The interest and search for natural active principles with therapeutic properties from plants are growing, given their potential for use by the cosmetic and pharmaceutical industries. Thus, the objective of this review was to carry out a systematic analysis of scientific productions that have explored some therapeutic potential of Caryocar brasiliense. The methodology of the preferred reporting items was adopted for systematic review and meta-analysis protocols (PRISMA). Articles published in the period from 2009 to 2019 in the Web of Science and Bireme were selected and evaluated. The descriptors used were C. brasiliense, extract, and therapeutic. After applying the exclusion criteria, 25 studies were selected, elucidating a miscellany of therapeutic potentials for pequi, such as antioxidant, antifungal, antibiotic, antineoplastic, neuroprotective, regulation of blood pressure as well as analysis of the toxicity of different parts of the plant. It was verified that the pulp extract was the most used for therapeutic purposes, mainly orally. Toxicological studies have shown low toxicity for all parts of the plant, in high doses. The therapeutic benefits observed consisted mainly of antioxidant, anti-inflammatory, antimicrobial, antineoplastic, antiparasitic, and blood pressure control activities.