MBQ-168

MBQ-168 is a small molecule dual inhibitor of the Rho GTPases Rac and Cdc42, currently in preclinical development by MBQ Pharma for the treatment of various cancers (pan-cancer). As a derivative of MBQ-167, it features a 9-ethyl-3-(1H-1,2,3-triazol-1-yl)-9H-carbazole core and acts by interfering with guanine nucleotide binding, which prevents the activation of downstream effectors like P21-activated kinases (PAK1-3). MBQ-168 has demonstrated significant efficacy in preclinical models of HER2-positive breast cancer, specifically inhibiting tumor growth and metastasis to the lungs, liver, and spleen. Notably, it exhibits approximately 10-fold less potency against CYP3A4 compared to its predecessor MBQ-167, suggesting a more favorable profile for potential combination therapy regimens.