Aquilaria spp. (agarwood) has been a part of Ayurvedic and Traditional Chinese Medicine for centuries. Agarwood has also been used as a traditional medicine in Southeast Asian countries, Bangladesh and Tibet. Its common uses include the treatment of joint pain, inflammatory-related ailments, and diarrhoea, as well as a stimulant, sedative and cardioprotective agent. In this paper, we aim to provide an overview of the phytochemistry, ethnomedicinal use, pharmacological activities and safety of plant materials from Aquilaria spp. as an evidence base to further appraise its potential use as a source of health beneficial compounds.