Drug intelligence / Profile preview

RBF197

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Rectal, Topical, Subcutaneous, Intramuscular, Intravenous, Transdermal, Inhalation, Intranasal, Intravaginal, Ophthalmic, Intraaural, Intracerebral, Sublingual, Buccal, Intra-arterial
01

Overview

RBF197 is a novel, highly potent, and selective small molecule inhibitor of eukaryotic initiation factor 4A (eIF4A), specifically targeting eIF4A1 with an IC50 of 55.2 pM against human eIF4A helicase activity. It functions by clamping eIF4A onto mRNA in an ATP-independent manner, thereby inhibiting cap-dependent translation and suppressing eIF4A-dependent oncogene expression. RBF197 demonstrates strong anti-tumor activity in diffuse large B-cell lymphoma (DLBCL) models, including ABC-DLBCL and double-hit lymphoma cell lines, reducing cell viability, proliferation, overall translation, colony formation, and key pathway proteins like MYC and MCL1, with EC50 values below 10 µM and minimal impact on non-malignant cells.[1][2][3][4][5]

02

Targets

EIF4A1 (Eukaryotic translation initiation factor 4A1)EIF4A2 (Eukaryotic translation initiation factor 4A2)

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