Tubulysin I is primarily investigated for its potent anticancer properties. It functions by disrupting microtubule dynamics, which are essential for cell division, making it highly effective in inhibiting the growth of cancer cells. Due to its mechanism of action, it is being explored as a potential component in targeted cancer therapies, particularly for tumors that are resistant to conventional treatments. Researchers are also studying its use in antibody-drug conjugates (ADCs), where it can be delivered directly to cancer cells, minimizing damage to healthy tissues. Additionally, its strong cytotoxic activity has sparked interest in developing derivatives with improved efficacy and reduced toxicity for broader therapeutic applications.