Repurposing itraconazole as an anticancer agent

Tsubamoto, Hiroshi; Ueda, Tomoko; Inoue, Kayo; Sakata, Kazuko; Shibahara, Hiroaki; Sonoda, Takashi

doi:10.3892/ol.2017.6325

Cited by 107Cancer, Lipids, and MetabolismBioactive Compounds and Antitumor AgentsAntifungal resistance and susceptibility

Repurposing itraconazole as an anticancer agent

Open access

Tsubamoto, Hiroshi, Ueda, Tomoko, Inoue, Kayo, Sakata, Kazuko, Shibahara, Hiroaki, Sonoda, Takashi·2017·Oncology Letters

DOI 10.3892/ol.2017.6325PMC PMC5529765

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Abstract

Itraconazole, a common anti-fungal agent, has demonstrated potential anticancer activity, including reversing chemoresistance mediated by P-glycoprotein, modulating the signal transduction pathways of Hedgehog, mechanistic target of rapamycin and Wnt/β-catenin in cancer cells, inhibiting angiogenesis and lymphangiogenesis, and possibly interfering with cancer-stromal cell interactions. Clinical trials have suggested the clinical benefits of itraconazole monotherapy for prostate cancer and basal cell carcinoma, as well as the survival advantage of combination chemotherapy for relapsed non-small cell lung, ovarian, triple negative breast, pancreatic and biliary tract cancer. As drug repurposing is cost-effective and timesaving, a review was conducted of preclinical and clinical data focusing on the anticancer activity of itraconazole, and discusses the future directions for repurposing itraconazole as an anticancer agent.

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Itraconazole's antifungal activity is likely independent of its anticancer effects.
“However, ITZ's antifungal activity is likely independent of its anticancer effects.9”
From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [9]
Itraconazole has recently shown promising anticancer activity.
“Itraconazole (ITZ), a triazole antifungal approved in 1992 and widely used for over 30 years, has recently shown promising anticancer activity.”
From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [9]
Evidence from both preclinical and clinical research supports itraconazole's potential as an anticancer agent, either used on its own or in combination with other chemotherapeutic drugs.
“Evidence from both preclinical and clinical research supports its potential as an anticancer agent, either used on its own or in combination with other chemotherapeutic drugs.9”
From Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights (2026) · cites this paper as [9]

