In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin …
D Zhang, TJ Chando, DW Everett, CJ Patten… - Drug Metabolism and …, 2005 - Elsevier
Several human immunodeficiency virus (HIV) protease inhibitors, including atazanavir,
indinavir, lopinavir, nelfinavir, ritonavir, and saquinavir, were tested for their potential to
inhibit uridine 5′-diphospho-glucuronosyltransferase (UGT) activity. Experiments were
performed with human cDNA-expressed enzymes (UGT1A1, 1A3, 1A4, 1A6, 1A9, and 2B7)
as well as human liver microsomes. All of the protease inhibitors tested were inhibitors of
UGT1A1, UGT1A3, and UGT1A4 with IC 50 values that ranged from 2 to 87 μM. The IC 50 …
indinavir, lopinavir, nelfinavir, ritonavir, and saquinavir, were tested for their potential to
inhibit uridine 5′-diphospho-glucuronosyltransferase (UGT) activity. Experiments were
performed with human cDNA-expressed enzymes (UGT1A1, 1A3, 1A4, 1A6, 1A9, and 2B7)
as well as human liver microsomes. All of the protease inhibitors tested were inhibitors of
UGT1A1, UGT1A3, and UGT1A4 with IC 50 values that ranged from 2 to 87 μM. The IC 50 …
