ArticleInvestigational new drugs2010
Tyrosine kinase inhibitors potentiate the cytotoxicity of MDR-substrate anticancer agents independent of growth factor receptor status in lung cancer cell lines.
Article in Investigational new drugs, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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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.
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Who cites it
20 citing papers in PubMed, 42 citations in OpenAlex.
- Pharmacological strategies to enhance the response of hepatoblastoma to chemotherapy through MDR1 inhibition.Acta pharmacologica Sinica · 2026Article
- DeepDrugs: a mechanism-aware tri-linear attention framework for synergistic drug-combination prediction.Briefings in bioinformatics · 2026Article
- Low-Dose Crizotinib, a Tyrosine Kinase Inhibitor, Highly and Specifically Sensitizes P-Glycoprotein-Overexpressing Chemoresistant Cancer Cells Through Induction of Late ApoptosisFrontiers in oncology · 2020Article
- Advances in nanotechnology-based delivery systems for EGFR tyrosine kinases inhibitors in cancer therapy.Asian journal of pharmaceutical sciences · 2020Review
- Review
- Dasatinib Treatment Increases Sensitivity to c-Met Inhibition in Triple-Negative Breast Cancer Cells.Cancers · 2019Article
- 'Et tu, inhibitor?': the potential for HIV inhibitors to prime P-gp-mediated chemoresistance in cancer.Future science OA · 2018Article
- Entinostat reverses P-glycoprotein activation in snail-overexpressing adenocarcinoma HCC827 cells.PloS one · 2018Article
- Novel Effects of Lapatinib Revealed in the African Trypanosome by Using Hypothesis-Generating Proteomics and Chemical Biology Strategies.Antimicrobial agents and chemotherapy · 2017Article
- A platinum-based hybrid drug design approach to circumvent acquired resistance to molecular targeted tyrosine kinase inhibitors.Scientific reports · 2016Article
- Biodegradable nanoparticles sequentially decorated with Polyethyleneimine and Hyaluronan for the targeted delivery of docetaxel to airway cancer cells.Journal of nanobiotechnology · 2015Article
- Afatinib circumvents multidrug resistance via dually inhibiting ATP binding cassette subfamily G member 2 in vitro and in vivo.Oncotarget · 2014Article
- The novel toluidine sulphonamide EL102 shows pre-clinical in vitro and in vivo activity against prostate cancer and circumvents MDR1 resistance.British journal of cancer · 2013Article
- Coadministration of lapatinib increases exposure to docetaxel but not doxorubicin in the small intestine of mice.Anti-cancer drugs · 2013Article
- The interaction of bortezomib with multidrug transporters: implications for therapeutic applications in advanced multiple myeloma and other neoplasias.Cancer chemotherapy and pharmacology · 2013Article
- Modulation of P-gp expression by lapatinib.Investigational new drugs · 2011Article
- Paclitaxel- and lapatinib-loaded lipopolymer micelles overcome multidrug resistance in prostate cancer.Drug delivery and translational research · 2011Article
- Anti-tumor activity of CrTX in human lung adenocarcinoma cell line A549.Acta pharmacologica Sinica · 2011Article
- Characterisation and manipulation of docetaxel resistant prostate cancer cell lines.Molecular cancer · 2011Article
- Clinical pharmacokinetics of tyrosine kinase inhibitors: focus on 4-anilinoquinazolines.Clinical pharmacokinetics · 2011Review
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
To investigate the interactions of Epidermal Growth Factor Receptor (EGFR)-inhibiting tyrosine kinase inhibitors (TKIs) on P-gp-mediated drug resistance, we tested three TKIs, lapatinib, gefitinib and erlotinib in direct ATPase assays and in Non-Small Cell Lung Cancer (NCSLC) cell lines with defined low levels of growth factor receptor expression. The three TKIs potentiated the action of known P-gp substrate cytotoxic drugs at therapeutically-relevant concentrations. However, more detailed analysis revealed that the interaction of lapatinib with P-gp was distinct from that of gefitinib and erlotinib, and was characterised by direct inhibition of the stimulated P-gp ATPase activity. Lapatinib proved the most potent P-gp modulator of the TKIs examined. Drug transport studies in the P-gp-over-expressing A549-Taxol cell line showed that lapatinib and erlotinib are capable of increasing docetaxel accumulation at clinically achievable concentrations. Combination studies with P-gp substrate chemotherapeutic agents, demonstrated that all three TKIs have significant potential to augment cytotoxic activity against P-gp-positive malignancies, however, interestingly, these agents also potentiated the toxicity of epirubicin in non-P-gp resistant parental cells. Our observations suggest that the combination of lapatinib with a taxane or anthracycline warrants clinical investigation in NSCLC to examine if beneficial or detrimental interactions may result.
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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.