Zotatifin (eFT226) is a selective eIF4A inhibitor with antiviral and anticancer activities, blocking tumor growth driven by receptor tyrosine kinases and inhibiting Sox4 translation, inducing apoptosis.

eIF4A:2 nM

Methods: Zotatifin (0.0001 μM-1 μM, 72 hours) was used to treat MDA-MB-231 cells, and the antiproliferative activity was determined.
Results: Zotatifin showed potent antiproliferative activity in MDA-MB-231 tumor cells, with a GI50 value of less than 15 nM.
TMD8 and Pfeiffer DLBCL tumor cells were treated with Zotatifin (30 μM-100 μM, 3 or 24 hours), and the changes in protein levels were detected by WB.
Results: Zotatifin reduced the expression of MYC, CCND3, BCL2, and MCL1 proteins in a time- and dose-dependent manner.[1]

Methods: Zotatifin (1 mg/kg, intravenous injection, 14-22 days) was used to treat mice bearing TMD8 xenografts, HBL1 xenografts, Pfeiffer xenografts, SU-DHL-6 xenografts, SU-DHL-10 xenografts, and Ramos xenografts, and the tumor inhibition rate was observed.
Results: The tumor growth percentages of various tumor xenograft model mice after Zotatifin treatment were 97%, 87%, 70%, 83%, 37%, and 75%, respectively.
Methods: Zotatifin (0.001 mg/kg-1 mg/kg, intravenous injection; 15 days) was used to treat mice bearing B-cell lymphoma xenograft models, and the tumor growth in vivo was observed.
Results: Zotatifin inhibited the growth of B-cell lymphoma xenografts and was well tolerated in B-cell lymphoma xenograft models in vivo.[2]