Orally bioavailable farnesyltransferase inhibitors as anticancer agents in transgenic and xenograft models

M Liu1, W R Bishop, L L Nielsen

  • 1Schering-Plough Research Institute, Kenilworth, New Jersey 07033-1300, USA.

Methods in Enzymology
|June 13, 2001
PubMed

Insights

Farnesyl transferase inhibitors (FTIs) like SCH 66336 show promise in preclinical cancer models. Further studies are needed to guide clinical development of these novel antitumor agents.

Area of Science:

  • Oncology
  • Pharmacology

Background:

  • Farnesyl transferase inhibitors (FTIs) are a novel class of anticancer agents.
  • SCH 66336 is a lead FTI identified through in vivo evaluation.

Purpose of the Study:

  • To evaluate the preclinical efficacy of FTIs, including SCH 66336.
  • To explore the potential of FTIs as single agents and in combination therapy for various human cancers.

Main Methods:

  • In vivo evaluation of SCH 66336 and other FTIs in preclinical cancer models.
  • Assessment of FTIs as single agents and in combination with cytotoxic chemotherapy.

Main Results:

  • Preclinical studies suggest FTIs may be effective against a broad spectrum of human cancers.
  • Tumor regression was observed in some cases with FTI monotherapy.
  • Combination therapy with cytotoxic agents showed enhanced efficacy in animal models.

Conclusions:

  • FTIs, including SCH 66336, demonstrate potential as antitumor agents for diverse cancers.
  • Combination strategies may improve the clinical efficacy of FPT inhibitors.
  • Further preclinical research is crucial for guiding the clinical development of FTIs.