INTRODUCTION: Inhibitors targeting oncogenic kinases, especially receptor tyrosine kinases (RTKs), are being vigorously developed, and some have been demonstrated to be effective in clinical settings. The amplification of certain RTKs (ErbB2, c-Met and FGFR2) is associated with gastric cancer progression, but the only recently approved inhibitor is trastuzumab, ErbB2-targeting antibody. Other well-known oncogenic kinases (PI3K and RAF) are also activated in a small portion of gastric cancers. Drugs targeting these kinases are promising and should be approved in an appropriate and expeditious way. AREAS COVERED: This article reviews novel inhibitors emerging in the field of advanced gastric cancer, based on basic research concerning altered oncogenes and the clinical trials of drugs targeting these oncogenes. EXPERT OPINION: Promising inhibitors of gastric cancer may be found in not only new investigative agents but also agents currently being used against other malignancies. The appropriate design for clinical trials of molecularly targeted therapeutic agents is also important. Targeted therapies tailored to individual genomic profiles would provide a more personalized treatment for advanced gastric cancer.