Ginsenoside Rh2 (G-Rh2), a rare saponin derived from the traditional medicinal herb Panax ginseng, is recognized as one of its most potent bioactive components. It exhibits diverse pharmacological properties, including anti-inflammatory, antibacterial, anti-allergic, cardioprotective, immunoregulatory, and neuroprotective effects, underscoring its considerable therapeutic potential. Preclinical studies have demonstrated that G-Rh2 exerts its anti-tumor activity through multiple mechanisms, such as inhibiting proliferation, inducing apoptosis, regulating autophagy, suppressing metastasis, modulating epigenetic and metabolic profiles, enhancing immunity, and reversing multidrug resistance. It also demonstrates efficacy in ameliorating adverse reactions induced by chemotherapy or radiotherapy. This review systematically summarizes the anti-tumor mechanisms of G-Rh2 across various cancer types and discusses relevant combination therapy strategies. We also outline recent advances in drug delivery systems designed to improve its pharmacokinetic profile and anti-tumor efficacy, aiming to provide new insights and potential targets for tumor treatment.