Lexibulin

**Lexibulin (CYT997)** is a synthetic small-molecule microtubule depolymerization inhibitor and vascular-disrupting agent (VDA) with potent preclinical antitumor activity across solid tumors (e.g., breast, prostate, colon), leukemias, glioblastoma, hepatocellular carcinoma (HCC), and acute myeloid leukemia (AML). Developed initially by Cytopia (later YM BioSciences), it binds tubulin to prevent microtubule polymerization, causing G2/M cell cycle arrest, apoptosis via caspase activation (extrinsic/intrinsic pathways), and tumor vasculature ablation, as evidenced by dynamic contrast-enhanced MRI changes, elevated von Willebrand factor, and caspase-cleaved cytokeratin-18. Orally bioavailable, it advanced to Phase I/II trials for advanced solid tumors and glioblastoma (with carboplatin), showing stable disease in 82% of Phase I patients, linear pharmacokinetics, reversible toxicities (e.g., QTc prolongation), and no peripheral neuropathy, with preclinical synergy potential alongside sorafenib or chemotherapy.[1][4][7][8]

Brand names

Lexibulin

Other names

SRI-32007SRI32007SRI 32007