Kuding tea (KT), a traditional Chinese bitter tea, has long been recognized as Food & Medicine Homology product, known for its various active components and health benefits. However, research on KT is fragmented, lacking a comprehensive review of its key chemical constituents, health-promoting effects, and potential future applications. This review outlines the development history and nutritional components of KT while examining its functional benefits and industrial applications. KT is a promising and cost-effective product, containing numerous bioactive constituents, including polyphenols, triterpenoids, phenylethanoids, and polysaccharides, which exhibit strong antioxidant, anti-obesity, anti-diabetic, anti-inflammatory, neuroprotective, and anti-cancer activities. We summarized the researches on the health-promoting effects of KT and emphasized its practical applications in the food, agricultural, and pharmaceutical industries. Overall, this review presents a forward-looking viewpoint on creative KT applications and offers insights into KT's potential for future sustainable growth.