The excretion and metabolism of (14)C-sucralose has been investigated in non-pregnant and pregnant rabbits after administration of single 10mg/kg oral doses. Means of 22% and 55% of the dose were excreted in urine and faeces, respectively, by non-pregnant animals during 5 days. Excretion was similar in pregnant animals with means of 22% and 65% of the dose in urine and faeces, respectively, during the same time. Following a single oral dose, a mean of approximately 7% of the dose was still being excreted during the 96-120-hr collection period. Only one major radioactive component was detected in urine samples which corresponded to unchanged sucralose.
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http://dx.doi.org/10.1016/s0278-6915(00)00033-8 | DOI Listing |
J Pharmacokinet Pharmacodyn
January 2025
Department of Clinical Pharmacy and Pharmacy Administration, West China school of Pharmacy, Sichuan University, Chengdu, 610064, China.
Alogliptin is a highly selective inhibitor of dipeptidyl peptidase-4 and primarily excreted as unchanged drug in the urine, and differences in clinical outcomes in renal impairment patients increase the risk of serious adverse reactions. In this study, we developed a comprehensive physiologically-based quantitative systematic pharmacology model of the alogliptin-glucose control system to predict plasma exposure and use glucose as a clinical endpoint to prospectively understand its therapeutic outcomes with varying renal function. Our model incorporates a PBPK model for alogliptin, DPP-4 activity described by receptor occupancy theory, and the crosstalk and feedback loops for GLP-1-GIP-glucagon, insulin, and glucose.
View Article and Find Full Text PDFJ Nucl Med
January 2025
Department of Nuclear Medicine, Medical University of Innsbruck, Innsbruck, Austria
Several exploratory studies have demonstrated the feasibility of cholecystokinin-2 receptor (CCK2R) targeting in patients with medullary thyroid carcinoma (MTC) and other neuroendocrine tumors (NETs). We report the results of a prospective phase I/IIA pilot study (clinicaltrials.gov NCT06155994) conducted at our center with the Ga-labeled peptide analog DOTA-DGlu-Ala-Tyr-Gly-Trp-(N-Me)Nle-Asp-1-Nal-Phe-NH (Ga-DOTA-MGS5).
View Article and Find Full Text PDFClin Pharmacokinet
January 2025
Leiden Academic Centre for Drug Research (LACDR), Leiden University, Leiden, The Netherlands.
Background And Objective: Psilocybin is currently being extensively studied as a potential therapeutic agent for multiple psychiatric disorders. Here, a systematic literature review of all published pharmacokinetic data on the pharmacologically active metabolite of psilocybin, psilocin, is presented.
Methods: The review includes clinical studies that reported pharmacokinetic data and/or parameters after psilocybin administration in humans.
Kidney Int Rep
January 2025
Department of Cardiovascular Sciences, University of Leicester, Leicester, Leicestershire, UK.
Introduction: Endothelin A (ETA) receptor activation is a driver of proteinuria, kidney inflammation, and fibrosis in IgA nephropathy (IgAN). Atrasentan, a selective ETA receptor antagonist, has potential to reduce proteinuria and preserve kidney function in IgAN. ALIGN (NCT04573478) is a phase 3, randomized, double-blind, placebo-controlled clinical trial of atrasentan in patients with IgAN at high risk of kidney function loss.
View Article and Find Full Text PDFJ Hazard Mater
January 2025
Department of Surgery, Clinical Advancement Department, Hamad Medical Corporation, Qatar; College of Health and Medical Sciences, Qatar University, Qatar. Electronic address:
Point of departure (POD) is a concept used in risk assessment to calculate the reference dose of exposure that is likely to have no appreciable risk on health. POD can be directly utilized from no observed adverse effect levels (NOAEL) which is the dose or exposure level at which there is little or no risk of adverse effects. However, NOAEL values are unavailable for most of the chemicals due to inconsistent animal toxicity data.
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