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Drug Repurposing for Cancer Treatment: A Comprehensive Review
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Drug repurposing—an emerging strategy in cancer therapeutics
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Breast Cancer Stem Cells: Signaling Pathways, Cellular Interactions, and Therapeutic Implications
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Drug repurposing: re-inventing therapies for cancer without re-entering the development pipeline—a review
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Repurposing itraconazole to the benefit of skin cancer treatment: A combined azole-DDAB nanoencapsulation strategy
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The activation of the adaptor protein STING depends on its interactions with the phospholipid PI4P
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Drug Repurposing, an Attractive Strategy in Pancreatic Cancer Treatment: Preclinical and Clinical Updates
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The Interplay among Radiation Therapy, Antibiotics and the Microbiota: Impact on Cancer Treatment Outcomes
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Improving Drug Delivery of Micellar Paclitaxel against Non‐Small Cell Lung Cancer by Coloading Itraconazole as a Micelle Stabilizer and a Tumor Vascular Manipulator
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Enhancing the in vitro and in vivo activity of itraconazole against breast cancer using miltefosine-modified lipid nanocapsules
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Inhibition of CAL27 Oral Squamous Carcinoma Cell by Targeting Hedgehog Pathway With Vismodegib or Itraconazole
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Drug repurposing: An emerging strategy in alleviating skin cancer
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Drug Repurposing Opportunities in Pancreatic Ductal Adenocarcinoma
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Unveiling the crossroads of STING signaling pathway and metabolic reprogramming: the multifaceted role of the STING in the TME and new prospects in cancer therapies
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Itraconazole inhibits proliferation of pancreatic cancer cells through activation of Bak‐1
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MDACT: A New Principle of Adjunctive Cancer Treatment Using Combinations of Multiple Repurposed Drugs, with an Example Regimen
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Co-Delivery of Repurposing Itraconazole and VEGF siRNA by Composite Nanoparticulate System for Collaborative Anti-Angiogenesis and Anti-Tumor Efficacy against Breast Cancer
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Why make it if you can take it: review on extracellular cholesterol uptake and its importance in breast and ovarian cancers
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Repurposing Itraconazole and Hydroxychloroquine to Target Lysosomal Homeostasis in Epithelial Ovarian Cancer
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Itraconazole inhibits tumor growth via <scp>CEBPB</scp>‐mediated glycolysis in colorectal cancer
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Synthesis and biological evaluation of novel 2-oxo-1,2-dihydroquinoline-4-carboxamide derivatives for the treatment of esophageal squamous cell carcinoma
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Oral itraconazole for epistaxis in hereditary hemorrhagic telangiectasia: a proof of concept study
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Development of PI3Kα inhibitors for tumor therapy
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Beyond cyclopamine: Targeting Hedgehog signaling for cancer intervention
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Itraconazole synergistically increases therapeutic effect of paclitaxel and 99mTc-MIBI accumulation, as a probe of P-gp activity, in HT-29 tumor-bearing nude mice
Ghadi, M., Hosseinimehr, S. J., Amiri, F. T., Mardanshahi, A., & Noaparast, Z. (2021) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2021.173892 · Cited by 17 · see citing works
Discovery of indoline derivatives as anticancer agents via inhibition of tubulin polymerization
Wang, S., Liu, X., Meng, L., Li, M., Li, Y.-R., Yu, G.-X., Song, J., Zhang, H., Chen, P., Zhang, S., et al. (2021) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2021.128095 · Cited by 17 · see citing works
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Old drugs, new challenges: reassigning drugs for cancer therapies
Czechowicz, P., Więch, A., Sławski, J., Collawn, J. F., & Bartoszewski, R. (2025) · Cellular & Molecular Biology Letters · doi:10.1186/s11658-025-00710-0 · Cited by 17 · see citing works
