ArticleBiomedicines2020
Doxazosin, a Classic Alpha 1-Adrenoceptor Antagonist, Overcomes Osimertinib Resistance in Cancer Cells via the Upregulation of Autophagy as Drug Repurposing.
Article in Biomedicines, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 21 citations in OpenAlex.
- Multi-Target Antitumor Effects of Natural Products and Approved Drug Repurposing in Non-Small Cell Lung Cancer: Advances in Mechanisms, Combination Regimens, Delivery System Optimization, and Clinical Challenges.International journal of molecular sciences · 2026Review
- Review
- Pancreatic Cancer: Pathogenesis and Clinical Studies.MedComm · 2025Review
- Arylpiperazine Derivatives and Cancer: A New Challenge in Medicinal Chemistry.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Inhibition of NNMT enhances drug sensitivity in lung cancer cells through mediation of autophagy.Frontiers in pharmacology · 2024Article
- Anti-cell Proliferative Mechanism of Doxazosin on Human Oral Cancer Cells Through the Modulation of Antioxidant and Apoptotic Pathway.Applied biochemistry and biotechnology · 2023Article
- YAP1 synergize with YY1 transcriptional co-repress DUSP1 to induce osimertinib resistant by activating the EGFR/MAPK pathway and abrogating autophagy in non-small cell lung cancer.International journal of biological sciences · 2023Article
- Elucidating a Complicated Enantioselective Metabolic Profile: A Study From Rats to Humans Using Optically Pure Doxazosin.Frontiers in pharmacology · 2022Article
- A novel signature based on autophagy-related lncRNA for prognostic prediction and candidate drugs for lung adenocarcinoma.Translational cancer research · 2022Article
- Blood Vessels and Peripheral Nerves as Key Players in Cancer Progression and Therapy Resistance.Cancers · 2021Review
- An Alternative Pipeline for Glioblastoma Therapeutics: A Systematic Review of Drug Repurposing in Glioblastoma.Cancers · 2021Review
- Doxazosin Attenuates Liver Fibrosis by Inhibiting Autophagy in Hepatic Stellate Cells via Activation of the PI3K/Akt/mTOR Signaling Pathway.Drug design, development and therapy · 2021Article
- The Relationship Between Anti-Hypertensive Drugs and Cancer: Anxiety to be Resolved in Urgent.Frontiers in pharmacology · 2020Review
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Osimertinib, which is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor, is an important anticancer drug because of its high efficacy and excellent safety profile. However, resistance against osimertinib is inevitable; therefore, therapeutic strategies to overcome the resistance are needed. Doxazosin, a classic quinazoline-based alpha 1-adrenoceptor antagonist is used to treat hypertension and benign prostatic hyperplasia with a known safety profile. The anticancer effects of doxazosin have been examined in various types of malignancies from the viewpoint of drug repositioning or repurposing. However, it currently remains unclear whether doxazosin sensitizes cancer cells to osimertinib. Herein, we demonstrated that doxazosin induced autophagy and enhanced the anticancer effects of osimertinib on the cancer cells and cancer stem cells of non-small cell lung cancer, pancreatic cancer, and glioblastoma at a concentration at which the growth of non-tumor cells was not affected. The osimertinib-sensitizing effects of doxazosin were suppressed by 3-methyladenine, an inhibitor of autophagy, which suggested that the effects of doxazosin were mediated by autophagy. The present study provides evidence for the efficacy of doxazosin as a combination therapy with osimertinib to overcome resistance against osimertinib.
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