The standard treatment for epithelial ovarian cancer remains surgical debulking and chemotherapy with carboplatin and paclitaxel. However, the majority of patients relapse, and few, if any, achieve a cure. Future advancement in treatment should aim at targeting the biology of the disease, specifically mechanisms critical to tumor initiation and progression. Several Phase I and II clinical trials have identified novel opportunities for therapy. The most promising venues appear to be the antiangiogenic agents and the inhibitors of intracellular signaling. Novel modalities of delivering cytotoxics to tumor cells by exploiting ovarian cancer-specific biomarkers are also being tested, and appear promising. Immunomodulatory agents are being developed for consolidation therapy. Although devoid of the common side effects associated with chemotherapy, the use of targeted agents is associated with specific toxicities, related to the biological processes they block. The main challenge for future successful clinical development will be defining molecular markers predictive of response and judicious patient selection based on the biological features of the tumor. Individualized treatment driven by molecular characteristics will open the door to a new age in anticancer medicine.