Allergic diseases have become global social health problems.  The binding of IgE with its high affinity receptor FcεRI plays a key step in I-type allergy.  Recently, more and more key molecules on the IgE/FcεRI signaling transduction pathway were to be the drug candidates against allergic diseases, with in-depth study of FcεRI signal pathway gradually.  The main drugs include molecule antibodies, peptides, vaccines, fusion proteins, small molecules, and other drugs related to IgE/FcεRI.  The recent progress in the study of mechanisms of representative drugs targeting on IgE/FcεRI signaling pathway was reviewed in this article.