ArticleActa pharmaceutica Sinica. B2018
Olmutinib (HM61713) reversed multidrug resistance by inhibiting the activity of ATP-binding cassette subfamily G member 2
Article in Acta pharmaceutica Sinica. B, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 26 citations in OpenAlex.
- A Review on EGFR-Tyrosine Kinase Inhibitors and their Resistance Mechanisms.Current pharmaceutical design · 2026Review
- The strategies to cure cancer patients by eradicating cancer stem-like cells.Molecular cancer · 2023Review
- Adagrasib, a KRAS G12C inhibitor, reverses the multidrug resistance mediated by ABCB1 in vitro and in vivo.Cell communication and signaling : CCS · 2022Article
- Cholesterol promotes EGFR-TKIs resistance in NSCLC by inducing EGFR/Src/Erk/SP1 signaling-mediated ERRα re-expression.Molecular cancer · 2022Article
- PD0325901, an ERK inhibitor, enhances the efficacy of PD-1 inhibitor in non-small cell lung carcinoma.Acta pharmaceutica Sinica. B · 2021Article
- The third-generation EGFR inhibitor almonertinib (HS-10296) resensitizes ABCB1-overexpressing multidrug-resistant cancer cells to chemotherapeutic drugs.Biochemical pharmacology · 2021Article
- Mitomycin C enhanced the efficacy of PD-L1 blockade in non-small cell lung cancer.Signal transduction and targeted therapy · 2020Article
- Olmutinib Reverses Doxorubicin Resistance in ETS1-Overexpressing Leukemia Cells.Medical science monitor : international medical journal of experimental and clinical research · 2020Article
- Rociletinib (CO-1686) enhanced the efficacy of chemotherapeutic agents in ABCG2-overexpressing cancer cellsActa pharmaceutica Sinica. B · 2020Article
- Review
- M3814, a DNA-PK Inhibitor, Modulates ABCG2-Mediated Multidrug Resistance in Lung Cancer Cells.Frontiers in oncology · 2020Article
- Discovery of WS-157 as a highly potent, selective and orally active EGFR inhibitor.Acta pharmaceutica Sinica. B · 2019Article
- Synergistic antitumor activity of artesunate and HDAC inhibitors through elevating heme synthesisActa pharmaceutica Sinica. B · 2019Article
- Development of precision medicine approaches based on inter-individual variability of BCRP/Acta pharmaceutica Sinica. B · 2019Review
- ERK is a Pivotal Player of Chemo-Immune-Resistance in Cancer.International journal of molecular sciences · 2019Review
- A Danshensu-Tetramethylpyrazine Conjugate DT-010 Overcomes Multidrug Resistance in Human Breast Cancer.Frontiers in pharmacology · 2019Article
- Review
- Editorial Preface for Targeted Cancer Therapy.Acta pharmaceutica Sinica. B · 2018Article
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Overexpressing of ATP-binding cassette (ABC) transporters is the essential cause of multidrug resistance (MDR), which is a significant hurdle to the success of chemotherapy in many cancers. Therefore, inhibiting the activity of ABC transporters may be a logical approach to circumvent MDR. Olmutinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), which has been approved in South Korea for advanced EGFR T790M-positive non-small cell lung cancer (NSCLC). Here, we found that olmutinib significantly increased the sensitivity of chemotherapy drug in ABCG2-overexpressing cells. Furthermore, olmutinib could also increase the retention of doxorubicin (DOX) and rhodamine 123 (Rho 123) in ABC transporter subfamily G member 2 (ABCG2)-overexpressing cells. In addition, olmutinib was found to stimulate ATPase activity and inhibit photolabeling of ABCG2 with [
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