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EFFECT OF CYP3A5 POLYMORPHISM ON TACROLIMUS METABOLIC CLEARANCE IN VITRO
Previous investigations of solid organ transplant patients treated with tacrolimus showed that individuals carrying a CYP3A5*1 allele have lower dose-adjusted trough blood concentrations comparedExpand
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ROLE OF ITRACONAZOLE METABOLITES IN CYP3A4 INHIBITION
Itraconazole (ITZ) is a potent inhibitor of CYP3A in vivo. However, unbound plasma concentrations of ITZ are much lower than its reported in vitro Ki, and no clinically significant interactions wouldExpand
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EVIDENCE OF SIGNIFICANT CONTRIBUTION FROM CYP3A5 TO HEPATIC DRUG METABOLISM
CYP3A4 and CYP3A5 exhibit significant overlap in substrate specificity but can differ in product regioselectivity and formation activity. To further explore this issue, we compared the kinetics ofExpand
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Contribution of Itraconazole Metabolites to Inhibition of CYP3A4 In Vivo
Itraconazole (ITZ) is metabolized in vitro to three inhibitory metabolites: hydroxy‐itraconazole (OH‐ITZ), keto‐itraconazole (keto‐ITZ), and N‐desalkyl‐itraconazole (ND‐ITZ). The goal of this studyExpand
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Processive Pulses of Retinoic Acid Propel Asynchronous and Continuous Murine Sperm Production1
ABSTRACT The asynchronous cyclic nature of spermatogenesis is essential for continual sperm production and is one of the hallmarks of mammalian male fertility. While various mRNA and proteinExpand
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The role of CYP26 enzymes in retinoic acid clearance
Retinoic acid (RA) is a critical signaling molecule that regulates gene transcription and the cell cycle. Understanding of RA signaling has increased dramatically over the past decades, but theExpand
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Qualitative analysis of the role of metabolites in inhibitory drug-drug interactions: literature evaluation based on the metabolism and transport drug interaction database.
Guidance from the Food and Drug Administration on drug interaction studies does not include a specific section on contributions of metabolites to observed inhibitory drug-drug interactions, and theExpand
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Expression and functional characterization of cytochrome P450 26A1, a retinoic acid hydroxylase.
Retinoic acid (RA) is a critical signaling molecule that performs multiple functions required to maintain cellular viability. It is also used in the treatment of some cancers. Enzymes in the CYP26Expand
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The relative importance of CYP26A1 in hepatic clearance of all-trans retinoic acid.
All-trans retinoic acid (RA) is a critical signaling molecule and its concentration is tightly regulated. Several P450 enzymes including CYP26A1, CYP2C8, and CYP3A4 have been proposed to beExpand
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Are Circulating Metabolites Important in Drug–Drug Interactions?: Quantitative Analysis of Risk Prediction and Inhibitory Potency
The potential of metabolites to contribute to drug–drug interactions (DDIs) is not well defined. The aim of this study was to determine the quantitative role of circulating metabolites in inhibitoryExpand
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