STATs constitute a large family of transcription activators and transducers of signals that have an important role in many cell functions as regulation of proliferation and differentiation of the cell also regulation of apoptosis and angiogenesis. STAT3 as a member of that family, recently was discovered to have a vital role in progression of different types of cancers. The activation of STAT3 was observed to regulate multiple gene functions during cancer-like cell proliferation, differentiation, apoptosis, metastasis, inflammation, immunity, cell survival, and angiogenesis. The inhibition of STAT3 activation has been an important target for cancer therapy. Inhibitors of STAT3 have been used for a long time for treatment of many types of cancers like leukemia, melanoma, colon, and renal cancer. In this review article, we summarize and discuss different drugs inhibiting the action of STAT3 and used in treatment of different types of cancer.