Inhibitors of the enzyme farnesyl protein transferase prevent a key step in
the post-translational processing of the Ras protein, and were developed i
nitially as a therapeutic strategy to inhibit cell signalling in ras-transf
ormed cells. As more has been learnt about the biological effects of farnes
yl transferase inhibitors (FTIs) on cancer cells, it is clear that tumours
without oncogenic ras mutations such as breast cancer may also be targets f
or FTI therapy. This article reviews the rationale for the development of F
TIs, focussing on early preclinical data in breast cancer models together w
ith preliminary results from the first phase II study of an FTI in advanced
breast cancer.