Evidence map›Paper›PMID 39590805›Full record

ArticleMetabolites2024

Species Differences in Ezetimibe Glucuronidation.

Shalom Emmanuel, Eric A Asare, Ting Du, Huan Xie, Dong Liang, Song Gao

Abstract read
In one paragraph

Article in Metabolites, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

1 citing paper in PubMed.

  1. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors.

Shalom EmmanuelDepartment of Pharmaceutical Science, College of Pharmacy and Health Sciences, Texas Southern University, 3100 Cleburne Street, Houston, TX 77004, USA.
Eric A AsareDepartment of Pharmaceutical Science, College of Pharmacy and Health Sciences, Texas Southern University, 3100 Cleburne Street, Houston, TX 77004, USA.ORCID 0009-0008-5621-7109
Ting DuDepartment of Pharmaceutical Science, College of Pharmacy and Health Sciences, Texas Southern University, 3100 Cleburne Street, Houston, TX 77004, USA.ORCID 0000-0002-7705-6913
Huan XieDepartment of Pharmaceutical Science, College of Pharmacy and Health Sciences, Texas Southern University, 3100 Cleburne Street, Houston, TX 77004, USA.ORCID 0000-0002-0591-5619
Dong LiangDepartment of Pharmaceutical Science, College of Pharmacy and Health Sciences, Texas Southern University, 3100 Cleburne Street, Houston, TX 77004, USA.ORCID 0000-0001-6632-8066
Song GaoDepartment of Pharmaceutical Science, College of Pharmacy and Health Sciences, Texas Southern University, 3100 Cleburne Street, Houston, TX 77004, USA.ORCID 0000-0003-2361-3494

Funding

Targeted Nano-drug-delivery-systems of Frist-in-class Drugs for CRPC: PK/PD Evaluation and Combination TherapyU54MD007605 · NIMHD · TEXAS SOUTHERN UNIVERSITY · PI Veronica B. Ajewole · 2020 to 2026
$22.0M
Selectively Manipulating Intestinal Glucuronidation to Alleviate Mycophenolate mofetil-induced DiarrheaR16GM149425 · NIGMS · TEXAS SOUTHERN UNIVERSITY · PI Song Gao · 2023 to 2026
$614k
CPRIT RP180748NIGMS NIH HHS R16 GM149425NIH HHS GM149425NIMHD NIH HHS U54 MD007605NIMHD NIH HHS U54MD007605
6 · The paper itself

Abstract

backgroundPeclinical and clinical studies have revealed that ezetimibe, an approved cholesterol-absorption inhibitor, is rapidly and extensively metabolized to a more potent metabolite, ezetimibe glucuronide. Since different species are commonly used in the pharmacokinetic and pharmacodynamic studies of ezetimibe, it is essential to determine the species difference in glucuronidation of ezetimibe in order to accurately evaluate ezetimibe's pharmacokinetics and pharmacodynamics. The purpose of the study was to compare species differences in ezetimibe glucuronidation rates using intestinal microsomes from humans, rats, mice, monkeys, and dogs.

methodIntestinal microsomes from different species were used to assess the ezetimibe glucuronidation rates. Multiple substrate concentrations at 0.5, 2, 5, 10, 20, 30, 40, and 50 µM were tested and fitted into the Michaelis-Menten model to determine the enzyme kinetic parameters.

resultsThe results showed that the glucuronidation rates with these tested species were significantly different. Kinetic studies revealed that the maximum metabolic rate (V

conclusionsThe study revealed that the rate of ezetimibe glucuronidation in the intestine was different in different species and has an impact on ezetimibe glucuronidation in the intestine. When analyzing the pharmacodynamics, pharmacokinetics, or toxicology of ezetimibe using different models, these species differences must be taken into consideration.

Indexed as

ezetimibeglucuronidationspecies differencesUGT

Identifiers

PMID39590805
PMCPMC11597066

What OpenQuestion holds

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.