Bilobalide is a natural sesquiterpene trilactone from Ginkgo biloba leaves. It has good water solubility and is widely used in food and pharmaceutical fields. In the last decade, a plethora of studies on the pharmacological activities of bilobalide has been conducted and demonstrated that bilobalide possessed an extensive range of pharmacological activities such as neuroprotective, antioxidative, antiinflammatory, anti‐ischemic, and cardiovascular protective activities. Pharmacokinetic studies indicated that bilobalide may have the characteristics of rapid absorption, good bioavailability, wide distribution, and slow elimination. This review aims to summarize the advances in pharmacological, pharmacokinetics, toxicity, and safety studies of bilobalide in the last decade with an emphasis on its neuroprotective and antiinflammatory activities, to provide researchers with the latest information and point out the limitations of relevant research at the current stage and the aspects that should be strengthened in future research.