Glioblastoma multiforme, is the most malignant glioma among other gliomas with high incidence. It has aggresive properties such as high proliferation, invasion and migration rates. Therefore, recently studies have focused on the development of new therapeutic targets in glioblastoma chemotherapy. Substance P, neurokinin-1 (SP/NK-1) receptor system has an important role in cancer development and metastasis. Therefore, NK-1 receptors are new therapeutic targets for glioblastoma therapy and development of NK-1 receptor antagonists. In this study, antiproliferative and apoptotic effects of aprepitant which is an antiemetic drug commonly using in chemotherapy on human U87MG glioblastoma cells were investigated. Antiproliferative effects of aprepitant were evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) and Real Time Analyses System (RTCA DP). Also apoptotic effects of aprepitant were evaluated by annexin-VPI and caspase-3 activity by using flow cytometer. According to the cell index values obtained from real-time cell analysis system, with 50 mu M and higher concentrations, cell proliferation was decreased and IC50 values were determined as 76.9, 62.5 and 59.2 mu M for 24, 48 and 72 hours respectively. Aprepitant showed significant antiproliferative effects on U87MG cells. Depending on increasing aprepitant concentrations, both early and late apoptotic cell ratios were increased. In addition, caspase-3 activation was slightly increased with IC25 and IC50 concentrations of aprepitant according to the control group. As a result, aprepitant showed important antiproliferative and apoptotic effects on U87MG cells. In conclusion, NK-1 receptor antagonists may have a potential therapeutic role for human glioblastoma chemotherapy.