Evidence map›Paper›PMID 37531179›Full record

ArticleChemical research in toxicology2023

Identifying the Reactive Metabolites of Tyrosine Kinase Inhibitor Pexidartinib In Vitro Using LC-MS-Based Metabolomic Approaches.

Xuan Qin, Yong Wang, Kevin R MacKenzie, John M Hakenjos, Si Chen, Saleh M Khalil, Sung Yun Jung, Damian W Young, Lei Guo, Feng Li

Open access · hybridAbstract read
In one paragraph

Article in Chemical research in toxicology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
1.4field-weighted citation impact, top 19% 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

4 citing papers in PubMed, 9 citations in OpenAlex.

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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

10 authors at 2 institutions in 1 country.

Xuan QinCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, United States.ORCID 0000-0003-3728-5911
Yong WangCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, United States.
Kevin R MacKenzieCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, United States.
John M HakenjosCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, United States.
Si ChenDivision of Biochemical Toxicology, National Center for Toxicological Research/U.S. Food and Drug Administration (FDA), Jefferson, Arkansas 72079, United States.
Saleh M KhalilCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, United States.
Sung Yun JungDepartment of Molecular & Cellular Biology, Baylor College of Medicine, Houston, Texas 77030, United States.ORCID 0000-0003-1521-7977
Damian W YoungCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, United States.
Lei GuoDivision of Biochemical Toxicology, National Center for Toxicological Research/U.S. Food and Drug Administration (FDA), Jefferson, Arkansas 72079, United States.
Feng LiCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, United States.ORCID 0000-0002-9680-4614
Baylor College of Medicine · USNational Center for Toxicological Research · US

Funding

Targeting sperm-specific proteins during meiosis and sperm morphogenesisP01HD087157 · NICHD · BAYLOR COLLEGE OF MEDICINE · PI MATZUK, MARTIN M. · 2017 to 2021
$6.2M
Kinases as Therapeutic Targets for EndometriosisR01HD110038 · NICHD · BAYLOR COLLEGE OF MEDICINE · PI MARTIN M. MATZUK · 2022 to 2026
$3.4M
Mechanisms of Liver Toxicity of Anit-Depressant DuloxetineR01DK121970 · NIDDK · BAYLOR COLLEGE OF MEDICINE · PI LI, FENG · 2020 to 2023
$1.8M
Elucidating Chemical Features that Block or Facilitate Passage across the Blood-Testis and/or Blood-Epidydimal Barriers in MiceR33HD099995 · NICHD · BAYLOR COLLEGE OF MEDICINE · PI LI, FENG · 2022 to 2024
$1.7M
Elucidating Chemical Features that Block or Facilitate Passage across the Blood-Testis and/or Blood-Epidydimal Barriers in MiceR61HD099995 · NICHD · BAYLOR COLLEGE OF MEDICINE · PI LI, FENG · 2020 to 2021
$862k
NICHD NIH HHS P01 HD087157NICHD NIH HHS R01 HD110038NICHD NIH HHS R33 HD099995NICHD NIH HHS R61 HD099995NIDDK NIH HHS R01 DK121970
6 · The paper itself

Abstract

Pexidartinib (PEX, TURALIO), a selective and potent inhibitor of the macrophage colony-stimulating factor-1 receptor, has been approved for the treatment of tenosynovial giant cell tumor. However, frequent and severe adverse effects have been reported in the clinic, resulting in a boxed warning on PEX for its risk of liver injury. The mechanisms underlying PEX-related hepatotoxicity, particularly metabolism-related toxicity, remain unknown. In the current study, the metabolic activation of PEX was investigated in human/mouse liver microsomes (HLM/MLM) and primary human hepatocytes (PHH) using glutathione (GSH) and methoxyamine (NH

Indexed as

Chemical and Drug Induced Liver InjuryCytochrome P-450 CYP3AAminopyridinesAnimalsChromatography, LiquidCytochrome P-450 CYP3A InhibitorsGlutathioneHumansMetabolomicsMiceMicrosomes, LiverProtein Kinase InhibitorsPyrrolesTandem Mass SpectrometryTyrosine Kinase InhibitorsAminopyridinesCytochrome P-450 CYP3ACytochrome P-450 CYP3A InhibitorsGlutathionepexidartinibProtein Kinase InhibitorsPyrrolesTyrosine Kinase Inhibitors

Identifiers

PMID37531179
PMCPMC10445284
OpenAlexW4385475975

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.