Given its significant role in cancer progression, CXCR2 is considered a promising therapeutic target. Several strategies are being explored to inhibit CXCR2 signaling, including small molecule inhibitors, monoclonal antibodies, and RNA interference. Preclinical studies have shown that blocking CXCR2 can reduce tumor growth, angiogenesis, and metastasis, as well as enhance the efficacy of existing therapies like chemotherapy and immunotherapy.