Biochemical pharmacology

The human UDP-glucuronosyltransferase UGT1A3 is highly selective towards N2 in the tetrazole ring of losartan, candesartan, and zolarsartan

A Alonen, M Finel, R Kostiainen

Index: Alonen, Anna; Finel, Moshe; Kostiainen, Risto Biochemical Pharmacology, 2008 , vol. 76, # 6 p. 763 - 772

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Citation Number: 33

Abstract

Losartan, candesartan, and zolarsartan are AT1 receptor antagonists that inhibit the effect of angiotensin II. We have examined their glucuronidation by liver microsomes from several animals and by recombinant human UDP-glucuronosyltransferases (UGTs). Large differences in the production of different glucuronide regioisomers of the three sartans were observed among liver microsomes from human (HLM), rabbit, rat, pig, moose, and bovine. ...