FTI-2148 diTFA, a dual inhibitor targeting both farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1), functions as a RAS C-terminal mimetic. It exhibits potent inhibitory capabilities with IC50 values of 1.4 nM for FT-1 and 1.7 μM for GGT-1, respectively.

GGT1:1.7 μM , FT-1:1.4 nM

FTI-2148 diTFA is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC50 values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I.FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells.

FTI-2148 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model. FTI-2148 (subcutaneous injection; 100 mg/kg/day; 4 days) results in 85–88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo settings.FTI-2148 (intraperitoneal injection;?25 or 50 mpk/day with a mini-pump;?started on day 15 and stopped on day 45 and restarted day 53-83) inhibits the tumor growth by 91% in human lung adenocarcinoma A-549 cells induced mouse model.?FTI-2148 (subcutaneous injection;?25 mpk/day with a mini-pump;?14 days) inhibits tumor growth by 77%by the end of the 2-week treatment in Human Xenograft Nude Mouse Model.