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The conduct of in vitro and in vivo drug-drug interaction studies: a Pharmaceutical Research and Manufacturers of America (PhRMA) perspective.
Current regulatory guidances do not address specific study designs for in vitro and in vivo drug-drug interaction studies. There is a common desire by regulatory authorities and by industry sponsorsExpand
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Comparative metabolic capabilities of CYP3A4, CYP3A5, and CYP3A7.
The human cytochromes P450 (P450) CYP3A contribute to the biotransformation of 50% of oxidatively metabolized drugs. The predominant hepatic form is CYP3A4, but recent evidence indicates that CYP3A5Expand
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In vitro glucuronidation using human liver microsomes and the pore-forming peptide alamethicin.
The UDP-glucuronosyltransferases (UGTs) are a superfamily of membrane-bound enzymes whose active site is localized inside the endoplasmic reticulum. Glucuronidation using human liver microsomes hasExpand
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Hepatic CYP2B6 Expression: Gender and Ethnic Differences and Relationship to CYP2B6 Genotype and CAR (Constitutive Androstane Receptor) Expression
CYP2B6 metabolizes many drugs, and its expression varies greatly. CYP2B6 genotype-phenotype associations were determined using human livers that were biochemically phenotyped for CYP2B6 (mRNA,Expand
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The human pregnane X receptor: genomic structure and identification and functional characterization of natural allelic variants.
The pregnane X receptor (PXR)/steroid and xenobiotic receptor (SXR) transcriptionally activates cytochrome P4503A4 (CYP3A4) when ligand activated by endobiotics and xenobiotics. We cloned the humanExpand
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Studies on the expression and metabolic capabilities of human liver cytochrome P450IIIA5 (HLp3).
The human P450III family has been shown to be composed of at least four members, P450IIIA3 (HLp), P450IIIA4 (P450NF), P450IIIA5 (HLp3), and P450IIIA6 (HLp2). Due to the lack of probes thatExpand
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Regioselective biotransformation of midazolam by members of the human cytochrome P450 3A (CYP3A) subfamily.
The capabilities of cytochrome P4503A4 (CYP3A4), CYP3A5, and fetal hepatic microsomes containing CYP3A7 to metabolize midazolam were investigated using human hepatic microsomes and purified CYP3A4Expand
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Isolation and characterization of human liver cytochrome P450 2C19: correlation between 2C19 and S-mephenytoin 4'-hydroxylation.
In an effort to identify and characterize minor forms of human liver cytochrome P450, immunoblot analyses of microsome samples were developed with antibodies to various P450s that recognized multipleExpand
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The role of hepatic and extrahepatic UDP-glucuronosyltransferases in human drug metabolism*†
At present, the methods and enzymology of the UDP-glucuronosyltransferases (UGTs) lag behind that of the cytochromes P450 (CYPs). About 15 human UGTs have been identified, and knowledge about theirExpand
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Metabolism and Disposition of the Thienopyridine Antiplatelet Drugs Ticlopidine, Clopidogrel, and Prasugrel in Humans
Ticlopidine, clopidogrel, and prasugrel are thienopyridine prodrugs that inhibit adenosine‐5′‐diphosphate (ADP)‐mediated platelet aggregation in vivo. These compounds are converted toExpand
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