Abstract: Macrophage colony stimulating factor receptor (c-Fms), the product encoded by proto-oncogene fms, is a type Ⅲ receptor tyrosine kinase. c-Fms and its ligand CSF-1 play important roles in the proliferation, growth and differentiation of tumor-associated macrophages. c-Fms is abnormally expressed in a variety of malignant and inflammatory diseases. The CSF-1/c-Fms axis might be an effective approach to the treatment of malignant tumors. Many small molecular inhibitors targeting c-Fms are under research and clinical development. This article describes the mechanisms of c-Fms and its roles in tumor immunotherapy, and reviews the latest research progress in small-molecule inhibitors of c-Fms, so as to provide reference for follow-up studies.