Endometriosis is a disease in which the lining of the endometrium is found outside of the uterus. Recent medical treatments for endometriosis have adverse effects, limiting their long-term use. Furthermore, the recurrence of the disease after the cessation of therapy is quite common, and most patients need to continue treatment to maintain a hypoestrogenic environment till conception. Notwithstanding recent advances in computational and chemical practices, traditional medicines are considered the most consistent sources for the discovery of new drugs. Numerous medicinal plants and plant-derived compounds have been tested against gynecological disorders, mainly endometriosis. This review aimed to describe the pharmacological activity profile of the medicinal plants and their active ingredients and draw attention to the discovery of multitargeted drug molecules for rational therapy.