Examination of Urinary Excretion of Unchanged Drug in Humans and Preclinical Animal Models: Increasing the Predictability of Poor Metabolism in Humans

Autor: Leslie Z. Benet, Chelsea Hosey-Cojocari, Connie M. Remsberg, Nadia O. Bamfo
Rok vydání: 2021
Předmět:
Zdroj: Pharm Res
ISSN: 1573-904X
0724-8741
DOI: 10.1007/s11095-021-03076-y
Popis: PURPOSE: A dataset of fraction excreted unchanged in the urine (fe) values was developed and used to evaluate the ability of preclinical animal species to predict high urinary excretion, and corresponding poor metabolism, in humans. METHODS: A literature review of fe values in rats, dogs, and monkeys was conducted for all Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3 and 4 drugs (n=352) and a set of Class 1 and 2 drugs (n=80). The final dataset consisted of 202 total fe values for 135 unique drugs. Human and animal data were compared through correlations, two-fold analysis, and binary classifications of high (fe ≥30%) versus low (
Databáze: OpenAIRE