Used in targeted cancer therapies, it functions as a prodrug linker in antibody-drug conjugates (ADCs). It enables the selective delivery of potent cytotoxic agents, such as Indibulin, to cancer cells while minimizing damage to healthy tissues. The Val-Cit dipeptide sequence is cleaved by cathepsin B, an enzyme overexpressed in many tumors, releasing the active drug specifically at the tumor site. This targeted approach enhances the efficacy of chemotherapy and reduces systemic side effects. It is particularly valuable in treating cancers with high cathepsin B activity, such as certain types of breast, lung, and colorectal cancers.