PLINABULIN Tubulin Polymerization Inhibitor Vascular-Disrupting Agent Oncolytic

Vascular-disrupting agents (VDAs) are a new class of compounds that target tumor vasculature, causing a rapid and acute collapse of the blood vessel network surrounding the tumor, slowing blood flow and ultimately resulting in tumor necrosis. Plinabulin is a small-molecule VDA that works by selectively binding to the colchicine binding site of endothelial tubulin, leading to disorganization of the endothelial cytoskeleton and inhibition of tumor blood flow. Clinical studies have shown that plinabulin markedly reduces tumor blood flow, providing significant clinical benefit to patients with solid tumors. Further results in patients with non-small cell lung cancer (NSCLC) demonstrated that plinabulin enhanced the antitumor activity of docetaxel, with a favorable safety profile. Plinabulin is currently undergoing phase I clinical studies as monotherapy for the treatment of solid tumors and lymphoma and phase II evaluation in combination with docetaxel for the treatment of NSCLC.