Clinical Pharmacokinetics and Disposition of Imrecoxib

Repaglinide metabolism by human hepatocytes reveals CYP2C8 dominance and misassignment of CYP3A4 by liver subcellular fractions and recombinant enzymes.

Repaglinide is an antidiabetic agent and Food and Drug Administration-endorsed clinical CYP2C8 probe with a well characterized human disposition profile in which a dicarboxylic acid, M2, is the main metabolite accounting for 66% of the administered dose. The remainder is distributed among M1 (4%), unchanged repaglinide...

Population Pharmacokinetics of Savolitinib and Its Active Metabolite M2 in Patients with Advanced Solid Tumour.

Pharmacokinetic and safety interactions between aildenafil and clarithromycin, cimetidine, or rifampin in healthy subjects.

AIMS Aildenafil citrate, an orally bioavailable phosphodiesterase type 5 (PDE5) inhibitor, is primarily metabolized by cytochrome P450 3A4 (CYP3A4). This study aimed to assess potential pharmacokinetic interactions between aildenafil citrate tablets and cytochrome P450 (CYP)3A modulators. METHODS This study involved...

Toxicokinetics, Biotransformation, and Tissue Distribution of Imidaclothiz in Rats

Imidaclothiz (IMZ), a next-generation neonicotinoid pesticide, has garnered significant attention due to its detection in human samples. In this study, we investigated its toxicokinetics and biotransformation in rats following oral administration. IMZ was rapidly absorbed, reaching peak plasma concentration at 0.75 h...

Evaluation of the Effect of Cendakimab on the Pharmacokinetics of CYP Probe Drugs in Patients With Eosinophilic Esophagitis

Cendakimab is a humanized monoclonal antibody that inhibits interleukin‐13 binding to its receptors. Although not expected to share clearance pathways with small molecules, its use in eosinophilic esophagitis, a type 2 inflammatory disease, may indirectly affect cytochrome P450 activity by modulating cytokine signaling...

Evaluating the Impact of CYP1A2 Inhibition on the Pharmacokinetics of Savolitinib: A Phase 1 Open‐Label Study

ABSTRACT Savolitinib is an oral, potent, selective CNS‐penetrant MET‐tyrosine kinase inhibitor that in vitro studies indicate is metabolized by cytochrome P450 (CYP) enzymes, including CYP1A2, and by non‐CYP enzymes, such as aldehyde oxidase (AO). Savolitinib primary metabolites, M2 and M3, are formed mainly by CYP1A2...