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Development of the pan-DAC inhibitor panobinostat (LBH589): successes and challenges

Peter Atadja1

  • 1Novartis Institutes for Biomedical Research, Cambridge, MA, USA. peter.atadja@novartis.com

Cancer Letters
|April 7, 2009
PubMed

Insights

Panobinostat, a histone deacetylase (HDAC) inhibitor, shows potent anti-tumor activity by inhibiting HDAC enzymes. This anticancer agent demonstrates promising clinical efficacy in various cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Histone deacetylase (HDAC) inhibitors are a promising class of anticancer agents.
  • HDAC enzymes play a crucial role in cancer development through protein deacetylation.
  • Panobinostat is a potent inhibitor of all HDAC enzymes implicated in cancer.

Purpose of the Study:

  • To review the development of panobinostat, an HDAC inhibitor.
  • To discuss its mechanism of action, preclinical anti-tumor activity, and clinical efficacy.
  • To highlight the successes and challenges in panobinostat's therapeutic journey.

Main Methods:

  • Review of preclinical studies on panobinostat's anti-tumor activity.
  • Analysis of clinical trial data for panobinostat in hematologic and solid tumors.
  • Examination of panobinostat's proposed molecular mechanism of action.

Main Results:

  • Panobinostat demonstrates potent inhibition of all HDAC enzymes.
  • Preclinical models show significant anti-tumor activity for panobinostat.
  • Early clinical trials indicate promising efficacy in both hematologic and solid tumors.

Conclusions:

  • Panobinostat is a potent HDAC inhibitor with demonstrated anti-tumor effects.
  • The drug shows promise for treating various cancers, including hematologic and solid tumors.
  • Further development is ongoing to address challenges and optimize its therapeutic use.

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