ArticleBasic & clinical pharmacology & toxicology2008
Antipsychotic drugs inhibit the function of breast cancer resistance protein.
Article in Basic & clinical pharmacology & toxicology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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.
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.
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Who cites it
23 citing papers in PubMed, 62 citations in OpenAlex.
- ABCG2 transporter: Structural and functional associations with gout (Review).International journal of molecular medicine · 2026Review
- From Therapeutic Drug to Xenobiotic in Cancer Repurposing: Clozapine Mechanisms, Metabolic Liabilities, and Human-Relevant Translational Approaches.Journal of xenobiotics · 2026Review
- Extrapyramidal and anticholinergic reactions in an adolescent patient: a case for pharmacogenetic consideration.Biochemia medica · 2026Article
- Impact of the transcription factor nuclear factor 1 B T>C polymorphism on clozapine metabolism in vivo and expression of intestinal transporters in vitro.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Editorial: Drug repurposing for cancer treatment: current and future directions.Frontiers in oncology · 2025Article
- Exposure to Low-Frequency Radiation Changes the Expression of Nestin, VEGF, BCRP and Apoptosis Markers During Glioma Treatment Strategy: AnCurrent radiopharmaceuticals · 2024Article
- Study on the daily dose and serum concentration of clozapine in psychiatric patients and possible influencing factors of serum concentration.BMC psychiatry · 2023Article
- Review
- Article
- The Antipsychotic Drug Haldol Modulates IQGAP1-Signaling and Inhibits Cell Proliferation in Triple Negative Breast Cancer Cell Lines.microPublication biology · 2023Article
- Perphenazine and prochlorperazine decrease glioblastoma U-87 MG cell migration and invasion: Analysis of the ABCB1 and ABCG2 transporters, E-cadherin, α-tubulin and integrins (α3, α5, and β1) levels.Oncology letters · 2022Article
- Repurposing Antipsychotics for Cancer Treatment.Biomedicines · 2021Review
- Uremic serum residue decreases SN-38 sensitivity through suppression of organic anion transporter polypeptide 2B1 in LS-180 colon cancer cells.Scientific reports · 2019Article
- Potential Influence of Centrally Acting Herbal Drugs on Transporters at the Blood-Cerebrospinal Fluid Barrier and Blood-Brain Barrier.European journal of drug metabolism and pharmacokinetics · 2018Review
- Paliperidone, a relatively novel atypical antipsychotic drug, is a substrate for breast cancer resistance protein.Experimental and therapeutic medicine · 2018Article
- PharmGKB summary: clozapine pathway, pharmacokinetics.Pharmacogenetics and genomics · 2018Article
- The predictive value of ABCB1, ABCG2, CYP3A4/5 and CYP2D6 polymorphisms for risperidone and aripiprazole plasma concentrations and the occurrence of adverse drug reactions.The pharmacogenomics journal · 2018Article
- Dual Modulation of Human P-Glycoprotein and ABCG2 with Prodrug Dimers of the Atypical Antipsychotic Agent Paliperidone in a Model of the Blood-Brain Barrier.Molecular pharmaceutics · 2017Article
- Compound signature detection on LINCS L1000 big data.Molecular bioSystems · 2015Article
- Psychotropic drug-drug interactions involving P-glycoprotein.CNS drugs · 2012Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
The ABCG2 transporter breast cancer resistance protein (BCRP) has been identified in several physiological sites. It has been suggested to play an important role in disposition of many drugs and environmental toxins. We investigated the effects of several antipsychotic drugs, including risperidone, 9-hydroxy-risperidone (paliperidone), olanzapine, quetiapine, clozapine, haloperidol and chlorpromazine, and a positive control inhibitor Ko143 on functions of BCRP in MCF7 and BCRP over-expressing MCF7/MX100 cell lines using a BCRP prototypical substrate mitoxantrone. Our findings indicated that the tested antipsychotics rank order of potency of inhibition of BCRP according to concentrations required to reach 50% of maximum inhibition (IC(50)) was as follows: Ko143 (0.07 microM) > risperidone (38.1 microM) > clozapine (42.0 microM) > paliperidone (51 microM) > chlorpromazine (52.2 microM) > quetiapine (66.1 microM) > olanzapine = haloperidol (>100.0 microM). We further tested the effects of various concentrations of risperidone on the BCRP-mediated transport of oestrone-3-sulfate in a colon carcinoma cell line, Caco-2, a widely used model to study drug absorption. Our findings show that risperidone at concentrations ranging from 1 to 100 microM significantly inhibited intracellular accumulation of oestrone-3-sulfate in Caco-2 cell monolayers. The present results suggest that a potential source of pharmacokinetic interactions exists between BCRP substrates and several antipsychotics.
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Registered trials
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.