OBJECTIVES: Cancer therapy has been revolutionized by the introduction of targeted therapy. Tremendous growth of its utilization was observed in Singapore over the past decade. Despite high treatment cost, most of the targeted therapies were not funded by Singapore’s unique healthcare financing system. Hence, this study aims to determine the trends of use of targeted therapy in National Cancer Centre Singapore from 2007-2011. In addition, treatment response and economic evaluation of Gefitinib as a first line therapy for advanced NSCLC will be conducted to aid decision making. METHODS: In this retrospective study, number of patients and annual consumption costs for each targeted therapy were determined. A total of 124 chemo naive patients were identified to examine treatment response and resources used for Gefitinib. These were reviewed via electronic databases and medical reports. A Markov model was developed by using patient level data and utility values from literature. Cost utility analysis was performed from healthcare provider’s perspective with inclusion of direct medical costs (2012 Singapore dollars) and discount rate of 3%. RESULTS: Dominant trends were observed in utilization of Trastuzumab (35%), Gefitinib (25%) and Bevacizumab (12%) over last 5 years. For Gefitinib, partial response and stable disease were 23.4% and 64.5% respectively. It resulted in a gain of 73.23 progression free days and 2.87 quality adjusted life year (QALY) with an additional cost of S$30,819.28. As a result, incremental cost-utility ratio (ICUR) of Gefitinib is S$10,749.86 per QALY and it was most sensitive to the cost of Gefitinib in one way sensitivity analysis. CONCLUSIONS: Top three drugs with high utilization and consumption costs were Trastuzumab, Gefitinib and Bevacizumab. If the acceptable ICUR threshold in Singapore is 1 to 3 times of gross domestic product range, Gefitinib can be considered cost-effective compared to chemotherapy as first line treatment of NSCLC for local population.