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Review
. 2023 Apr;15(8):517-537.
doi: 10.2217/epi-2023-0142. Epub 2023 Jun 14.

Role of epigenetic drugs in sensitizing cancers to anticancer therapies: emerging trends and clinical advancements

Deepti Singh  1 , Mohammad Afsar Khan  1 , Hifzur R Siddique  1
Affiliations
Review

Role of epigenetic drugs in sensitizing cancers to anticancer therapies: emerging trends and clinical advancements

Deepti Singh et al. Epigenomics. 2023 Apr.

Abstract

Epigenetic changes play a significant role in cancer progression, maintenance and therapy resistance. Generally, epigenetic modifications are reversible, thereby gaining attention for therapeutic interventions. However, limited efficacy and therapy resistance remain the significant limitations of conventional and epigenetic anticancer therapies. Recently, combination therapies with epigenetic drugs (epi-drugs) and conventional anticancer treatment have gained widespread attention. Here, epi-drugs are administered with anticancer therapies to increase their therapeutic efficacy and sensitize cancer cells resistant to therapies. This review summarizes the mechanism of epi-drugs in reversing resistance to anticancer therapies. Further, the challenges faced during developing combination therapies with epi-drugs are discussed. We believe the clinical benefit of combination therapies could be increased by overcoming the challenges faced during epi-drug development.

Keywords: DNMTi; HDACi; cancer epigenetics; conventional therapies; epi-drugs; therapy resistance.

Plain language summary

Epigenetic changes play a significant role in cancer development and progression. Epigenetic drugs (epi-drugs) target enzymes involved in regulating epigenetic changes to maintain normal cell functioning. Epi-drugs include histone deacetylase inhibitors and DNA methyltransferase inhibitors, among others. These drugs have shown potential as standalone treatments for cancer and have also been found to work well in combination with other therapies (chemotherapy, radiotherapy and immunotherapy), helping to overcome treatment resistance. By targeting the epigenetic alterations that contribute to treatment resistance, epi-drugs have the potential to enhance the effectiveness of these therapies. This review article focuses on how epi-drugs overcome resistance to different cancer treatments. Combining epi-drugs with conventional anticancer therapies could provide better management of cancer. However, more preclinical and clinical research is needed to understand the potential benefits and optimize the use of these combinations fully. Overall, epi-drugs offer a promising avenue for improving cancer treatment outcomes and warrant further investigation.

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