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Farnesyltransferase inhibitors
S M Hahn1, E Bernhard, W G McKenna
1Department of Radiation Oncology, Hospital of the University of Pennsylvania, Philadelphia, PA 19104-4283, USA.
Seminars in Oncology
|November 14, 2001
Summary
Targeting Ras protein farnesylation with farnesyltransferase inhibitors (FTIs) is a novel cancer therapy strategy. Clinical trials are evaluating FTIs for improved cancer treatment selectivity and patient selection.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Targeting molecular abnormalities in neoplasms can enhance cancer therapy selectivity.
- Ras mutations are frequent in human cancers, and other genetic changes can activate ras-dependent pathways.
- Inhibiting Ras protein farnesylation is an emerging cancer treatment strategy.
Purpose of the Study:
- To evaluate farnesyltransferase inhibitors (FTIs) as a novel cancer treatment strategy.
- To determine the toxicity and maximally tolerated doses of FTIs.
- To develop assays for measuring FTI biological effects and improve patient selection.
Main Methods:
- Clinical evaluation of several FTIs in Phase I trials.
- Assessment of FTI toxicity and maximally tolerated doses.
- Investigation of surrogate markers for farnesylation inhibition.
Main Results:
- Several FTIs have undergone Phase I clinical trials.
- Toxicity and maximally tolerated doses for multiple FTIs have been established.
- Ongoing research focuses on developing assays to measure biological effects.
Conclusions:
- Farnesyltransferase inhibitors represent a promising targeted cancer therapy.
- Further research is needed to elucidate FTI mechanisms of action and optimize patient selection for clinical trials.