Tipifarnib in the treatment of acute myeloid leukemia
Authors Xavier Thomas, Mohamed Elhamri
Published 15 February 2008 Volume 2007:1(4) Pages 415—424
Xavier Thomas, Mohamed Elhamri
Hematology, Edouard Herriot Hospital, Lyon, France
Abstract: Farnesyltransferase inhibitors (FTIs) are a new class of biologically active anticancer drugs. The exact anti-tumorigenic mechanism is currently unknown. FTIs inhibit farnesylation of a wide range of target proteins. In preclinical models, tipifarnib (R115777, Zarnestra®), a non-peptidomimetic competitive FTI, showed great potency against leukemic cells. Although it has recently demonstrated clinical responses in adults with refractory and relapsed acute myeloid leukemia (AML), and in older adults with newly diagnosed poor-risk AML, its activity was far less than anticipated. However, it appears that tipifarnib as a single agent may be important in selected groups of patients. Much remains to be learned to optimize such therapy in patients with AML. To this end, trials that combine tipifarnib with cytotoxics are ongoing.
Keywords: tipifarnib, farnesyltransferase inhibitor, acute myeloid leukemia, prognosis, targeted therapy