Abstract: Chemotherapy-induced nausea and vomiting （CINV） is one of the most common adverse events for patients undergoing chemotherapy. Severe nausea and vomiting can cause malnutrition and disturbance of water and electrolyte which may have a negative effect on patients’ quality of life and adherence to chemotherapy. 5-hydroxytryptamine 3 receptor （5-HT3） antagonists are included in the National Comprehensive Cancer Network guidelines as first-line option in the preventive antiemetic therapy. Granisetron transdermal system is the first antiemetic 5-HT3 antagonist available in a transdermal formulation. A number of pre-clinical studies have demonstrated that granisetron transdermal system is not inferior to oral granisetron. Besides it can steadily control CINV for up to 7 days. In this paper，we reviewed the progress in researches from the aspects of pharmacokinetics and clinical application of granisetron transdermal system.