Inflammation is a defensive reaction of the human body to numerous detrimental stimuli, including physical trauma, noxious chemicals, as well as microbial agents. Uncontrolled inflammation is the pathological basis of multiple diseases, such as rheumatoid arthritis? (RA), neurodegenerative diseases, liver disease, and lung inflammation. Lanostane triterpenoids are natural tetracyclic triterpenoids with significant anti?inflammatory activity. An extensive review of the published literature regarding the phytochemistry and anti?inflammatory pharmacology of lanostane triterpenoids has been performed and analyzed using several search engines, such as SciFinder, Web of Science, Scopus, PubMed, Google Scholar, and ScienceDirect. This review is devoted to naturally occurring lanostane?type triterpenes with anti?inflammatory activity, including their sources, biosynthesis, and mechanism of action. This review also discusses the inflammation?related diseases and the clinical significance of traditional Chinese medicine as multi?target therapeutic agents for the prevention and treatment of inflammatory diseases. In the past 30?years, more than 100 new lanostane?type triterpenes have been reported from the families Schisandraceae, Ganodermataceae, and Polyporaceae. Six compounds, fomitopinic acid A, fomitosides E and F, obtusifoliol, 4α, l4α?dimethyl?5α?ergosta?7,9(11), 24(28)?trien?3 β?ol, and gramisterol exhibited the most potent anti?inflammatory activity against cyclooxygenase?1?(COX?1) and COX?2, with IC50 values ranging from 0.087 to 1.15 μM. Some of these compounds exhibited significant activity by mediating the inhibition of the pro?inflammatory cytokines, inducible nitric oxide synthase, and COX?2 expression. This review provides a basis for identifying anti?inflammatory drugs with high selectivity, high potency, and few adverse effects from lanostane?type triterpenes.