Peach kernel, a dual-purpose food and medicinal material, is rich in nutrients and bioactive components with complex mechanisms of action. It contains unsaturated fatty acids, proteins, flavonoids, phenylpropanoids, and cyanogenic glycosides, which confer anticoagulant, antiatherosclerotic, antioxidant, and antitumor activities. However, peach kernels also contain amygdalin. Despite possessing bioactivity, this component exhibits toxicity and bitterness, restricting the extensive application of peach kernels in the food industry. This review systematically examines the main components and bioactivities of peach kernels, discusses amygdalin toxicity and removal methods, and highlights advances in detoxification and debittering using traditional processing methods and modern technologies (e.g., ultrasound, fermentation, and microwave). The goal is to provide a basis for the deep processing and application of peach kernels, promoting their innovative use in functional foods.