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Promises and challenges of anticancer drugs that target the epigenome

Inge Verbrugge1, Ricky W Johnstone, Michael Bots

  • 1Cancer Therapeutics Program, Peter MacCallum Cancer Centre, St Andrews Place, East Melbourne 3002, Victoria, Australia.

Epigenomics
|December 1, 2011
PubMed

Insights

Epigenetic aberrations drive cancer, but epigenetic drugs show limited success in solid tumors. Strategies are discussed to enhance drug responses in both blood and solid cancers.

Area of Science:

  • Oncology
  • Epigenetics
  • Cancer Biology

Background:

  • Epigenetic aberrations are key drivers of tumorigenesis across various cancers.
  • Small molecule inhibitors targeting epigenetic enzymes show preclinical promise against hematological and solid tumors.

Purpose of the Study:

  • To review epigenetic aberrations in diverse cancers.
  • To analyze clinical responses to epigenetic drugs.
  • To explore strategies for improving epigenetic drug efficacy in solid tumors.

Main Methods:

  • Literature review of epigenetic aberrations in cancer.
  • Analysis of clinical trial data for epigenetic inhibitors.
  • Discussion of therapeutic strategies to overcome resistance.

Main Results:

  • Epigenetic inhibitors are effective in preclinical models but clinically limited, mainly to hematological malignancies.
  • Significant epigenetic alterations are observed in both hematological and solid tumors.
  • Clinical efficacy of epigenetic drugs is restricted in solid tumors compared to hematological cancers.

Conclusions:

  • Despite preclinical promise, clinical efficacy of epigenetic drugs is largely confined to hematological malignancies.
  • Further research is needed to understand and overcome resistance mechanisms in solid tumors.
  • Developing novel strategies is crucial to broaden the therapeutic application of epigenetic drugs in oncology.

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