Saikosaponin A (SSA), the primary active monomer derived from the Radix bupleuri, demonstrates a diverse array of pharmacological activities, including anti-inflammatory, antitumor, analgesic, anti-fibrotic, antidepressant, and immune-modulating properties. Despite its potential therapeutic impact on various human diseases, comprehensive studies exploring SSA's efficacy in these contexts remain limited. This review synthesizes the current research landscape regarding SSA's therapeutic applications across different diseases, highlighting critical insights to overcome existing limitations and clinical challenges. The findings underscore the importance of further investigations into SSA's mechanisms of action, facilitating the development of targeted therapeutic strategies and their translation into clinical practice.