Farnesyltransferase inhibitors in Hutchinson-Gilford progeria – RGH Pharmacy E-Bulletin

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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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A joint initiative of the Patient Services Section and the Drug and Therapeutics Information Service of the Pharmacy Department, Repatriation General Hospital, Daw Park, South Australia. The RGH Pharmacy E-Bulletin is distributed in electronic format on a weekly basis, and aims to present concise, factual information on issues of current interest in therapeutics, drug safety and cost-effective use of medications.
Editor: Assoc. Prof. Chris Alderman, University of South Australia – Director of Pharmacy, RGH © Pharmacy Department, Repatriation General Hospital, Daw Park, South Australia 5041.

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