Evidence map›Paper›PMID 31040114›Full record

ArticleDrug metabolism and disposition: the biological fate of chemicals2019

Contributions of Hepatic and Intestinal Metabolism to the Disposition of Niclosamide, a Repurposed Drug with Poor Bioavailability.

Xiaoyu Fan, Hongmin Li, Xinxin Ding, Qing-Yu Zhang

Open access · bronzeAbstract read
In one paragraph

Article in Drug metabolism and disposition: the biological fate of chemicals, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed, 1 pooled it
3.1field-weighted citation impact, top 9% of its field
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

19 citing papers in PubMed, 1 synthesis or guideline pooled it, 33 citations in OpenAlex.

  1. Pooled it
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  14. Assessing cytochrome P450 function using genetically engineered mouse models.Advances in pharmacology (San Diego, Calif.) · 2022
    Review
  15. Niclosamide encapsulated in mesoporous silica and geopolymer: A potential oral formulation for COVID-19.Microporous and mesoporous materials : the official journal of the International Zeolite Association · 2021
    Article
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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

4 authors at 3 institutions in 1 country.

Xiaoyu FanDepartment of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, Arizona (X.F., X.D., Q.-Y.Z.); and Wadsworth Center, New York State Department of Health, and School of Public Health, University at Albany, Albany, New York (H.L.).
Hongmin LiDepartment of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, Arizona (X.F., X.D., Q.-Y.Z.); and Wadsworth Center, New York State Department of Health, and School of Public Health, University at Albany, Albany, New York (H.L.).
Xinxin DingDepartment of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, Arizona (X.F., X.D., Q.-Y.Z.); and Wadsworth Center, New York State Department of Health, and School of Public Health, University at Albany, Albany, New York (H.L.).
Qing-Yu ZhangDepartment of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, Arizona (X.F., X.D., Q.-Y.Z.); and Wadsworth Center, New York State Department of Health, and School of Public Health, University at Albany, Albany, New York (H.L.) qyzhang@pharmacy.arizona.edu.
University at Albany, State University of New York · USNew York State Department of Health · USWadsworth Center · US

Funding

SOUTHWEST ENVIRONMENTAL HEALTH SCIENCES CENTERP30ES006694 · NIEHS · UNIVERSITY OF ARIZONA · PI DEAN BILLHEIMER · 1994 to 2026
$36.7M
Intestinal P450 and Xenobiotic MetabolismR01GM082978 · NIGMS · WADSWORTH CENTER · PI ZHANG, QING-YU · 2008 to 2018
$3.3M
High throughput screening of orthosteric inhibitors of flavivirus proteaseR01AI131669 · NIAID · WADSWORTH CENTER · PI LI, HONGMIN · 2018 to 2022
$2.6M
High throughput screening of orthosteric inhibitors of flavivirus proteaseR56AI131669 · NIAID · WADSWORTH CENTER · PI LI, HONGMIN · 2017 to 2017
$524k
New Use of Old Drugs for Zika VirusR21AI134568 · NIAID · WADSWORTH CENTER · PI LI, HONGMIN · 2017 to 2018
$447k
NIAID NIH HHS R01 AI131669NIAID NIH HHS R21 AI134568NIAID NIH HHS R56 AI131669NIEHS NIH HHS P30 ES006694NIGMS NIH HHS R01 GM082978
6 · The paper itself

Abstract

Niclosamide, an antiparasitic, has been repositioned as a potential therapeutic drug for systemic diseases based on its antiviral, anticancer, and anti-infection properties. However, low bioavailability limits its in vivo efficacy. Our aim was to determine whether metabolic disposition by microsomal P450 enzymes in liver and intestine influences niclosamide's bioavailability in vivo, by comparing niclosamide metabolism in wild-type, liver-Cpr-null (LCN), and intestinal epithelium-Cpr-null (IECN) mice. In vitro stability of niclosamide in microsomal incubations was greater in the intestine than in liver in the presence of NADPH, but it was much greater in liver than in intestine in the presence of UDPGA. NADPH-dependent niclosamide metabolism and hydroxy-niclosamide formation were inhibited in hepatic microsomes of LCN mice, but not IECN mice, compared with wild-type mice. In intestinal microsomal reactions, hydroxy-niclosamide formation was not detected, but rates of niclosamide-glucuronide formation were ∼10-fold greater than in liver, in wild-type, LCN, and IECN mice. Apparent Km and

Indexed as

Drug RepositioningAnimalsAntiparasitic AgentsBiological AvailabilityHumansIntestinal MucosaMiceMicrosomes, LiverNiclosamideAntiparasitic AgentsNiclosamide

Identifiers

PMID31040114
PMCPMC6592404
OpenAlexW2943418093

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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.