Mass Balance and Metabolic Pathways of Eliapixant, a P2X3 Receptor Antagonist, in Healthy Male Volunteers
ConclusionComplete recovery of administered eliapixant-related radioactivity was observed in healthy male subjects with predominant excretion via feces. Eliapixant was almost exclusively cleared by oxidative biotransformation (>  90% of dose), with major involvement of cytochrome P450 3A4. Excretion of parent drug was of minor importance (~ 1% of dose).Clinical trial registrationClinicalTrials.gov: NCT04487431 (registered 27 July 2020)/EudraCT number: 2020-000519-54 (registered 3 February 2020), NCT02817100 (registered 26 June 2016), NCT03310645 (registered 16 October 2017). (Source: European Journal of Drug Metabolis...
Source: European Journal of Drug Metabolism and Pharmacokinetics - December 3, 2023 Category: Drugs & Pharmacology Source Type: research

Pharmacokinetic Parameters of Recombinant Human Cyclophilin A in Mice
ConclusionThis study identified promising target organs for rhCypA ’s potential therapeutic effects. The mode of rhCypA accumulation and retention in organs could be primarily due to the expression of its receptors in them. For the first time, rhCypA was shown to cross the blood–brain barrier and accumulate in the brain. These rhCypA pharmacokinetic data could be extrapolated to humans as preliminary data for possible clinical trials. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - December 1, 2023 Category: Drugs & Pharmacology Source Type: research

Pharmacokinetics of Imatinib Mesylate and Development of Limited Sampling Strategies for Estimating the Area under the Concentration –Time Curve of Imatinib Mesylate in Palestinian Patients with Chronic Myeloid Leukemia
ConclusionThe LSS using one timepoint, especiallyC0, can effectively predict imatinib AUC. This approach offers practical benefits in optimizing dose regimens and improving adherence. However, for more precise estimation of imatinib AUC, utilizing two- or three-timepoint concentrations is recommended over relying on a single point. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - November 25, 2023 Category: Drugs & Pharmacology Source Type: research

Pharmacokinetics of 4-Hydroxybenzaldehyde in Normal and Cerebral Ischemia –Reperfusion Injury Rats Based on Microdialysis Technique
ConclusionsThe rapid absorption and low absolute bioavailability of 4-HBd by gavage in rats are  followed by rapid and wide distribution to various tissues and organs, including the brain. The prototype drug is excreted in the feces and urine in low amounts, and it is metabolized to 4-HBA in large amounts in vivo; the pathological state of the MCAO/R model mainly affects its absorption degree and metabolism rate. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - November 24, 2023 Category: Drugs & Pharmacology Source Type: research

Ticagrelor Steady-State Trough Concentration in Chinese Patients Undergoing Percutaneous Coronary Intervention
ConclusionsThis study provides robust and reliable insights into the optimal therapeutic steady-state trough concentrations of ticagrelor in Chinese patients with post-percutaneous coronary intervention. These findings have significant implications for guiding the rational use of antiplatelet drugs and facilitating precise drug administration in Chinese patients undergoing percutaneous coronary intervention. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - November 24, 2023 Category: Drugs & Pharmacology Source Type: research

Distribution, Metabolism, and Excretion of Cenobamate in Adult, Fetal, Neonatal, and Lactating Rats
ConclusionsDistribution of cenobamate was widespread into many rat tissues, including brain, amniotic fluid, fetal plasma, breast milk, and breastfeeding rat pups. These distribution findings, along with the results of the metabolism and excretion studies, may help inform treatment decisions for patients with epilepsy being treated with cenobamate, including pregnant or nursing mothers. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - November 3, 2023 Category: Drugs & Pharmacology Source Type: research

Acknowledgement to Referees
(Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - October 30, 2023 Category: Drugs & Pharmacology Source Type: research