Humans have long used natural remedies like plants and herbs to treat disease. Furthermore, research has been ongoing to find alternative pharmaceutical drugs based on traditionally used plants, as natural products show fewer side effects compared to synthetic drugs. Medicinal plants have long been targeted in drug development due to their bioactive compounds like alkaloids, flavonoids, and terpenoids. This is not only the case for terrestrial plants, but marine environments also provide a larger diversity of flora and fauna with medicinal bioactive compounds. Vitex rotundifolia, also known as Beach Vitex, is a coastal plant that has been traditionally used to treat a variety of diseases including premenstrual syndrome, headaches, migraines, colds, and eye pain. There have been many review papers on V. rotundifolia, emphasizing its taxonomy, distribution, and biological activity. Our current mini-review not only summarizes the pharmacology and bioactivity of V. rotundifolia, but it also provides new information on the main bioactive compounds of V. rotundifolia such as flavonoids, phenolic acid, and terpenes and their current pharmacological activity in vitro and in vivo research. This information can be useful for developing new pharmaceutical and nutraceutical agents to treat and manage disease.