The power and the promise of epigenetic drugs in oncology
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Updated: Jan 20, 2026

Toxicological Assays for Testing Effects of an Epigenetic Drug on Development, Fecundity and Survivorship of Malaria Mosquitoes
Published on: January 16, 2015
Thalita Basso Scandolara1, Isabelle Vasconcelos Menegoy Siqueira2, Luis Felipe Ribeiro Pinto2
1Laboratory of Experimental Oncology, Post-Graduation Program in Translational Medicine, Drug Research and Development Center (NPDM), Federal University of Ceará, Fortaleza, Ceará, Brazil.
Abstract:
Epigenetic dysregulation is commonly observed in cancer and has been shown to contribute to different steps of carcinogenesis, from initiation, making cells more prone to transformation, to progression and treatment resistance. Therefore, based on their frequency, relevance and reversibility, epigenetic alterations are promising therapeutic targets in oncology. Although the concept of targeting epigenetic mechanisms is not new, recent advances have been made in reducing toxicity, augmenting specificity, diversifying the targets and combining therapies. In this scoping review, we introduce the main epigenetic mechanisms of gene expression regulation and bring the current knowledge on available epidrugs, focusing on their mechanisms of action and ongoing clinical trials.
Insights
Epigenetic alterations drive cancer development and resistance. Targeting these reversible changes with novel epigenetic drugs (epidrugs) offers a promising therapeutic strategy in oncology.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Epigenetic dysregulation is a hallmark of cancer, influencing carcinogenesis from initiation to treatment resistance.
- Epigenetic alterations are frequent, relevant, and reversible, making them attractive therapeutic targets.
Purpose of the Study:
- To review the primary epigenetic mechanisms regulating gene expression.
- To summarize current knowledge on available epigenetic drugs (epidrugs).
- To focus on epidrug mechanisms of action and clinical trial status.
Main Methods:
- Scoping review methodology.
- Literature search for epigenetic mechanisms and epidrugs.
- Analysis of drug mechanisms and clinical trial data.
Main Results:
- Overview of key epigenetic regulatory mechanisms.
- Identification of currently available epidrugs.
- Summary of ongoing clinical trials investigating epidrugs.
Conclusions:
- Epigenetic therapies are advancing with improved specificity and reduced toxicity.
- Targeting epigenetic alterations represents a significant therapeutic avenue in cancer treatment.
- Further research and clinical trials are crucial for optimizing epidrug efficacy.
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