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Updated: May 10, 2026

Evaluating the Effectiveness of Cancer Drug Sensitization In Vitro and In Vivo
Published on: February 6, 2015
[Epigenetic cancer drugs and their role in anticancer therapy]
1Interní klinika 1. lékařské fakulty UK a VFN v Praze. pavel.klener@ruk.cuni.cz
Abstract:
Epigenetic modification have been causally linked to cancer development and progression, and are potentially reversible by treatments with epigenetic cancer drugs. The aim of this review is to give an overview of the basic current knowledge on molecular mechanisms of epigenetic cancer drugs and their possible clinical use. Many of them are in in clinical trials. However only two demethylating agents ie. inhibitors of DNA methyltransferase (5- azacytidin and decitabin) are approved in the treatment of myelodysplastic syndrome and a few inhibitors of histonacetylase (vorinostat, romidepsin and panobinostat) are approved in the treatment of hematological malignancies, particularly in refractory or relapsed cutaneous T cell lymhoma.
Insights
Epigenetic drugs offer reversible cancer treatments by targeting DNA methylation and histone acetylation. Approved drugs include DNA methyltransferase inhibitors for myelodysplastic syndrome and histone acetylase inhibitors for certain blood cancers.
Area of Science:
- Oncology
- Epigenetics
- Pharmacology
Background:
- Epigenetic modifications are key drivers in cancer development and progression.
- These epigenetic changes are potentially reversible, presenting therapeutic opportunities.
- Epigenetic cancer drugs aim to reverse these alterations.
Purpose of the Study:
- To review current knowledge on the molecular mechanisms of epigenetic cancer drugs.
- To explore the potential clinical applications of these drugs.
- To provide an overview of epigenetic drugs in clinical trials and approved therapies.
Main Methods:
- Literature review of basic science and clinical data on epigenetic cancer drugs.
- Focus on molecular mechanisms, including DNA methyltransferase and histone acetylase inhibition.
- Analysis of approved drugs and their indications, as well as drugs in clinical trials.
Main Results:
- Several epigenetic drugs are currently undergoing clinical trials.
- Two demethylating agents (5-azacytidine and decitabine) are approved for myelodysplastic syndrome.
- Histone acetylase inhibitors (vorinostat, romidepsin, panobinostat) are approved for hematological malignancies, especially T-cell lymphoma.
Conclusions:
- Epigenetic drugs represent a promising class of cancer therapeutics.
- Approved epigenetic drugs have shown efficacy in specific hematological malignancies.
- Ongoing clinical trials suggest expanding applications for these reversible therapies.
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