FTI-2148

FTI-2148 is a selective small molecule farnesyltransferase inhibitor (FTI) developed for the treatment of KRas-mutant cancers. It functions by inhibiting the enzyme farnesyltransferase, which is responsible for the post-translational farnesylation of Ras proteins, a step necessary for their membrane localization and subsequent oncogenic signaling activity. While effective at inhibiting farnesylation, FTI-2148 and similar selective FTIs often face resistance in KRas-driven tumors because KRas can undergo alternative prenylation by geranylgeranyltransferase-1 (GGT-1). Consequently, FTI-2148 is frequently utilized in preclinical research to evaluate the efficacy of Ras-targeting strategies and to compare selective inhibition against dual farnesyl/geranylgeranyltransferase inhibitors.