ArticleBritish journal of cancer2013
Aerosolised 5-azacytidine suppresses tumour growth and reprogrammes the epigenome in an orthotopic lung cancer model.
Article in British journal of cancer, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 35 citations in OpenAlex.
- Low E-cadherin expression is associated with poor prognosis in pulmonal adenocarcinoma.Scientific reports · 2026Article
- Review
- 5-Azacytidine treatment inhibits the development of lung cancer models via epigenetic reprogramming and activation of cellular pathways with anti-tumor activity.Medicine and pharmacy reports · 2024Article
- Functional characterization of age-dependent p16 epimutation reveals biological drivers and therapeutic targets for colorectal cancer.Journal of experimental & clinical cancer research : CR · 2023Article
- Inhalation delivery dramatically improves the efficacy of topotecan for the treatment of local and distant lung cancer.Drug delivery · 2021Article
- 5-Azacytidine inhaled dry powder formulation profoundly improves pharmacokinetics and efficacy for lung cancer therapy through genome reprogramming.British journal of cancer · 2020Article
- Inhalable nanotherapeutics to improve treatment efficacy for common lung diseases.Wiley interdisciplinary reviews. Nanomedicine and nanobiotechnology · 2020Review
- Inhalation delivery of topotecan is superior to intravenous exposure for suppressing lung cancer in a preclinical model.Drug delivery · 2018Article
- Inhalable oridonin-loaded poly(lactic-Acta pharmaceutica Sinica. B · 2017Article
- miR-196b Is Epigenetically Silenced during the Premalignant Stage of Lung Carcinogenesis.Cancer research · 2016Article
- Toxicity and Pharmacokinetic Studies of Aerosolized Clinical Grade Azacitidine.Clinical lung cancer · 2016Article
- Epigenetics in non-small cell lung cancer: from basics to therapeutics.Translational lung cancer research · 2016Review
- Poly(I:C) and CpG-ODN combined aerosolization to treat lung metastases and counter the immunosuppressive microenvironment.Oncoimmunology · 2015Article
- Augmenting antitumor immune responses with epigenetic modifying agents.Frontiers in immunology · 2015Review
- Clinical importance and therapeutic implication of E-cadherin gene methylation in human ovarian cancer.Medical oncology (Northwood, London, England) · 2014Article
- Advances in device and formulation technologies for pulmonary drug delivery.AAPS PharmSciTech · 2014Review
- Aerosol azacytidine inhibits orthotopic lung cancers in mice through Its DNA demethylation and gene reactivation effects.PloS one · 2014Article
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
backgroundEpigenetic silencing by promoter methylation and chromatin remodelling affects hundreds of genes and is a causal event for lung cancer. Treatment of patients with low doses of the demethylating agent 5-azacytidine in combination with the histone deacetylase inhibitor entinostat has yielded clinical responses. The subcutaneous dosing route for consecutive days and reduced bioavailability of 5-azacytidine because of inactivation by cytidine deaminase may limit the expansion of epigenetic therapy into Phase III trials. To mitigate these barriers, an aerosol of 5-azacytidine was generated and characterised.
methodsThe effect of aerosol vs systemic delivery of 5-azacytidine on tumour burden and molecular response of engrafted lung tumours in the nude rat was compared.
resultsPharmacokinetics revealed major improvement in the half-life of 5-azacytidine in lung tissue with aerosol delivery. Aerosolised 5-azacytidine significantly reduced lung tumour burden and induced global demethylation of the epigenome at one-third of the comparable effective systemic dose. High commonality for demethylation of genes was seen in tumours sampled throughout lung lobes and across treated animals receiving the aerosolised drug.
conclusionCollectively, these findings show that aerosolised 5-azacytidine targets the lung, effectively reprogrammes the epigenome of tumours, and is a promising approach to combine with other drugs for treating lung cancer.
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