In this perspective, we provide a broad overview of pathophysiological processes involved in endometriosis, including the role of inflammation, fibrosis, angiogenesis, hormonal regulation, and genetic factors. For each of the functional changes involved with the etiology of the disease, we showcase a selection of active principles in various stages of preclinical and clinical development. Finally, we highlight the role of drug delivery for endometriosis, particularly oral vs. vaginal administration. In doing so, we wish to draw the community's attention to this debilitating disease and highlight the need for interdisciplinary approaches to endometriosis treatment development.