Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a tubulin-binding microtubule polymerization inhibitor that targets the colchicine-binding site. By inducing tubulin depolymerization, Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway and leads to the deactivation of AKT. It possesses both anti-tumor and anti-vascular properties.
Combretol has leishmanicidal activity, it showed moderate activity (growth inhibition 87.3 and 73.0 %, respectively, at 50 μM) against a multidrug-resistant L. tropica line. Combretol also shows weakly active cytotoxic activity.
MC-Val-Cit-PAB-Retapamulin is a drug-linker conjugate for antibody-drug conjugates (ADC) that exhibits potent antitumor activity. This compound utilizes Retapamulin, a ribosome inhibitor, connected through the ADC linker MC-Val-Cit-PAB.