Phytotherapy has long represented a widely accepted treatment alternative to conventional therapy. Bitter melon is a vine with potent antitumor effects against numerous cancer entities. To date, no review article has, however, been published on the role of bitter melon in breast and gynecological cancer prevention and therapy. The current work constitutes the most comprehensive, up-to-date review of the literature, which highlights the promising anticancer effects of bitter melon on breast, ovarian, and cervical cancer cells and discusses future research recommendations.