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Identification of the Human Cytochrome P450 Enzymes Involved in the Two Oxidative Steps in the Bioactivation of Clopidogrel to Its Pharmacologically Active Metabolite
TLDR
Identifying the human cytochrome P450 isoforms involved in the two oxidative steps in the bioactivation of clopidogrel to its pharmacologically active metabolite helped explain the role of genetic polymorphism of CYP2C19 and also the effect of potent CYP3A inhibitors on the pharmacokinetics and pharmacodynamics of clopsinogrel in humans and on clinical outcomes.
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 to
INTERACTIONS OF TWO MAJOR METABOLITES OF PRASUGREL, A THIENOPYRIDINE ANTIPLATELET AGENT, WITH THE CYTOCHROMES P450
TLDR
Scaling of in vitro intrinsic clearance values from expressed enzymes to the whole liver using a relative abundance approach indicated that either CYP3A4 alone or CYP4 and CYP2B6 are the major contributors to R-138727 formation, which is expected to substantially inhibit the P450-mediated metabolism of coadministered drugs.
Predictability of Idiosyncratic Drug Toxicity Risk for Carboxylic Acid-Containing Drugs Based on the Chemical Stability of Acyl Glucuronide
TLDR
The KPB system was considered to be the best for evaluating the stability of AGs, and the classification value of the half-life in KPB serves as a useful key predictor for the IDT risk.
The Disposition of Prasugrel, a Novel Thienopyridine, in Humans
TLDR
Prasugrel was extensively metabolized in humans, first by hydrolysis to a thiolactone, followed by ring opening to form R-138727, which was further metabolized by S-methylation and conjugation with cysteine, suggesting limited penetration of prasug Rel metabolites into red blood cells.
Comparison of mechanism-based inhibition of human cytochrome P450 2C19 by ticlopidine, clopidogrel, and prasugrel
TLDR
Clopidogrel is potent mechanism-based inhibitors of CYP2C19 as well as ticlopidine, whereas prasugrel did not inactivate CYP 2C19, andimation of in vivo drug–drug interaction using in vitro parameters predicted clinically observed data.
A Zone Classification System for Risk Assessment of Idiosyncratic Drug Toxicity Using Daily Dose and Covalent Binding
TLDR
A zone classification system is established using covalent binding in human hepatocytes and daily dose for the risk assessment of idiosyncratic drug toxicity (IDT) and it is indicated that both covalents binding and daily doses were significantly correlated with safety category and that covalENT binding in hepatocytes was the best predictor among the three systems.
Human Pharmacokinetic Prediction of UDP-Glucuronosyltransferase Substrates with an Animal Scale-Up Approach
TLDR
Monkeys would be more reliable than other animal species in predicting human pharmacokinetics and fm,UGT for drugs metabolized by UGTs.
Quantitative determination of clopidogrel active metabolite in human plasma by LC-MS/MS.
TLDR
The validated method was successfully used to analyze clinical samples and determine the pharmacokinetics of clopidogrel AM.
6β-Hydroxycortisol Is an Endogenous Probe for Evaluation of Drug–Drug Interactions Involving a Multispecific Renal Organic Anion Transporter, OAT3/SLC22A8, in Healthy Subjects
TLDR
It is suggested that 6β-OHF can be used to investigate the perpetrators of the pharmacokinetic drug interactions involving OAT3 in humans using the appropriate in vivo inhibitors, probenecid and pyrimethamine, for Oat3 and MATEs.
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