A leading cause of death worldwide, breast cancer is the second most prevalent cancer in women. Triple-negative breast cancer is an aggressive subtype that lacks targeted therapies and requires novel therapeutic approaches in clinical practice to improve the overall survival. Theranostic agents that integrate diagnostic and therapeutic capabilities in a single entity are promising strategies for personalized cancer management. Hybrid compounds combining biologically relevant moieties with different modes of action can enhance cytotoxicity and improve pharmacological properties. We focus on a hybrid containing coumarin, triazole, and [10]-gingerol, a compound with known antimetastatic potential in TNBC. The LSPN281 hybrid exhibited superior cytotoxic activity in a TNBC cell line compared to the individual coumarin and [10]-gingerol controls. Additionally, the hybrid shows enhanced cellular uptake and mitochondrial localization, suggesting its potential as a theranostic agent for TNBC.