plinabulin

Plinabulin is an orally active small molecule and a member of the 2,5-diketopiperazine class with potent antineoplastic and immunomodulatory activity. It acts as a selective immunomodulating microtubule-binding agent (SIMBA), binding reversibly to the colchicine-binding site of β-tubulin in αβ-tubulin heterodimers, thereby disrupting microtubule dynamics. This disruption leads to mitotic spindle assembly inhibition, cell cycle arrest at M phase, and blockage of cell division. Plinabulin also induces dendritic cell maturation via release of GEF-H1, enhancing both innate and adaptive immune responses through increased antigen presentation and T-cell activation. Additionally, it has vascular disrupting properties that inhibit tumor vasculature function. Plinabulin is being developed primarily for prevention of chemotherapy-induced neutropenia (CIN) in combination with granulocyte colony-stimulating factor (G-CSF), as well as for treatment of non-small cell lung cancer (NSCLC).

Other names

plinabulinaplinabuline