An FDA-Approved Antifungal, Ketoconazole, and Its Novel Derivative Suppress tGLI1-Mediated Breast Cancer Brain Metastasis by Inhibiting the DNA-Binding Activity of Brain Metastasis-Promoting Transcription Factor tGLI1
Doheny, D. L., Manore, S. G., Sirkisoon, S. R., Zhu, D., Aguayo, N. R., HARRISON, A. V., Najjar, M. K., Anguelov, M., Cox, A. O., Furdui, C. M., et al. (2022) · Cancers · doi:10.3390/cancers14174256 · Cited by 16 · see citing works
Itraconazole treatment of primary malignant melanoma of the vagina evaluated using positron emission tomography and tissue cDNA microarray: a case report
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The Antitumor Activity of a Lead Thioxanthone is Associated with Alterations in Cholesterol Localization
Lima, R. T., Sousa, D., Gomes, A. S., Mendes, N. M., Matthiesen, R., Pedro, M., Marques, F., Pinto, M. M. M., Sousa, E., & Vasconcelos, M. H. (2018) · Molecules · doi:10.3390/molecules23123301 · Cited by 15 · see citing works
Resurgence and Repurposing of Antifungal Azoles by Transition Metal Coordination for Drug Discovery
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Drug design strategies for the treatment azole-resistant candidiasis
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Topical delivery of seriniquinone for treatment of skin cancer and fungal infections is enabled by a liquid crystalline lamellar phase
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S-1, Oxaliplatin, Nab-paclitaxel and Itraconazole for Conversion Surgery for Advanced or Recurrent Gastric Cancer
SAWASAKI, M., Tsubamoto, H., Nakamoto, Y., Kakuno, A., & Sonoda, T. (2020) · Anticancer Research · doi:10.21873/anticanres.14033 · Cited by 13 · see citing works
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Enhancement of Liposomal Plasmid DNA and siRNA Delivery by Itraconazole through Intracellular Cholesterol Accumulation
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Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains
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Role of Fungi in Tumorigenesis: Promises and Challenges
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Learning Opportunities for Drug Repositioning via GWAS and PheWAS Findings.
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Investigation of the Antifungal and Anticancer Effects of the Novel Synthesized Thiazolidinedione by Ion-Conductance Microscopy
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Imidazole Antifungals: A Review of Their Action Mechanisms on Cancerous Cells
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Intratracheal Administration of Itraconazole-Loaded Hyaluronated Glycerosomes as a Promising Nanoplatform for the Treatment of Lung Cancer: Formulation, Physiochemical, and In Vivo Distribution
Aati, S., Farouk, H. O., Elkarmalawy, M. H., Aati, H. Y., Tolba, N. S., Hassan, H. M., Rateb, M. E., & Hamad, D. S. (2024) · Pharmaceutics · doi:10.3390/pharmaceutics16111432 · Cited by 9 · see citing works
Plant-derived extracellular vesicles for itraconazole delivery across the blood-brain barrier for potential glioblastoma treatment
Bhom, N., Ramburrun, P., Somandi, K., & Choonara, Y. E. (2026) · Scientific Reports · doi:10.1038/s41598-025-33187-0 · Cited by 9 · see citing works
The bromodomain inhibitor IBET-151 attenuates vismodegib-resistant esophageal adenocarcinoma growth through reduction of GLI signaling
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Epithelial-Mesenchymal Transition in Cancer: A Focus on Itraconazole, a Hedgehog Inhibitor
Kulkarni, A. M., Gayam, P. K. R., Baby, B. T., & Aranjani, J. M. (2025) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2025.189279 · Cited by 8 · see citing works
Repurposing Drugs Based on Evolutionary Relationships Between Targets of Approved Drugs and Proteins of Interest
Chakraborti, S., Ramakrishnan, G., & Srinivasan, N. (2018) · Methods in molecular biology · doi:10.1007/978-1-4939-8955-3_3 · Cited by 7 · see citing works
Antiparasitic and Antifungal Medications for Targeting Cancer Cells Literature Review and Case Studies.
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Unfolding antifungals: as a new foe to pancreatic ductal adenocarcinoma—a mini-review
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Inhibition of hedgehog signaling by stereochemically defined des-triazole itraconazole analogues
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Strategies for the treatment of breast cancer: from classical drugs to mathematical models
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Exploring the role of pomalidomide in androgen-dependent prostate cancer: a computational analysis
