Farnesyltransferase inhibitors (FTIs) are a new class of biologically active agents originally developed as potential anticancer drugs, and are currently unavailable in Australia.
FTIs inhibit the enzyme farnesyltransferase, preventing the farnesylation and hence activation of a wide range of target proteins, including Ras (which is mutated in 30 % of all human cancers), ultimately resulting in cell growth arrest. In preclinical models, farnesyl transferase inhibitors showed great potency as a novel anti-cancer agent; yet in clinical studies, the early potential of FTIs were not realised.
This was attributed to several reasons: the molecular pharmacology and biology of FTIs had not yet been fully elucidated, an escape mechanism for the inhibition by FTIs was discovered (known as geranylgeranylation) and a well-defined proof of the concept of clinical studies was lacking.
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Editor: Assoc. Prof. Chris Alderman, University of South Australia – Director of Pharmacy, RGH © Pharmacy Department, Repatriation General Hospital, Daw Park, South Australia 5041.