Plinabulin (NPI-2358)

Mechanism of action

From the NCI Drug Dictionary: 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.

Preliminary data

Non-small cell lung cancer

1. Abstract: Ramon W. Mohanlal, Ken LLoyd, Lan Huang, Lyudmila Bazhenova. Plinabulin as a novel small molecule clinical stage immuno-oncology agent for NSCLC. J Clin Oncol 35, 2017 (suppl 7S; abstract 139) link to abstract