lisavanbulin

Lisavanbulin is an orally available, highly water-soluble lysine prodrug of avanbulin (BAL27862), a synthetic small molecule with potential antitumor activity. Upon administration, lisavanbulin is converted to its active form, which binds to the colchicine site on tubulin—a site distinct from those targeted by vinca alkaloids and taxanes—preventing tubulin polymerization and destabilizing microtubules. This leads to cell cycle arrest at the G2/M phase, activation of the spindle assembly checkpoint, blockage of cell division, and induction of tumor cell death. In addition to directly targeting tumor cells, lisavanbulin also disrupts tumor vasculature. It has demonstrated preclinical and early clinical activity in glioblastoma—including MGMT promoter unmethylated models—and in platinum-resistant or refractory ovarian cancer. The drug can be administered orally or intravenously and crosses the blood-brain barrier[1][4][5][6][8].

Other names

1263384-43-5Lisavanbulin [INN]Lisavanbulin [USAN]