Hydrolysis of angiotensin II receptor blocker prodrug olmesartan medoxomil by human serum albumin and identification of its catalytic active sites.

@article{Ma2005HydrolysisOA,
  title={Hydrolysis of angiotensin II receptor blocker prodrug olmesartan medoxomil by human serum albumin and identification of its catalytic active sites.},
  author={Siyuan Ma and Makoto Anraku and Y. Iwao and Keishi Yamasaki and Ulrich Kragh-Hansen and Noriyuki Yamaotsu and Shuichi Hirono and Toshihiko Ikeda and Masaki Otagiri},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2005},
  volume={33 12},
  pages={
          1911-9
        }
}
In the present study, we investigated the esterase-like activity of human serum albumin (HSA) and the mechanism by which it hydrolyzes, and thereby activates, olmesartan medoxomil (CS-866), a novel angiotensin II receptor antagonist. CS-866 has previously been shown to be rapidly hydrolyzed in serum in which HSA appeared to play the most important role in catalyzing the hydrolysis. We found that the hydrolysis of CS-866 by HSA followed Michaelis-Menten kinetics. Compared with the release of p… CONTINUE READING

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Two prodrugs activated by serum esterases including albumin

  • T Ikeda
  • Proceedings of the International Symposium on…
  • 2000
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