Protium heptaphyllum Aubl. belongs to the Burseraceae family. It is commonly called 'almecegueira' and is known to produce an amorphous resin which has constituents such as α- and β-amyrin, taraxastan-3-oxo-20-ol and sitostenonein. The α- and β-amyrin from P. heptaphyllum have pharmacological activities in several systems, such as central and peripheral nervous system, gastrointestinal tract and immunological system. In this study, our objective was to review pharmacological activities and to gather more information on the mixture of α- and β-amyrin obtained from P. heptaphyllum to guide future preclinical and clinical studies using this compound. This review consisted of searches performed using scientific databases such as PubMed, SciELO, LILACS, SciFinder and Science Direct. Some uses of α- and β-amyrin have been partially confirmed by previous studies demonstrating analgesic, anti-inflammatory, anticonvulsant, antidepressive, gastroprotective, hepatoprotective, antipancreatitic, anticholytic, antihyperglycemic and hypolipidemic effects. It is noteworthy that there are no α- and β-amirin toxicity tests described in the literature as recommended in the international guidelines, and such tests are one of the research stages to proceed in clinical and preclinical trials if this compound was to be used.