Background In traditional medicine of Southeast Asian countries, Baeckea frutescens L. (family Myrtaceae) has a long history of use. Numerous research projects have shown that this plant contains metabolites with remarkable medicinal value. No review document, to date, has given an insight into the role of B frutescens constituents in pharmacological development. Objective The current review briefly offers crucial information on the phytochemistry, biosynthesis, synthesis, and pharmacology of B frutescens. Methods B frutescens is the most meaningful keyword to search for literature data. It was used either on its own or in combination with other keywords. References have been gathered from various resources such as Google Scholar, SciFinder, and PubMed. More than 50 electronic references were collected from the 1960s. Results Approximately 130 metabolites have been isolated and structurally determined from this medicinal plant. They included phloroglucinols, phloroglucinol-based meroterpenoids, sesquiterpenoids, triterpenoids, flavonoids, chromones, 5-membered ring compounds, and others. B frutescens fresh tissues were thought to be a rich resource of essential oils. Tasmanone is a precursor in the biosynthesis of various B frutescens compounds, while phloroglucinol derivatives can be seen as initial compounds in the synthetic procedures of various B frutescens molecules. B frutescens plant extracts and compounds isolated from them possess a variety of pharmacological properties, such as cytotoxic, antimicrobial, anti-inflammatory, antioxidant, antirheumatoid, skin protective, and mosquito larvicidal activities. Conclusion More experimental reports on phytochemistry and pharmacology are required. In vivo pharmacological studies on the mechanisms of action of the active compounds are urgently required since most of the results obtained so far have been from in vitro assays.