Pseudostellaria heterophylla, a dual-purpose medicinal and edible herb, has shown significant pharmacological potential, particularly through its immunomodulatory and antitumor activities. This review provides insights into the phytohormone regulatory mechanisms and active-component biosynthesis, highlighting key metabolic pathways and yield-optimization strategies. The interactions between hormones and genes in root morphology and metabolite accumulation are discussed, offering new perspectives for molecular breeding. Additionally, a multidisciplinary framework is proposed to address cultivation challenges and quality enhancement, laying the groundwork for sustainable utilization of this valuable medicinal plant.