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An orally active diketopiperazine derivative with potential antineoplastic activity. Plinabulin selectively binds to the colchicine-binding site of tubulin, thereby interrupting equilibrium of microtubule dynamics; mitotic spindle assembly is disrupted, resulting in cell cycle arrest at the M phase and blockage of cell division in tumor cells. In addition, this agent induces tubulin depolymerization in vascular endothelial cells, resulting in the disruption of tumor blood vessel architecture and a selective collapse of tumor vasculature. Check for active clinical trials using this agent. (NCI Thesaurus)