This integrative pharmacology-based investigation combining iTRAQ-coupled 2-D LC-MS/MS analysis and network investigation revealed that the anti-NPC effects of RO might relate to its regulatory effects on the PI3K-AKT signaling pathway, the Wnt signaling pathway, and the cAMP signaling pathway by targeting VEGFA, TP53, and HSPA8, which could improve our understanding of NPC during deciphering the mechanism of NPC treatments in response to RO. The gene discussed is HSPA8; the disease is nasopharyngeal carcinoma.