Lexibulin (CYT997) is primarily investigated for its potential as an anticancer agent due to its ability to disrupt microtubule dynamics in rapidly dividing cells. It functions as a microtubule-destabilizing compound, inhibiting tubulin polymerization, which leads to cell cycle arrest and apoptosis in tumor cells. This mechanism makes it a candidate for treating various solid tumors, including those resistant to other chemotherapeutic agents. It has shown promising activity in preclinical models against cancers such as non-small cell lung cancer, prostate cancer, and glioblastoma. Its ability to cross the blood-brain barrier enhances its potential for treating brain tumors and central nervous system metastases. Lexibulin is also being explored for its anti-angiogenic properties, meaning it may help prevent the formation of new blood vessels that support tumor growth. Due to its potent cytotoxic effects and unique pharmacological profile, it has been evaluated in early-phase clinical trials to assess safety, dosing, and efficacy in advanced cancer patients.