Metabolism of efavirenz and 8-hydroxyefavirenz by P450 2B6 leads to inactivation by two distinct mechanisms.

@article{Bumpus2006MetabolismOE,
  title={Metabolism of efavirenz and 8-hydroxyefavirenz by P450 2B6 leads to inactivation by two distinct mechanisms.},
  author={Namandj{\'e} N Bumpus and Ute M. Kent and Paul F. Hollenberg},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2006},
  volume={318 1},
  pages={
          345-51
        }
}
Efavirenz is a non-nucleoside human immunodeficiency virus (HIV)-1 reverse transcriptase inhibitor used in combination therapy to treat HIV-1. Efavirenz metabolism is catalyzed primarily by the polymorphic enzyme P450 2B6. Metabolism of efavirenz by P450 2B6 and the naturally occurring P450 2B6.4 mutant led to the formation of 8-hydroxyefavirenz. Efavirenz inactivated the 7-ethoxy-4-(trifluoromethyl)coumarin activity of the wild-type P450 2B6 enzyme in a time-, concentration-, and NADPH… CONTINUE READING

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References

Publications referenced by this paper.
SHOWING 1-10 OF 39 REFERENCES

Influence of 516G>T polymorphisms at the gene encoding the CYP450-2B6 isoenzyme on efavirenz plasma concentrations in HIV-infected subjects.

  • Clinical infectious diseases : an official publication of the Infectious Diseases Society of America
  • 2005
VIEW 4 EXCERPTS
HIGHLY INFLUENTIAL

CYP2B6 mediates the in vitro hydroxylation of bupropion: potential drug interactions with other antidepressants.

  • Drug metabolism and disposition: the biological fate of chemicals
  • 2000
VIEW 4 EXCERPTS
HIGHLY INFLUENTIAL

Validation of bupropion hydroxylation as a selective marker of human cytochrome P450 2B6 catalytic activity.

  • Drug metabolism and disposition: the biological fate of chemicals
  • 2000
VIEW 4 EXCERPTS
HIGHLY INFLUENTIAL

Formation of a metabolic intermediate complex of cytochrome P4502B1 by clorgyline.

  • Drug metabolism and disposition: the biological fate of chemicals
  • 1996
VIEW 3 EXCERPTS
HIGHLY INFLUENTIAL

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