Grounded by the wide ethnopharmacological application of natural product, medicinal plants uses and its phar- macological properties have been actively discovered. This paper undertakes a comprehensive and updated review on Rhodomyrtus tomentosa leaves and its active compound – rhodomyrtone current state of research discovery. A search was conducted in PubMed, ScienceDirect, and Web of Science meeting the parameters and keywords of ‘Rhodomyrtus’, ‘R. tomentosa’ and ‘rhodomyrtone’. There are 147 articles published since 1975 about Rhodomyr- tus’s pharmacological activities and their isolated compounds. Numerous studies exist showed increased interest in the therapeutic properties of this plant, mainly for its active ingredients, which include rhodomyrtone. This arti- cle provides an updated review on phytochemistry studies and pharmacological activities including antimicrobial, anti-inflammatory, antioxidant and anticancer activities of R. tomentosa leaves and rhodomyrtone as major active constituent.