Copaifera is a genus of large trees found in Brazil, mainly in Amazon forest, but also in Atlantic forest and cerrado biomes. It has also been found in other countries in South America. In Africa, it is found mainly in Congo, Cameroon, Guinea and Angola. Its oleoresin has been used in folk medicine in the treatment of numerous healthy disorders, such as urinary, respiratory, skin and inflammatory diseases, for which there are several studies corroborating its ethnopharmacological uses. It is also extensively employed in the pharmaceutical and cosmetic industries in the development of ointments, pills, soaps, perfumes, among others. Copaifera oleoresin contains mainly diterpenes, such as: kaurenoic acid, kaurenol, copalic acid, agathic acid, hardwiickic acid, polyalthic acid, and sesquiterpenes, comprising β-caryophyllene, caryophyllene oxide, α-copaene, α–humulene, γ-muurolene and β-bisabolol, among other compounds. On the other hand, Copaifera leaves contain mainly phenolic compounds, such as flavonoids and methylated galloylquinic acid derivatives. Therefore, considering the economic importance of Copaifera oleoresin, its ethnopharmacological uses, the need to develop new pharmaceuticals for the treatment of many diseases, as well as the pharmacological potential of the compounds found in Copaifera spp., it was undertaken a review covering mostly the last two decades on the distribution, chemistry, pharmacology, quality control and safety of Copaifera species.