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Farnesyltransferase inhibitors as anticancer agents: critical crossroads

Ronald J Doll1, Paul Kirschmeier, W Robert Bishop

  • 1Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033-1300, USA. ronald.doll@spcorp.com

Current Opinion in Drug Discovery & Development
|September 2, 2004
PubMed

Insights

Farnesyltransferase (FT) inhibitors show anticancer effects beyond Ras mutations, targeting other proteins. Research explores their development and clinical trials to improve efficacy for cancer treatment.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Farnesyltransferase (FT) inhibitors were initially developed as anticancer drugs targeting mutant Ras proteins.
  • Subsequent research revealed antitumor effects independent of Ras mutations, indicating broader mechanisms of action.
  • This highlights the involvement of other protein targets in the efficacy of FT inhibitors.

Purpose of the Study:

  • To discuss the preclinical and clinical development of farnesyltransferase inhibitors.
  • To review the clinical results of tipifarnib and lonafarnib in Phase III trials.
  • To explore strategies for enhancing the success of FT inhibitors as anticancer drugs.

Main Methods:

  • Review of preclinical data on FT inhibitor development.
  • Analysis of clinical trial outcomes for tipifarnib and lonafarnib.
  • Inclusion of information on novel FT inhibitors reported since 2003.

Main Results:

  • Tipifarnib and lonafarnib are the only FT inhibitors to reach Phase III clinical trials.
  • Clinical results from these trials are presented, with a focus on therapeutic potential.
  • New FT inhibitors and their development status since early 2003 are detailed.

Conclusions:

  • FT inhibitors possess anticancer activity through mechanisms beyond Ras farnesylation.
  • Clinical development of FT inhibitors like tipifarnib and lonafarnib has been significant.
  • Further research and strategic development are crucial for optimizing FT inhibitor-based cancer therapies.

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