European Journal of Drug Metabolism and Pharmacokinetics This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

Tigecycline Soft Tissue Penetration in Obese and Non-obese Surgical Patients Determined by Using In  Vivo Microdialysis
ConclusionFollowing a single dose of tigecycline, concentrations in the ISF of subcutaneous adipose tissue are decreased in heavily obese subjects, calling for an increased loading dose.EU Clinical Trials Registration NumberEudraCT No. 2012-004383-22. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - August 9, 2022 Category: Drugs & Pharmacology Source Type: research

Is Monitoring of the Intracellular Active Metabolite Levels of Nucleobase and Nucleoside Analogs Ready for Precision Medicine Applications?
This article reviewed the relationships between NA intracellular active metabolite levels and their efficacy or adverse effects. The factors affecting t he formation of intracellular active metabolites and combination regimens that elevate intracellular active metabolite levels were also reviewed. Given the mechanism of NA cytotoxicity, NA intracellular active metabolite levels may be predictive of clinical outcomes. Many clinical studies support th is hypothesis. Therefore, the monitoring of intracellular active metabolite levels is beneficial for individualized NA treatment. However, to perform clinical monitoring in pr...
Source: European Journal of Drug Metabolism and Pharmacokinetics - August 1, 2022 Category: Drugs & Pharmacology Source Type: research

Nonclinical Pharmacokinetic Evaluation of Desidustat: a Novel Prolyl Hydroxylase Inhibitor for the Treatment of Anemia
ConclusionTaken together, desidustat is well absorbed orally. It showed a dose-dependent increase in exposure, did not accumulate in tissue, and was eliminated via dual routes. It is metabolically stable, has minimal potential to cause clinical drug –drug interactions (DDIs), and demonstrates discriminable pharmacokinetic properties for the treatment of anemia. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - July 26, 2022 Category: Drugs & Pharmacology Source Type: research

Population Pharmacokinetic Modeling of Lucitanib in Patients with Advanced Cancer
ConclusionsThe PopPK model adequately described lucitanib pharmacokinetics. High between-subject pharmacokinetic variability supports a safety-based dose-titration strategy currently being used in an ongoing clinical study of lucitanib to optimize drug exposure and clinical benefit.Trial RegistrationClinicalTrials.gov Identifier: NCT01283945, NCT02053636, ISRCTN23201971, NCT02202746, NCT02109016. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - July 18, 2022 Category: Drugs & Pharmacology Source Type: research

Physiologically-Based Pharmacokinetic Models of CYP2D6 Substrate and Inhibitors Nebivolol, Cinacalcet and Mirabegron to Simulate Drug –Drug Interactions
ConclusionsThe developed PBPK models can be used to assess the DDI potential liability of new chemical entities that are substrates or inhibitors of CYP2D6. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - July 15, 2022 Category: Drugs & Pharmacology Source Type: research

Effect of Human Cytochrome P450 2D6 Polymorphism on Progesterone Hydroxylation
ConclusionsThese results suggest that CYP2D6 polymorphism can affect the stimulation/inhibition of progesterone 21-hydroxylation. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - July 15, 2022 Category: Drugs & Pharmacology Source Type: research

External Validation of a Vancomycin Population Pharmacokinetic Model and Developing a New Dosage Regimen in Neonates
ConclusionThe pharmacokinetic model built in the previous study can be used to conduct reliable population simulations of our Asian neonatal population in Singapore. The new dosage regimen was able to achieve target trough concentrations and AUC24 better than existing institutional and NeoFax® dosage regimens. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - July 8, 2022 Category: Drugs & Pharmacology Source Type: research

Contribution of Humanized Liver Chimeric Mice to the Study of Human Hepatic Drug Transporters: State of the Art and Perspectives
AbstractChimeric mice with humanized livers constitute an attractive emergent experimental model for investigating human metabolism and disposition of drugs. The present review was designed to summarize key findings about the use of this model for studying human hepatic drug transporters, which are now recognized as important players in pharmacokinetics and consequently have to be considered from a regulatory perspective  during pharmaceutical drug development. The reviewed data indicate that chimeric mice with humanized livers have been successfully used for analysing the implications of human hepatic drug transporters f...
Source: European Journal of Drug Metabolism and Pharmacokinetics - July 6, 2022 Category: Drugs & Pharmacology Source Type: research