Small molecule inhibitors of tyrosine kinase activity and monoclonal antibodies are among the widely used drugs for targeted based cancer therapy, and bind to intracellular and cell-surface molecules. Chemotherapy has been used for cancer treatment for several decades and is based on the treatment with cytotoxic drugs that affect normal tissues with serious side effects that deteriorate patient’s life quality. The term “oncogenic addiction” was coined by Weinstein in 2000 and demonstrated that cancer cells might show addiction to an oncogenic signaling molecule or pathway to sustain tumor activity such as survival and proliferation. Vatalanib or PTK787 suppresses tumor angiogenesis and has been investigated for the treatment for various cancers. Tivozanib has displayed antitumor activity in human colon, ovarian, pancreas, liver, breast, prostate, and lung cancers as well as in brain xenografted models. Neratinib has been noted to have promising effects in non-small cell lung cancer and breast cancer, as described in preclinical studies.