Centella asiatica, a traditional Chinese medicine belonging to the Umbelliferae family, was recorded in the Eastern Han Dynasty. Owing to its wide developmental prospects, many scholars have extensively explored C. asiatica and made significant progress in recent years. In this study, we summarize the phytochemistry, pharmacology, and clinical applications of C. asiatica (L.) Urban based on Google Scholar, PubMed, and CNKI databases. Triterpenes and their glycosides, flavonoids, terpenoids, and volatile oils occur in herbs. The pharmacological effects mainly comprise improving cognition and memory impairment in Alzheimer’s disease and anti-inflammation activity. Clinical applications include the treatment of chronic kidney diseases, malignant intestinal obstruction, radiation dermatitis, precancerous lesions, chronic prostatitis, Alzheimer’s disease, and other diseases. This review provides insights into the phytochemistry, pharmacology, and clinical applications of C. asiatica and summarizes the shortcomings of the research in recent years to provide a reference for future research.