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The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors.
Currently available HIV-1 protease inhibitors are potent agents in the therapy of HIV-1 infection. However, limited oral absorption and variable tissue distribution, both of which are largelyExpand
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OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine.
Fexofenadine, a nonsedating antihistamine, does not undergo significant metabolic biotransformation. Accordingly, it was hypothesized that uptake and efflux transporters could be importantly involvedExpand
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Identification of functionally variant MDR1 alleles among European Americans and African Americans
MDR1 (P‐glycoprotein) is an important factor in the disposition of many drugs, and the involved processes often exhibit considerable interindividual variability that may be genetically determined.Expand
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Drug metabolism and variability among patients in drug response.
  • G. Wilkinson
  • Medicine
  • The New England journal of medicine
  • 26 May 2005
Differences in drug responsiveness are common, often leading to challenges in optimizing the dosage regimen for a particular patient. Recent advances provide a rational framework for understandingExpand
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A physiological approach to hepatic drug clearance
A physiological approach has been developed recognizing that hepatic blood flow, the activity of the overall elimination process (intrinsic clearance), drug binding in the blood, and the anatomicalExpand
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Oral first‐pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A‐mediated metabolism
To determine in humans the relative roles of intestinal and hepatic metabolism in the oral first‐pass elimination of a CYP3A substrate using midazolam as a model compound.
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Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study
Objectives: Efavirenz is an effective antiretroviral agent, but central nervous system side effects occur commonly, and population (racial) differences in pharmacokinetics and response have beenExpand
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Genetic variability in CYP3A5 and its possible consequences.
The cytochrome P450 3A (CYP3A) subfamily members are the most abundant and important drug-metabolizing enzymes in humans, and wide interindividual variability in CYP3A expression and function isExpand
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The major genetic defect responsible for the polymorphism of S-mephenytoin metabolism in humans.
The metabolism of the anticonvulsant drug mephenytoin exhibits a genetic polymorphism in humans, with the poor metabolizer trait being inherited in an autosomal recessive fashion. There are largeExpand
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Commentary: a physiological approach to hepatic drug clearance.
A physiological approach has been developed recognizing that hepatic blood flow, the activity of the overall elimination process (intrinsic clearance), drug binding in the blood, and the anatomicalExpand
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