ArticleBiochemical pharmacology2010
Lapatinib and erlotinib are potent reversal agents for MRP7 (ABCC10)-mediated multidrug resistance.
Article in Biochemical pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers.
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48 citing papers in PubMed, 98 citations in OpenAlex.
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- Epithelial-mesenchymal transition (EMT) and its role in acquired epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) chemoresistance in non-small cell lung cancer (NSCLC).Cancer pathogenesis and therapy · 2025Review
- Drug Treatment Direction Based on the Molecular Mechanism of Breast Cancer Brain Metastasis.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Cellular and molecular aspects of drug resistance in cancers.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2024Review
- The Role of Small Molecules Containing Fluorine Atoms in Medicine and Imaging Applications.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Establishment and Characterization of Multi-Drug Resistant p53-Negative Osteosarcoma SaOS-2 Subline.Diagnostics (Basel, Switzerland) · 2023Article
- Deciphering treatment resistance in metastatic colorectal cancer: roles of drug transports, EGFR mutations, and HGF/c-MET signaling.Frontiers in pharmacology · 2023Review
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- Infigratinib (BGJ 398), a Pan-FGFR Inhibitor, Targets P-Glycoprotein and Increases Chemotherapeutic-Induced Mortality of Multidrug-Resistant Tumor Cells.Biomedicines · 2022Article
- How Physiologic Targets Can Be Distinguished from Drug-Binding Proteins.Molecular pharmacology · 2021Article
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- Nuclear factor erythroid 2-related factor 2 modulates HER4 receptor in ovarian cancer cells to influence their sensitivity to tyrosine kinase inhibitors.Exploration of targeted anti-tumor therapy · 2021Article
- Effect of sodium butyrate on ABC transporters in lung cancer A549 and colorectal cancer HCT116 cells.Oncology letters · 2020Article
- Repurposing Tyrosine Kinase Inhibitors to Overcome Multidrug Resistance in Cancer: A Focus on Transporters and Lysosomal Sequestration.International journal of molecular sciences · 2020Review
- 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
- ATP-binding cassette transporters in progression and clinical outcome of pancreatic cancer: What is the way forward?World journal of gastroenterology · 2018Review
- Tyrosine kinase inhibitors enhanced the efficacy of conventional chemotherapeutic agent in multidrug resistant cancer cells.Molecular cancer · 2018Review
- ABCC10 Plays a Significant Role in the Transport of Gefitinib and Contributes to Acquired Resistance to Gefitinib in NSCLC.Frontiers in pharmacology · 2018Article
- Quizartinib (AC220) reverses ABCG2-mediated multidrug resistance:Oncotarget · 2017Article
- In vitro evaluation of combination of EGCG and Erlotinib with classical chemotherapeutics on JAR cells.In vitro cellular & developmental biology. Animal · 2017Article
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
Abstract
In recent years, a number of TKIs (tyrosine kinase inhibitors) targeting epidermal growth factor receptor (EGFR) family have been synthesized and some have been approved for clinical treatment of cancer by the FDA. We recently reported a new pharmacological action of the 4-anilinoquinazoline derived EGFR TKIs, such as lapatinib (Tykerb) and erlotinib (Tarceva), which significantly affect the drug resistance patterns in cells expressing the multidrug resistance (MDR) phenotype. Previously, we showed that lapatinib and erlotinib could inhibit the drug efflux function of P-glycoprotein (P-gp, ABCB1) and ABCG2 transporters. In this study, we determined if these TKIs have the potential to reverse MDR due to the presence of the multidrug resistance protein 7 (MRP7, ABCC10). Our results showed that lapatinib and erlotinib dose-dependently enhanced the sensitivity of MRP7-transfected HEK293 cells to several established MRP7 substrates, specifically docetaxel, paclitaxel, vinblastine and vinorelbine, whereas there was no or a less effect on the control vector transfected HEK293 cells. [(3)H]-paclitaxel accumulation and efflux studies demonstrated that lapatinib and erlotinib increased the intracellular accumulation of [(3)H]-paclitaxel and inhibited the efflux of [(3)H]-paclitaxel from MRP7-transfected cells but not in the control cell line. Lapatinib is a more potent inhibitor of MRP7 than erlotinib. In addition, the Western blot analysis revealed that both lapatinib and erlotinib did not significantly affect MRP7 expression. We conclude that the EGFR TKIs, lapatinib and erlotinib reverse MRP7-mediated MDR through inhibition of the drug efflux function, suggesting that an EGFR TKI based combinational therapy may be applicable for chemotherapeutic practice clinically.
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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.