Given its role in cancer progression, targeting the CXCL12/CXCR4 axis offers a promising therapeutic strategy. Several therapeutic agents and inhibitors are in development or clinical trials, aiming to block the interaction between CXCL12 and CXCR4. These include small molecule inhibitors, monoclonal antibodies, and peptide antagonists. By disrupting this axis, these therapies seek to inhibit tumor growth, reduce metastasis, and potentially enhance the efficacy of other cancer treatments.