Buckwheat possesses remarkable nutritional and medicinal properties, making it a valuable crop for enhancing the food industry through nutrient-dense bakery, non-bakery, and fermented products. Its stress resilience, high flavonoid content, and potent antioxidant activity position it as a promising “smart food.” This study provides a comprehensive review of buckwheat’s breeding and genetic advancements, bioactive compounds, biological functions, and potential applications in food and pharmaceuticals. Identifying superior cultivars is crucial for developing gluten-free foods, beverages (such as tea, beer, and wine), and nutraceuticals. Rich in bioactive compounds, buckwheat exhibits antioxidant, antimicrobial, anti-glycemic, and anticancer properties, highlighting its therapeutic potential. This chapter summarizes current research on buckwheat’s role in human nutrition and health, along with future prospects for its utilization.