Pathak, S., Singh, V. K., Gupta, P. K., Mahapatra, A. K., Giri, R., Sahu, R., Sharma, R., & Garg, N. (2024) · Molecular Diversity · doi:10.1007/s11030-024-11081-7 · Cited by 6 · see citing works
Itraconazole Increases Resolvin E3 Concentration and 12/15-lipoxygenase Inhibitor Attenuates Itraconazole Cytotoxicity in Cervical Cancer Cells
ISONO, R., TSUBAMOTO, H., INOUE, K., UEDA, T., TAKIMOTO, Y., SAKATA, K., SHINOHARA, M., & SHIBAHARA, H. (2021) · Anticancer Research · doi:10.21873/anticanres.15231 · Cited by 6 · see citing works
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PaSTe. Blockade of the Lipid Phenotype of Prostate Cancer as Metabolic Therapy: A Theoretical Proposal
Romo‐Pérez, A., Domínguez-Gómez, G., Chávez-Blanco, A. D., González‐Fierro, A., Correa‐Basurto, J., & Dueñas‐González, A. (2023) · Current Medicinal Chemistry · doi:10.2174/0929867330666230607104441 · Cited by 6 · see citing works
Itraconazole Promotes Macrophage M1 Polarization and Phagocytic Capacity of Macrophage to Candida Albicans
Zheng, X., Liang, G., Shi, D., Yao, H., Zhang, L., Liu, W., & Chen, G. (2019) · International Journal of Dermatology and Venereology · doi:10.1097/jd9.0000000000000044 · Cited by 6 · see citing works
Physicochemical and pathohistological changes in experimental fibrosarcoma tumors of hamsters treated with metformin and itraconazole
Popović, K. J., Popović, D. J., Miljković, D., Lalošević, D., Čapo, I., & Popović, J. K. (2019) · Oncology Letters · doi:10.3892/ol.2019.10509 · Cited by 6 · see citing works
Identification of Keratinocyte Cytoprotectants against Toxicity by the Multikinase Inhibitor Sorafenib Using Drug Repositioning
Kamata, Y., Kato, R., Tominaga, M., Toyama, S., Komiya, E., Utsumi, J., Kaneko, T., Suga, Y., & Takamori, K. (2024) · JID Innovations · doi:10.1016/j.xjidi.2024.100271 · Cited by 5 · see citing works
Breast Cancer Drug Repurposing a Tool for a Challenging Disease
Malik, J. A., Jan, R., Ahmed, S., & Anwar, S. (2022) · IntechOpen eBooks · doi:10.5772/intechopen.101378 · Cited by 5 · see citing works
Itraconazole Improves Vulvodynia in Fungus Culture-Negative Patients Post Fluconazole Failure
Rothenberger, R., Jones, W., & MacNeill, C. (2021) · Sexual Medicine · doi:10.1016/j.esxm.2021.100383 · Cited by 5 · see citing works
IC Regimen: Delaying Resistance to Lorlatinib in ALK Driven Cancers by Adding Repurposed Itraconazole and Cilostazol
Kast, R. E. (2024) · Cells · doi:10.3390/cells13141175 · Cited by 4 · see citing works
In silico drug repurposing: An antifungal drug, itraconazole, repurposed as an anticancer agent using molecular docking
Srivastav, A., Dhorje, S., & Lavhate, P. (2020) · MGM Journal of Medical Sciences · doi:10.4103/mgmj.mgmj_31_20 · Cited by 4 · see citing works
Non-Polio Enterovirus Inhibitors: Scaffolds, Targets, and Potency─What’s New?
Roux, H., Touret, F., Rathelot, P., Sciò, P., Coluccia, A., Vanelle, P., & Roche, M. (2024) · ACS Infectious Diseases · doi:10.1021/acsinfecdis.4c00606 · Cited by 3 · see citing works
Novel Azole-Modified Porphyrins for Mitochondria-Targeted Photodynamic Therapy
Rangasamy, S., Bandini, E., Venturini, A., Bozzuto, G., Migani, S., Calcabrini, A., Sennato, S., Zuffa, C., Maini, L., Brion, A., et al. (2025) · Molecules · doi:10.3390/molecules30132688 · Cited by 3 · see citing works
Drug repurposing in leukemia treatment and hematopoietic stem cell transplantation
Чухловин, А. Б. (2019) · Cellular Therapy and Transplantation · doi:10.18620/ctt-1866-8836-2019-8-1-12-19 · Cited by 3 · see citing works
Non-self glycan structures as possible modulators of cancer progression: would polysaccharides from Cryptococcus spp. impact this phenomenon?
Diniz-Lima, I., da Fonseca, L. M., dos Reis, J. S., Decotè-Ricardo, D., Morrot, A., Previato, J. O., Mendonça‐Previato, L., Freire-de-Lima, C. G., & Freire‐de‐Lima, L. (2023) · Brazilian Journal of Microbiology · doi:10.1007/s42770-023-00936-0 · Cited by 3 · see citing works
Drug Repositioning for Ovarian Cancer Treatment: An Update
Cavalluzzi, M. M., Viale, M., Rotondo, N. P., Ferraro, V., & Lentini, G. (2024) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/0118715206282904240122063914 · Cited by 3 · see citing works
IC Regimen: Delaying Resistance to Lorlatinib in ALK Driven Cancers Using Repurposed Itraconazole and CilostazolPreprint
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Recent advances in anticancer drug discovery: A review
Tadesse, A., Nemomsa, K., & Beyene, F. (2023) · International Journal of Pharmaceutical Chemistry and Analysis · doi:10.18231/j.ijpca.2023.039 · Cited by 2 · see citing works
Immunohistochemical evidences of anticancer actions of metformin with other repurposed drug combinations and correlation with hamster fibrosarcoma tumor size
