Multidrug resistance–associated protein 1 (MRP1/ABCC1) is an important membrane transporter that contributes to cellular disposition of many endobiotic and xenobiotic agents, and it can also confer multidrug resistance. This study aimed to investigate the role of human noncoding microRNA-1291 (hsa-miR-1291) in regulation of ABCC1 and drug disposition. Bioinformatics analyses indicated that hsa-...

Disposition kinetics and urinary excretion of levofl oxacin was investigated after a single intravenous dose of 3 mg.kg-1 in male buffalo calves. The drug concentration was estimated in plasma and urine by microbiological assay using E. coli as the test organism. Disposition kinetic parameters were determined using a two-compartment open model and an appropriate dosage schedule was computed. Dr...

Preventing and treating malaria in pregnancy is a global health priority. However little is known regarding the impact of malaria infection on the maternal and fetal disposition of pharmaceuticals and other xenobiotics. Our objective was to characterize expression of key determinants of drug-disposition in maternal and fetal tissues in a validated murine model of experimental placental malaria....

Clinical applications of cancer nanomedicines have been challenged by tumor heterogeneity and patient variation. CT imaging nanoparticle extravasation into solid tumors upon intravenous administration, enabled this novel contrast, provides critical insights on characteristics potential for disposition drug delivery prior to treatment. This is reported Xiuling Lu co-workers in article number 220...

There is increasing evidence that pregnancy alters the function of drug-metabolizing enzymes and drug transporters in a gestationalstage and tissue-specific manner. In vivo probe studies have shown that the activity of several hepatic cytochrome P450 enzymes, such as CYP2D6 and CYP3A4, is increased during pregnancy, whereas the activity of others, such as CYP1A2, is decreased. The activity of s...

Epacadostat (EPAC) is a first-in-class, orally active inhibitor of the enzyme indoleamine 2,3-dioxygenase 1 and has demonstrated promising clinical activity. In humans, three major plasma metabolites have been identified: M9 (a glucuronide-conjugate), M11 (a gut microbiota metabolite), and M12 (a secondary metabolite formed from M11). It is proposed, based on the human pharmacokinetics of EPAC,...

Uptake and efflux transporters determine plasma and tissue concentrations of a broad variety of drugs. They are localized in organs such as small intestine, liver, and kidney, which are critical for drug absorption and elimination. Moreover, they can be found in important blood-tissue barriers such as the blood-brain barrier. Inhibition or induction of drug transporters by coadministered drugs ...

1. Progress in Therapeutics 3 Robert E. Stitzel and Joseph J. McPhillips 2. Mechanisms of Drug Action 10 William W. Fleming 3. Drug Absorption and Distribution 20 Timothy S. Tracy 4. Metabolism and Excretion of Drugs •• Timothy S. Tracy 5. Pharmacokinetics •• Timothy S. Tracy 6. Drug Metabolism and Disposition in Pediatric and Gerontological Stages of Life •• Jeane McCarthy 7. Principles of Tox...