Grapefruit juice has been found to significantly increase oral bioavailability of several drugs
metabolized by cytochrome P450 3A4 (P450 3A4) through inhibiting the enzymatic activity …

The bile salt export pump protein (BSEP), expressed on the canalicular membranes of
hepatocytes, is primarily responsible for the biliary excretion of bile salts. The inhibition of BSEP …

Troglitazone (TGZ), the first glitazone used for the treatment of type II diabetes mellitus and
removed from the market for liver toxicity, was shown to bind covalently to microsomal protein …

Atorvastatin (AT) is a second-generation potent inhibitor of 3-hydroxy-3-methylglutaryl-CoA
reductase, clinically approved for lowering plasma cholesterol. Using a mixture of [D 5 /D 0 ] …

1. Tacrine (1,2,3,4‐tetrahydro‐9‐aminoacridine‐hydrochloride: THA) underwent metabolism
in vitro by a panel (n = 12) of human liver microsomes genotyped for CYP2D6, in the …

Mifepristone (RU486), an 11β-substituted nor-steroid containing a 17α-1-propynyl group
used clinically as an antiprogestin agent for medical abortions, was demonstrated to be a …

Oxicam class nonsteroidal antiinflammatory drugs (NSAIDs) display many of the clinical
properties of aspirin-like drugs including analgesic, antipyretic,

1. (Z)- and (E)-6-Hydroxyketamine have been synthesized and their metabolism by hepatic
microsomal preparations studied to elucidate the metabolism of ketamine. 2. Both 6-…

Tacrine (1,2,3,4-tetrahydro-9-aminoacridine hydrochloride; THA) is known to undergo
extensive oxidative metabolism to a variety of mono- and dihydroxylated metabolites in animals …

Interference of bile salt transport is one of the underlying mechanisms for drug-induced liver
injury (DILI). We developed a novel bile salt transport activity assay involving in situ …