Indibulin (ZIO 301) is primarily investigated for its potential as an anticancer agent, specifically as a microtubule-targeting compound. It functions by inhibiting tubulin polymerization, which disrupts the formation of the mitotic spindle during cell division, leading to cell cycle arrest and apoptosis in rapidly dividing cancer cells. This mechanism is similar to other tubulin inhibitors but with a distinct pharmacological profile that may offer advantages in terms of reduced neurotoxicity and improved oral bioavailability. It has shown activity in preclinical studies against various solid tumors, including breast, prostate, and lung cancers. Notably, Indibulin retains efficacy in multidrug-resistant cancer models, making it a candidate of interest for overcoming resistance to conventional chemotherapeutics like taxanes and vinca alkaloids. Its oral administration route further enhances its potential for convenient, long-term treatment regimens in outpatient settings. Clinical development has focused on evaluating its safety and effectiveness both as a monotherapy and in combination with other anticancer drugs. Ongoing research aims to identify optimal dosing schedules and patient populations most likely to benefit from treatment.