Abstract: Chemotherapy is the most important method for cancer treatment. However, side effects such as nausea and emesis cause fear among patients and weaken their body resistance. Therefore, effective antiemetics are indispensable during chemotherapy. At present, 5-HT3 and NK-1 receptor antagonists are mainly used as antiemetics. After aprepitant, the first NK-1 receptor antagonist, was authorized for use by the FDA, several NK-1 receptor antagonists have been marketed. As antiemetics, NK-1 receptor antagonists provide a more effective, economical, diversified, and safer choice for preventing and treating chemotherapy-induced nausea and vomiting (CINV). NK-1 receptor antagonists encourage compliance and prevent the unstable curative effect and intolerance to other antiemetics caused by CINV during chemotherapy. This review introduces the application of NK-1 receptor antagonists as antiemetics for cancer chemotherapy.