Evidence map›Paper›PMID 42101808›Full record

ArticlePharmacological reports : PR2026

The novel third-generation antipsychotic drug brexpiprazole affects hepatic transcription factors, serum hormone levels, and cytochrome P450 enzymes after prolonged treatment: pharmacological significance.

Przemysław J Danek, Renata Pukło, Władysława A Daniel

Abstract read
In one paragraph

Article in Pharmacological reports : PR, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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1 · What the graph read from it

What it found

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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

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3 · Its place in the literature

Who cites it

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No citing paper in PubMed yet.

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

3 authors.

Przemysław J DanekDepartment of Pharmacokinetics and Drug Metabolism, Maj Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland.ORCID http://orcid.org/0000-0002-7137-2990
Renata PukłoDepartment of Pharmacokinetics and Drug Metabolism, Maj Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland.ORCID http://orcid.org/0000-0003-4820-9084
Władysława A DanielDepartment of Pharmacokinetics and Drug Metabolism, Maj Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland. nfdaniel@cyf-kr.edu.pl.ORCID http://orcid.org/0000-0002-1226-1721

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundBrexpiprazole is a third-generation antipsychotic used for the treatment of schizophrenia or as an adjunctive drug for the treatment of affective and neurological disorders. The combined treatments with brexpiprazole and other drugs that are also cytochrome P450 (CYP) substrates may lead to pharmacokinetic drug-drug interactions. Our present work aimed to investigate the effects of prolonged administration of brexpiprazole on the expression of hepatic transcription factors and CYP drug-metabolizing enzymes.

methodsMale Wistar rats received brexpiprazole (1 mg/kg ip.) for two weeks. Their livers were excised 24 h after the last dose, and the activities (HPLC), protein levels (Western blotting), and mRNAs (qRT-PCR) of CYP enzymes were measured. In parallel, the expression of hepatic transcription factors (Western blotting, qRT-PCR) and the concentration of serum hormones (ELISA) were assessed.

resultsBrexpiprazole produced a broad-spectrum effect on CYP expression and activity. It enhanced the expression and activity of CYP1A, CYP2A, CYP3A1/2, and the activity of CYP2B, but decreased the expression/activity of CYP2Ds and CYP2E1. The observed changes in CYP enzymes corresponded to alterations in transcription factors: the increased expression of PXR and AhR, and decreased expression of PPARγ, LXR, and FXR. The above modifications in CYP enzymes' expression were accompanied by enhanced corticosterone and reduced T

conclusionsBrexpiprazole affects the expression of hepatic transcription factors and CYP, which may impact its own biotransformation and the metabolism of endogenous substances and concomitantly administered drugs, and lead to drug-drug interactions of pharmacological/clinical importance.

Indexed as

Antipsychotic AgentsCytochrome P-450 Enzyme SystemHormonesLiverQuinolonesThiophenesTranscription FactorsAnimalsDrug InteractionsMaleRatsRats, WistarAntipsychotic AgentsbrexpiprazoleCytochrome P-450 Enzyme SystemHormonesQuinolonesThiophenesTranscription FactorsBrexpiprazoleCytochrome P450 (CYP)Enzyme expression/activityLiverSerum hormonesTranscription factors

Identifiers

PMID42101808
PMCPMC13275521

What Socratic holds

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LicenceCC BY-NC-ND
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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 Socratic graph.