In this review, the literature data on recent advances of the medicinal plant Brucea javanica (L.) Merr. (Simaroubaceae), both phytochemical and biological investigations, are compiled. Brucea javanica is an evergreen shrub distributed widely in Southeast Asia and northern Australia. In China, the seeds of Brucea javanica have been used as traditional herbal medicine due to its multifaceted activities. To date, 153 compounds have been reported from the seeds and aerial parts of Brucea javanica. Quassinoids are the main constituents of this species. The extract of Brucea javanica and the isolated compounds especially quassinoids exhibited various biological properties, such as antitumor and antimalarial effects.