10.1111/j.1464-410X.2005.05821.x] This enzyme is involved in the formation of DHEA and androstenedione, which may ultimately be metabolized into testosterone. Cougar Biotechnology are the biotechnology company conducting the research.cite web | url = http://www.cougarbiotechnology.com/cb7630.html | title = Abiraterone Acetate (CB7630) | author = | authorlink = | coauthors = | date = | format = | work = Research and Development Pipeline | publisher = Cougar Biotechnology, Inc. | pages = | language = | archiveurl = | archivedate = | quote = | accessdate = 2008-08-20]

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.cite journal | author = 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 | title = Phase I Clinical Trial of a Selective Inhibitor of CYP17, Abiraterone Acetate, Confirms That Castration-Resistant Prostate Cancer Commonly Remains Hormone Driven | url = | journal = Journal of Clinical Oncology | volume = 26 | issue = | pages = | year = 2008 | month = | pmid = 18645193| doi = 10.1200/JCO.2007.15.9749 ] However others have cautioned that it is too early to know whether abiraterone treatment will have long term benefit.cite journal | author = Cole A | title = Cancer expert doubts claims about prostate cancer trial | journal = BMJ | volume = 337 | issue = | pages = a979 | year = 2008 | pmid = 18653636 | doi = 10.1136/bmj.a979 | url = ] cite journal | author = Attard G, Reid AH, Dearnaley D, De Bono JS | title = New prostate cancer drug: Prostate cancer's day in the sun | journal = BMJ | volume = 337 | issue = | pages = a1249 | year = 2008 | pmid = 18694888 | doi = 10.1136/bmj.a979 | url = http://www.bmj.com/cgi/eletters/337/jul24_3/a979#199727 ]

Results of two Phase II trials indicate that abiraterone may reduce prostate specific antigen (PSA) levels, as well as shrink tumors. [cite web | url = http://www.esmo.org/news/?news_id=97 | title = Hormone inhibitor promising for hard-to-treat prostate cancer | author = | date = 2007-07-08 | work = Press release | publisher = European Society for Medical Oncology | pages = | language = | doi = | quote = | accessdate = 2008-07-22 ] 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.cite web | url = http://news.bbc.co.uk/2/hi/health/7502238.stm | title = Drug for deadly prostate cancer | author = | authorlink = | coauthors = | date = 2008-07-21 | format = | work = Health | publisher = BBC NEWS | pages = | language = | archiveurl = | archivedate = | quote = | accessdate = 2008-08-20]

A Phase III trial is planned for 2008.cite web | url = http://www.clinicaltrials.gov/ct2/show/NCT00638690 | title = NCT00638690 | author = | authorlink = | coauthors = | date = | format = | work = | publisher = ClinicalTrials.gov | pages = | language = | archiveurl = | archivedate = | quote = Abiraterone Acetate in Castration-Resistant Prostate Cancer Previously Treated With Docetaxel-Based Chemotherapy | accessdate = 2008-08-22]

References

News reports

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