Galectin-3 is a member of the galectin family, which are β-galactoside-binding lectins with ≥1 evolutionary conserved carbohydrate-recognition domain. It binds proteins in a carbohydrate-dependent and -independent manner. Galectin-3 is predominantly located in the cytoplasm; however, it shuttles into the nucleus and is secreted onto the cell surface and into biological fluids including serum and urine. It serves important functions in numerous biological activities including cell growth, apoptosis, pre-mRNA splicing, differentiation, transformation, angiogenesis, inflammation, fibrosis and host defense. Numerous previous studies have indicated that galectin-3 may be used as a diagnostic or prognostic biomarker for certain types of heart disease, kidney disease and cancer. With emerging evidence to support the function and application of galectin-3, the current review aims to summarize the latest literature regarding the biomarker characteristics and potential therapeutic application of galectin-3 in associated diseases.