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14-September-2008 11:27:24 - Abiraterone 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-cyclopentaaphenanthren-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. ? Legal status Routes ? 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.1 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.2 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.3 However others have cautioned that it is too early to know whether abiraterone treatment will have long term benefit.45 Results of two Phase II trials indicate that abiraterone may reduce prostate specific antigen PSA levels, as well as shrink tumors.6 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.7 A Phase III trial is planned for 2008.8 References ^ 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. ^ Abiraterone Acetate CB7630. Research and Development Pipeline. Cougar Biotechnology, Inc.. Retrieved on 2008-08-20. ^ 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. doi:10.1200/JCO.2007.15.9749. PMID 18645193. ^ Cole A 2008. Cancer expert doubts claims about prostate cancer trial. BMJ 337: a979. doi:10.1136/bmj.a979. PMID 18653636. ^ 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. ^ Hormone inhibitor promising for hard-to-treat prostate cancer. Press release. European Society for Medical Oncology 2007-07-08. Retrieved on 2008-07-22. ^ Drug for deadly prostate cancer. Health. BBC NEWS 2008-07-21. Retrieved on 2008-08-20. ^ NCT00638690. ClinicalTrials.gov. Retrieved on 2008-08-22. Abiraterone Acetate in Castration-Resistant Prostate Cancer Previously Treated With Docetaxel-Based Chemotherapy News reports New Study Shows Drug Combats Previously Untreatable Prostate Cancers. Press Release. The Institute of Cancer Research 2008-07-22. Retrieved on 2008-08-20. 'The change has been phenomenal'. Health. BBC NEWS 2008-07-21. Retrieved on 2008-08-20. Tablets This pharmacology-related article is a stub. Retrieved from http://en..org/wiki/Abiraterone Categories: Pharmacology stubs | Antiandrogens | Pyridines Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 22 August 2008, at 12:20
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