ArticleBritish journal of cancer2020
5-Azacytidine inhaled dry powder formulation profoundly improves pharmacokinetics and efficacy for lung cancer therapy through genome reprogramming.
Article in British journal of cancer, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Zwitterion-Based Polymeric Carriers for Efficient Drug Delivery across Biological Barriers.Polymer science & technology (Washington, D.C.) · 2026Review
- Spray-Drying Process Optimization and Modeling for an Inhaled Dry Powder of 5-Azacytidine for Treating Local and Metastatic Lung Cancer.Molecular pharmaceutics · 2025Article
- Unmasking Pediatric Asthma: Epigenetic Fingerprints and Markers of Respiratory Infections.International journal of molecular sciences · 2025Review
- Progressive lung fibrosis: reprogramming a genetically vulnerable bronchoalveolar epithelium.The Journal of clinical investigation · 2025Review
- Approaches and applications in transdermal and transpulmonary gene drug delivery.Frontiers in bioengineering and biotechnology · 2024Review
- Inhaled Medicines for Targeting Non-Small Cell Lung Cancer.Pharmaceutics · 2023Review
- Parental methylation mediates how progeny respond to environments of parents and of progeny themselves.Annals of botany · 2022Article
- Simultaneous Spray Drying for Combination Dry Powder Inhaler Formulations.Pharmaceutics · 2022Article
- Inhalation delivery dramatically improves the efficacy of topotecan for the treatment of local and distant lung cancer.Drug delivery · 2021Article
- Local Treatment of Non-small Cell Lung Cancer with a Spray-Dried Bevacizumab Formulation.AAPS PharmSciTech · 2021Article
- First-in-human study of inhaled Azacitidine in patients with advanced non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands) · 2021Article
- Review
Corrections and comments
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Authors and funding
15 authors.
Funding
Abstract
backgroundEpigenetic therapy through demethylation of 5-methylcytosine has been largely ineffective in treating lung cancer, most likely due to poor tissue distribution with oral or subcutaneous delivery of drugs such as 5-azacytidine (5AZA). An inhalable, stable dry powder formulation of 5AZA was developed.
methodsPharmacokinetics of inhaled dry powder and aqueous formulations of 5AZA were compared to an injected formulation. Efficacy studies and effect of therapy on the epigenome were conducted in an orthotopic rat lung cancer model for inhaled formulations.
resultsInhaled dry powder 5AZA showed superior pharmacokinetic properties in lung, liver, brain and blood compared to the injected formulation and for all tissues except lung compared to an inhaled aqueous formulation. Only dry powder 5AZA was detected in brain (~4-h half-life). Inhaled dry powder was superior to inhaled aqueous 5AZA in reducing tumour burden 70-95%. Superiority of inhaled 5AZA dry powder was linked to effectively reprogramming the cancer genome through demethylation and gene expression changes in cancer signalling and immune pathways.
conclusionsThese findings could lead to widespread use of this drug as the first inhaled dry powder therapeutic for treating local and metastatic lung cancer, for adjuvant therapy, and in combination with immunotherapy to improve patient survival.
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