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Hsp90 inhibitors in the clinic

S Pacey1, U Banerji, I Judson

  • 1Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey.

Handbook of Experimental Pharmacology
|April 14, 2006
PubMed

Insights

Heat shock protein 90 (Hsp90) inhibitors are advancing in clinical trials for metastatic cancers. These agents show promise by blocking multiple cancer pathways, with manageable toxicity and early signs of activity.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Heat shock protein 90 (Hsp90) is crucial for stabilizing proteins involved in cancer cell growth and survival.
  • Dysregulation of protein folding is implicated in various diseases, including cancer.
  • Hsp90 inhibitors offer a novel therapeutic strategy by simultaneously targeting multiple oncogenic pathways.

Purpose of the Study:

  • To provide an update on current clinical trials involving Hsp90 inhibitors.
  • To highlight the potential of Hsp90 inhibitors in treating metastatic cancers and other diseases.
  • To discuss the future relevance of Hsp90 inhibitors in clinical practice over the next five years.

Main Methods:

  • Review of ongoing and completed Phase I and Phase II clinical trials of Hsp90 inhibitors.
  • Analysis of efficacy and toxicity data from these trials.
  • Assessment of the rationale for Hsp90 inhibitor use in diseases beyond cancer.

Main Results:

  • The first Hsp90 inhibitor, 17-AAG, has completed Phase I and is in Phase II trials.
  • Manageable toxicity profiles have been observed.
  • Evidence of clinical activity has been noted in metastatic melanoma, prostate cancer, and multiple myeloma.

Conclusions:

  • Hsp90 inhibitors represent a promising therapeutic class for cancer treatment due to their multi-targeted approach.
  • Further development of Hsp90 inhibitors with improved properties is underway.
  • Hsp90 inhibitors are expected to play an increasingly significant role in clinical oncology.

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