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Farnesyl transferase inhibitors: current developments and future perspectives

F A Eskens1, G Stoter, J Verweij

  • 1Department of Medical Oncology, Rotterdam Cancer Institute (Daniel den Hoed Kliniek), Rotterdam, The Netherlands. eskens@oncd.azr.nl

Cancer Treatment Reviews
|September 28, 2000
PubMed

Insights

Ras oncogene inhibition is a promising anticancer strategy. Farnesyl transferase inhibitors show potential, with early clinical studies defining new endpoints for treatment assessment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Ras oncogenes are critical drivers of human carcinogenesis.
  • Ras oncoprotein activity, regulated by farnesyl transferase, is essential for tumor development.
  • Targeting farnesyl transferase is a key strategy in anticancer drug development.

Purpose of the Study:

  • To review the role of Ras oncogenes in cancer.
  • To discuss the development and therapeutic potential of farnesyl transferase inhibitors.
  • To highlight the need for new endpoints in clinical trials for these agents.

Main Methods:

  • Review of preclinical and clinical data on farnesyl transferase inhibitors.
  • Analysis of the mechanism of Ras-dependent carcinogenesis.
  • Evaluation of emerging clinical trial designs and endpoints.

Main Results:

  • Farnesyl transferase inhibitors demonstrate significant in vitro and in vivo antitumor activity.
  • Early clinical studies with these inhibitors are underway.
  • New endpoints are required to accurately assess clinical value.

Conclusions:

  • Farnesyl transferase inhibitors represent a promising therapeutic avenue for Ras-driven cancers.
  • Further clinical investigation is necessary to establish their efficacy and optimal use.
  • Defining appropriate endpoints is crucial for successful clinical development.

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