Results 11 to 20 of about 76,948 (211)
Alflutinib (AST2818), primarily metabolized by CYP3A4, is a potent CYP3A4 inducer [PDF]
Acta Pharmacologica Sinica, 2020 Alflutinib (AST2818) is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Previous study has shown that after multiple dosages, alflutinib exhibits nonlinear pharmacokinetics and displays a time- and dose-dependent increase in the apparent clearance, probably due to its
Liu, Xiao-yun +8 more
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CYP3A4 and CYP3A5genotyping by Pyrosequencing [PDF]
BMC Medical Genetics, 2005 Human cytochrome P450 3A enzymes, particularly CYP3A4 and CYP3A5, play an important role in drug metabolism. CYP3A expression exhibits substantial interindividual variation, much of which may result from genetic variation. This study describes Pyrosequencing assays for key SNPs in CYP3A4 (CYP3A4*1B, CYP3A4*2, and CYP3A4*3) and CYP3A5 (CYP3A5*3C and ...
McLeod Howard L +2 more
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CYP3A4 intronic SNP rs35599367 (CYP3A4*22) alters RNA splicing [PDF]
Pharmacogenetics and Genomics, 2016 Cytochrome P450 3A4 (CYP3A4) metabolizes 30-50% of clinically used drugs. Large interperson variability in CYP3A4 activity affects response to CYP3A4 substrate drugs. We had demonstrated that an intronic single nucleotide polymorphism rs35599367 (CYP3A4*22, located in intron 6) reduces mRNA/protein expression; however, the underlying mechanism remained
Danxin, Wang, Wolfgang, Sadee
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An epoxidation mechanism of carbamazepine by CYP3A4 [PDF]
Bioorganic & Medicinal Chemistry, 2008 Human CYP3A4 catalyzes the 10,11-epoxidation of carbamazepine (CBZ). However, the epoxide is less stable in terms of potential energy than hydroxides of the six-membered aromatic ring. To clarify the reason why CYP3A4 produces such an energetically unfavorable compound, the mechanism of epoxidation of CBZ by CYP3A4 was investigated by theoretical ...
Hata, Masayuki +8 more
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Metabolism and Metabolic Inhibition of Xanthotoxol in Human Liver Microsomes [PDF]
, 2016 Cytochrome p450 (CYP450) enzymes are predominantly involved in Phase I metabolism of xenobiotics. In this study, the CYP450 isoforms involved in xanthotoxol metabolism were identified using recombinant CYP450s.
Cai, Jiqun +5 more
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The Use of Isomeric Testosterone Dimers to Explore Allosteric Effects in Substrate Binding to Cytochrome P450 CYP3A4 [PDF]
, 2016 : Cytochrome P450 CYP3A4 is the main drug-metabolizing enzyme in the human liver, being responsible for oxidation of 50% of all pharmaceuticals metabolized by human P450 enzymes.
Bastien, Dominic +6 more
core +2 more sources
World Journal of Traditional Chinese Medicine, 2021 Objective: To explore the mechanism underlying the effect of Panax notoginseng saponins (PNS) on the pharmacokinetics of nifedipine (NF) in rats. Materials and Methods: Twenty-four rats were randomly divided into blank (BL) group, PNS group, NF group ...
Qiu-Hong Li +7 more
doaj +1 more source
Physiology-based IVIVE predictions of tramadol from in vitro metabolism data [PDF]
, 2014 To predict the tramadol in vivo pharmacokinetics in adults by using in vitro metabolism data and an in vitro-in vivo extrapolation (IVIVE)-linked physiologically-based pharmacokinetic (PBPK) modeling and simulation approach (SimcypA (R)).
Allegaert, Karel +10 more
core +1 more source
Imidazopyridines as selective CYP3A4 inhibitors [PDF]
Bioorganic & Medicinal Chemistry Letters, 2012 Cytochrome P450s are the major family of enzymes responsible for the oxidative metabolism of pharmaceuticals and xenobiotics. CYP3A4 and CYP3A5 have been shown to have overlapping substrate and inhibitor profiles and their inhibition has been demonstrated to be involved in numerous pharmacokinetic drug-drug interactions. Here we report the first highly
Xinyi, Song +6 more
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In vitro inhibitory effects of dihydromyricetin on human liver cytochrome P450 enzymes
Pharmaceutical Biology, 2017 Context: Dihydromyricetin (DHM) is the most abundant and active flavonoid component isolated from Ampelopsis grossedentata (Hand-Mazz) W.T. Wang (Vitaceae) and it possesses numerous pharmacological activities. However, whether DHM affects the activity of
Lu Liu +3 more
doaj +1 more source