| 摘要 |
The present invention is directed to a method of inhibiting CYP3A4 induction. The method involves administering a compound of the following formula: <?in-line-formulae description="In-line Formulae" end="lead"?>R<SUB>1</SUB>-X-(CH<SUB>2</SUB>)<SUB>n</SUB>-N-C-S<?in-line-formulae description="In-line Formulae" end="tail"?> with R<SUB>1</SUB>, X, and n defined herein, binds to a Pregnane X Receptor or Steroid and Xenobiotic Receptor (SXR or NR1I2) under conditions effective to inhibit CYP3A4 gene induction. The present invention also include a method of administering a compound, described herein, together with the CYP3A4 inducer to prevent a loss of efficacy in the subject to whom the CYP3A4 inducer is repeatedly administered. In addition, such compounds can be administered to block the interaction between a CYP3A4 inducer and another drug being administered that is a substrate of CYP3A4.
|
