With a growing public emphasis on oral health, efficacy-focused toothpastes have become mainstream. By combining chemical active ingredients with mechanical cleaning, these products deliver multifunctional benefits, such as caries prevention, dentin hypersensitivity relief, whitening, and anti-inflammation. This article systematically reviews recent advances in key efficacious ingredients across four functional domains: fluoride, often supplemented with calcium-phosphorus compounds, probiotics, and herbal preparations, primarily prevents caries; antibacterial and anti-inflammatory effects arise from multi-ingredient synergy; anti-hypersensitivity works via physical occlusion and nerve inhibition, with herbal extracts as natural alternatives; and whitening involves mechanical abrasion, chemical action, and optical modification. However, current research remains fragmented and repetitive, lacking a systematic evidence base. This complicates evidence-based consumer choice, while studies on precision and personalized formulations are still limited. Future efforts should establish comprehensive efficacy evaluation systems, investigate multi-component synergies, and advance precision toothpaste development tailored to individual oral microbiomes and needs. By summarizing ingredients, mechanisms, efficacy, and safety elements, this review aims to support optimized toothpaste formulation and clinical application, thereby contributing to oral healthcare precision.