As a commonly employed traditional Chinese medicine, Peucedani Radix (Qian-hu in Chinese), which consists of the dried roots of Peucedanum praeruptorum Dunn, has a long history of application for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper air-way infections in traditional medicinal practice. The current review aims to summarize the research progress on the botany, phytochemistry, chemical analysis, pharmacological assay, and pharmacokinetic profile of this famous herbal drug. All available information on this traditional medicine was obtained via electronic search (using ACS, PubMed, Web of Science, Google Scholar, Baidu Scholar, and CNKI). Phytochemical investigations revealed that angular-type pyranocoumarins (APs), mainly (±)-praeruptorin A (Pd-Ia), (+)-praeruptorin A, (±)-praeruptorin B, (+)-praeruptorin B (Pd-II) and (+)-praeruptorin E (Pd-III), were the main active components in Qian-hu, while some other types of ingredients were also identified from this herb. The crude extract and pure compounds from Peucedani Radix exhibited a wide spectrum of in vitro and in vivo pharmacological activities, including vasorelaxant, cardioprotective, hepatoprotective, anti-tumor and anti-platelet aggregative effects. Conversely to the well-defined chemical constituents and activities, the properties of absorption, pharmacokinetics, and metabolism were rarely characterized. However, further investigations are wistful for the development of new drugs and therapies for various diseases, especially cardiovascular disorders. Collectively, the present review on the phytochemistry, chemical analysis, pharmacological evaluation, and pharmacokinetic profile of Peucedani Radix will provide meaningful information for further studies and commercial exploitation of the herbal medicine.