These studies fully demonstrate that BPRCX807, a highly selective, safe, and potent CXCR4 antagonist, possesses more in vitro and in vivo efficacy than its marketed counterpart AMD3100 under various HCC settings with supreme benefits on combination therapy, whereby it can significantly synergize with not only antiangiogenic therapy (sorafenib) but also immunotherapy (anti–PD-1) to further extend overall survival (Fig. 9). The gene discussed is CXCR4; the disease is hepatocellular carcinoma.