Oxidation of the angiotensin II receptor antagonist losartan (DuP 753) in human liver microsomes. Role of cytochrome P4503A(4) in formation of the active metabolite EXP3174.

@article{Yun1995OxidationOT,
  title={Oxidation of the angiotensin II receptor antagonist losartan (DuP 753) in human liver microsomes. Role of cytochrome P4503A(4) in formation of the active metabolite EXP3174.},
  author={Chul-Ho Yun and Hye Suk Lee and Jong Kook Rho and Hye Gwang Jeong and F Peter Guengerich},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={1995},
  volume={23 2},
  pages={285-9}
}
The oxidative metabolism of losartan (DuP 753), a novel angiotensin II receptor antagonist, by human liver microsomes and purified cytochrome P450 (P450) enzymes, was studied. The primary route of metabolism of losartan is by oxidation of the C5-hydroxymethyl to the carboxylic acid (EXP3174), which is an active metabolite of losartan. When microsomes prepared from different human liver samples were compared, EXP3174 formation activity was well correlated (r2 = 0.93) with nifedipine oxidation (a… CONTINUE READING