Therapeutics in oncology are rapidly changing, with the advent of the so-called “targeted drugs.” A clear example is trastuzumab, an anti-HER2 monoclonal antibody, and its role in the treatment of breast cancer. Trastuzumab was followed by other monoclonal antibodies like cetuximab (anti-EGFR) and bevacizumab (anti-VEFG) and by tyrosine kinase inhibitors such as imatinib, gefitinib (anti-EGFR) and others. The complex biology of the cancer cell leads us to search combination strategies to act simultaneously in different points of signals transduction pathways to enhance the anticancer effect. Here we review various clinical trials and also experimental data exploring these new drugs in combination. Combination with chemotherapy is beyond the scope of this review. For this review, we have selected the following agents: cetuximab, trastuzumab, bevacizumab, panitumumab, imatinib, erlotinib, gefitinib, sorafenib, sunitinib, and lapatinib.