RO5323441

RO5323441 (also known as RG7426) is a small molecule multi-kinase inhibitor developed by Hoffmann-La Roche. It specifically targets the vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3) and the Tie2 (TEK) receptor tyrosine kinase. These receptors are critical mediators of angiogenesis and lymphangiogenesis, processes that tumors exploit to establish a blood supply and metastasize. By inhibiting these pathways, RO5323441 aims to reduce tumor vascularization and inhibit growth. It was evaluated in Phase 1 clinical trials for metastatic treatment-refractory colorectal and ovarian cancers, where dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) was used as a biomarker to assess its impact on tumor blood flow and permeability. Development of the compound appears to have been discontinued following the completion of early-phase exploratory studies.