Tipifarnib (Zarnestra, R115777, IND 58359) is a farnesyltransferase inhibitor (IC50=0.6 nM) that is used in patients 65 years of age and older with newly diagnosed acute myeloid leukemia (AML). It is also being tested in clinical trials in patients in certain stages of breast cancer. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. |