KGP265

KGP265 is a water-soluble, benzosuberene-based phosphate prodrug of KGP18, a potent tubulin-binding agent and vascular disrupting agent (VDA) structurally inspired by the natural product combretastatin A-4 (CA4). Upon administration, KGP265 is rapidly dephosphorylated by endogenous alkaline phosphatases to release the active parent compound, KGP18. KGP18 binds to the colchicine binding site of tubulin, inhibiting tubulin polymerization and disrupting the microtubule cytoskeleton of tumor endothelial cells. This leads to endothelial cell rounding, blebbing, and detachment, culminating in selective tumor vascular shutdown, hemorrhage, and necrosis. KGP265 has demonstrated significant antitumor and vascular-disrupting efficacy in preclinical models of breast and kidney cancers, both as a monotherapy and in combination with chemotherapeutic agents like carboplatin.

Other names

KGP18 phosphateKGP-18 phosphateKGP 18 phosphateKGP18 phosphate prodrugKGP-18 phosphate prodrugKGP 18 phosphate prodrugKGP18 prodrugKGP-18 prodrugKGP 18 prodrug