G3-CA4

G3-CA4 (nanocombretastatin) is a nanoparticle-based vascular disrupting agent (VDA) consisting of combretastatin A4 (CA4) conjugated to a third-generation (G3) succinimic acid-functionalized poly(amidoamine) (PAMAM) dendrimer. CA4 is a potent tubulin-binding agent that destabilizes the microtubule cytoskeleton of endothelial cells, leading to the rapid collapse of tumor vasculature and subsequent tumor necrosis. By conjugating the water-insoluble CA4 to a water-soluble dendrimer, the formulation overcomes the poor solubility of free CA4 and enhances intratumoral delivery, particularly across the compromised blood-brain tumor barrier. In preclinical models of glioblastoma (e.g., U-251 glioma), G3-CA4 has demonstrated superior efficacy compared to free CA4 in reducing tumor perfusion and inducing central necrosis, as measured by non-invasive MRI biomarkers.

Other names

nanocombretastatinG3-succinimic acid PAMAM dendrimer-combretastatin A4 conjugateG-3-succinimic acid PAMAM dendrimer-combretastatin A4 conjugateG 3-succinimic acid PAMAM dendrimer-combretastatin A4 conjugate