Importance: Irrespective of the precise mechanisms leading to endometriosis, angiogenesis is essential for the establishment and long-term proliferation of the disease. As current surgical and medical management options for women with endometriosis have substantial drawbacks and limitations, novel agents are needed and molecules targeting the angiogenic cascade could serve as potential candidates.Objective: Our aim was to review current data about the role of angiogenesis in the pathophysiology of endometriosis and summarize the novel antiangiogenic agents that could be potentially used in clinical management of patients with endometriosis.Evidence Acquisition: Original research and review articles were retrieved through a computerized literature search.Results: Loss of balance between angiogenic activators and suppressors triggers the nonphysiological angiogenesis observed in endometriotic lesions. Several proangiogenic mediators have been identified and most of them have demonstrated increased concentrations in the peritoneal fluid and/or serum of women with endometriosis. Among the antiangiogenic molecules, anti-vascular endothelial growth factor agents, dopamine agonists, romidepsin, and statins have shown the most promising results so far.Conclusions and Relevance: Given the limitations of current treatments of endometriosis, there is a need for novel, more efficient agents. Antiangiogenic molecules could be used potentially in clinical management of women with endometriosis; however, their safety and efficiency should be carefully assessed prior to that. Further large prospective trials in humans are needed before any treatment is introduced into daily clinical practice.Target Audience: Obstetricians and gynecologists, family physicians Learning Objectives: After participating in this activity, physicians should be better able to summarize current knowledge about the role of proangiogenic and antiangiogenic mediators in the development of endometriosis; outline the main antiangiogenic agents that are under investigation; and describe their effect on the angiogenic mediators of endometriosis.Endometriosis is a benign disorder characterized by the presence of endometrial tissue (glandular epithelium and stroma) outside the uterine cavity, mainly in the pelvic peritoneum, the ovaries, the torus uterinus, the uterosacral ligaments, and the rectovaginal septum. 1 This functional endometrial tissue triggers a chronic inflammatory response, resulting in peritoneal fibrosis, formation of adhesions, and, subsequently, development of chronic pelvic All authors, faculty, and staff in a position to control the content of this CME activity and their spouses/life partners (if any) have disclosed that they have no financial relationships with, or financial interests in, any commercial organizations relevant to this educational activity.