J-L. Harousseau Tipifarnib in hematologic malignancies

Farnesyltranferase inhibitors (FTI) are signal transduction inhibitors that block farnesylation of a number of proteins including Ras that are involved in key cellular functions (proliferation,survival and differentiation).1,2 Tipifarnib is a potent inhibitor of farnesyltransferase that is orally bioavailable. Tipifarnib was initially developed with the goal of targeting Ras in cancers with a high incidence of Ras mutations. However, after failure of large clinical trials in solid tumors (pancreas, colon) further development was mainly focused on hematologic malignancies