High-Performance Liquid Chromatographic Determination of the Enantiomers of the Benzoquinolinone LY 191704, a Human Type 1 5α-Reductase Inhibitor, in Plasma
March 1997
in “
Journal of Chromatography B: Biomedical Sciences and Applications
”
5α-reductase inhibitor androgenic alopecia benign prostate hyperplasia acne prostate cancer enantiomers stereoselective disposition first-pass metabolism 5-alpha reductase inhibitor male pattern baldness BPH pimples cancer of the prostate mirror-image molecules selective distribution initial metabolism
TLDR Researchers developed a method to measure different forms of a drug that could help treat prostate issues and hair loss, and found how these forms behave in animals.
In 1997, researchers developed an HPLC method to determine the enantiomeric ratio of LY300502 and LY300503, enantiomers of LY191704, a selective inhibitor of the enzyme human type 1 5α-reductase, which is linked to prostate cancer, benign prostate hyperplasia, acne, and androgenic alopecia. The method used extraction from rat and dog plasma and achieved enantiomer recovery rates of 82% to 96% with accuracy ranging from 88% to 114%. The study revealed stereoselective and species-specific disposition of the enantiomers in rats and dogs, with one enantiomer experiencing greater first-pass metabolism in rats. This research aided in selecting the most promising compound for further development based on the in vivo behavior of the enantiomers.
