Chemotherapy is a major therapeutic approach for malignant neoplasms; however, due to the mostcommon adverse events of nausea and vomiting, scheduled chemotherapeutic programs may be impeded oreven interrupted, which severely impairs the efficacy. Aprepitants, 5-HT3 antagonists and dexamethasone areprimary drugs used to prevent chemotherapy-induced nausea and vomiting (CINV). These drugs have excellentefficacy for control of acute vomiting but are relatively ineffective for delayed vomiting. Aprepitant may remedythis deficiency. Substance P was discovered in the 1930s and its association with vomiting was confirmed in the1950s. This was followed by a period of non-peptide neurokinin-1 (NK-1) receptor antagonist synthesis andinvestigation in preclinical studies and clinical trials (phases Ⅰ, Ⅱ and Ⅲ). The FDA granted permission for theclinical chemotherapeutic use of aprepitant in 2003. At present, the combined use of aprepitant, 5-HT3 antagonistsand dexamethasone satisfactorily controls vomiting but not nausea. Therefore, new therapeutic approaches anddrugs are still needed.