Popović, J. K., Popović, D. J., Popović, K. J., Miljković, D., Lalošević, D., Dolicanin, Z. C., & Čapo, I. (2024) · Journal of the Serbian Chemical Society · doi:10.2298/jsc231203007p · Cited by 2 · see citing works
Effects of metformin and its combinations with other repurposed drugs on fibrosarcoma in hamsters
Popović, D. J., Popović, K. J., Lalošević, D., & Popović, J. K. (2024) · Srpski arhiv za celokupno lekarstvo · doi:10.2298/sarh230325027p · Cited by 2 · see citing works
Advances in genetic understanding of gorlin syndrome and emerging treatment options
Shih, S., Dai, C., Ansari, A., Urso, B., Laughlin, A. I., & Solomon, J. A. (2018) · Expert Opinion on Orphan Drugs · doi:10.1080/21678707.2018.1483233 · Cited by 2 · see citing works
The Expendables: Overlooked Medications with Anti-Cancer Properties
Deshpande, A. J., Munoz, J. L., & Kurzrock, R. (2025) · Current Oncology Reports · doi:10.1007/s11912-025-01721-y · Cited by 1 · see citing works
Molecular mechanisms and therapeutic perspectives in vulvodynia: From current evidence to future investigations
ALBANO, A., Brasi, L., Loperfido, F., Griffante, G., Cianci, M. A., Donati, G., & Proserpio, V. (2026) · Cell Reports Medicine · doi:10.1016/j.xcrm.2026.102917 · Cited by 1 · see citing works
Drug Repurposing in Biomedical Research: Benefits and Challenges
Sharma, A., & Kaur, J. (2022) · Springer eBooks · doi:10.1007/978-981-16-9232-1_3 · Cited by 1 · see citing works
Effect of Shear Strain on the Supercooled Itraconazole
Knapik-Kowalczuk, J., Kramarczyk, D., Jachowicz, R., & Paluch, M. (2023) · Journal of Pharmaceutical Sciences · doi:10.1016/j.xphs.2023.01.020 · Cited by 1 · see citing works
Discovery of anticancer therapeutics: Computational chemistry and Artificial Intelligence-assisted approach
Das, S. K., Talukdar, A. D., Nath, D., & Choudhury, M. D. (2023) · Elsevier eBooks · doi:10.1016/b978-0-443-15280-1.00007-8 · Cited by 1 · see citing works
A Review on Repurposing of Drug
Jannat, A., Rafique, S., Javed, S., Habib, A., & Afzal, Z. (2024) · Pakistan Journal of Medical and Health Sciences · doi:10.53350/pjmhs0202317112 · Cited by 1 · see citing works
WITHDRAWN: Discovery of indoline derivatives as anticancer agents via inhibition of tubulin polymerization
Wang, S., Liu, X., Meng, L., Li, M., Li, Y.-R., Yu, G.-X., Song, J., Zhang, H., Chen, P., Zhang, S., et al. (2021) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2021.128131 · Cited by 1 · see citing works
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Itraconazole as a repurposed anti-cancer agent: focusing on synthesis, mechanisms of action and therapeutic insights
Marzi, M., Ghasemian, A., Ghanbariasad, A., Nournia, E., & Zarenezhad, E. (2026) · RSC Advances · doi:10.1039/d5ra09799a
Clinical trials on combination of repurposed drugs and anticancer therapies
Ölgen, S. (2020) · Elsevier eBooks · doi:10.1016/b978-0-12-819668-7.00015-4
Miltefosina como alternativa para o tratamento da criptococose: mecanismo de ação e nanopartículas de alginato como carreadores.
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STING activation depends on ACBD3 and other phosphatidylinositol 4-phosphate-regulating proteinsPreprint
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Authors: Tsubamoto, H., Ueda, T., Inoue, K., Sakata, K., Shibahara, H., & Sonoda, T.
Affiliations: Hyogo Medical University (JP)
Meiwa Hospital (JP)
ORCID: Tsubamoto, Hiroshi
Sakata, Kazuko
Shibahara, Hiroaki
Venue: Oncology Letters
Publisher: Spandidos Publications
Published: 2017-06-07
Volume: 14
Issue: 2
Pages: 1240-1246
ISSN: 1792-1074 (ISSN-L)
1792-1082
DOI: 10.3892/ol.2017.6325
PMC: PMC5529765
OpenAlex: W2622188990
Cited by: 107
References: 57
Citations by year: 2026: 7 · 2025: 9 · 2024: 16 · 2023: 11 · 2022: 15 · 2021: 13 · 2020: 15 · 2019: 8 · 2018: 13
FWCI: 3.31
Type: journal article
Language: en
Open access: diamond
doi.org
Locations: Oncology Letters (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Funders: Japan Society for the Promotion of Science (16K11166)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Lipids, and Metabolism
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Toxicology › Bioactive Compounds and Antitumor Agents
Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
Keywords: itraconazole, drug repurposing, anticancer activity, P-glycoprotein, chemoresistance, Hedgehog signaling, mTOR signaling, Wnt/β-catenin signaling, angiogenesis inhibition, lymphangiogenesis, prostate cancer, basal cell carcinoma, combination chemotherapy, non-small cell lung cancer, ovarian cancer, triple-negative breast cancer, pancreatic cancer, biliary tract cancer

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