In conclusion, we unveiled the post-squalenic enzyme OSC as a crucial target to inhibit tumor angiogenesis, halt metastatic dissemination, normalize the vasculature and, consequently, enhance the efficacy of chemotherapeutic drugs, assigning to Ro 48-8071, its specific inhibitor, the role of potential novel anti-angiogenic and anti-metastatic drug. The gene discussed is LSS; the disease is neoplasm.