17α-Alkynyl 3α, 17β-androstanediol non-clinical and clinical pharmacology, pharmacokinetics and metabolism

@article{Ahlem201017Alkynyl31,
  title={17α-Alkynyl 3α, 17β-androstanediol non-clinical and clinical pharmacology, pharmacokinetics and metabolism},
  author={C. Ahlem and Michael R. Kennedy and Theodore M. Page and D. Bell and E. Delorme and S. Villegas and C. Reading and S. White and D. Stickney and J. Frincke},
  journal={Investigational New Drugs},
  year={2010},
  volume={30},
  pages={59-78}
}
  • C. Ahlem, Michael R. Kennedy, +7 authors J. Frincke
  • Published 2010
  • Medicine
  • Investigational New Drugs
  • Summary17α-ethynyl-5α-androstane-3α, 17β-diol (HE3235, Apoptone) is an orally bioavailable synthetic analogue of 3β-androstanediol, that is active in rodent models of prostate and breast cancer, and is in Phase IIa clinical trials for the treatment of early- and late-stage prostate cancer. In preparation for clinical studies, nuclear hormone receptor and P450 interactions for HE3235 and major metabolites were characterized in vitro, and pharmacokinetics and metabolite profiles were studied in… CONTINUE READING
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