Scopoletin, a coumarin compound found in various medicinal and edible plants, has been extensively studied for its pharmacological activities and potential therapeutic applications. This review provides an overview of scopoletin's pharmacology, pharmacokinetics, and toxicity. Scopoletin exhibits a wide range of beneficial properties, including antimicrobial, anticancer, anti-inflammatory, anti-angiogenic, antioxidant, antidiabetic, antihypertensive, hepatoprotective, neuroprotective, and immunomodulatory effects. It inhibits enzymes such as choline acetyltransferase, acetylcholinesterase, and monoamine oxidase. Pharmacokinetic studies indicate low bioavailability, rapid absorption, and extensive metabolism of scopoletin, which may be due to its poor solubility in aqueous media. Toxicity research suggests that scopoletin is non-toxic to most cell types tested, indicating its potential as a safe and effective drug candidate for treating various diseases. However, further studies are needed to explore its molecular mechanisms, verify its toxicity, and enhance its oral bioavailability. The review also discusses the prospects and future research directions for scopoletin, highlighting its potential as a lead compound for developing new, efficient, and low-toxicity derivatives.Scopoletin, a coumarin compound found in various medicinal and edible plants, has been extensively studied for its pharmacological activities and potential therapeutic applications. This review provides an overview of scopoletin's pharmacology, pharmacokinetics, and toxicity. Scopoletin exhibits a wide range of beneficial properties, including antimicrobial, anticancer, anti-inflammatory, anti-angiogenic, antioxidant, antidiabetic, antihypertensive, hepatoprotective, neuroprotective, and immunomodulatory effects. It inhibits enzymes such as choline acetyltransferase, acetylcholinesterase, and monoamine oxidase. Pharmacokinetic studies indicate low bioavailability, rapid absorption, and extensive metabolism of scopoletin, which may be due to its poor solubility in aqueous media. Toxicity research suggests that scopoletin is non-toxic to most cell types tested, indicating its potential as a safe and effective drug candidate for treating various diseases. However, further studies are needed to explore its molecular mechanisms, verify its toxicity, and enhance its oral bioavailability. The review also discusses the prospects and future research directions for scopoletin, highlighting its potential as a lead compound for developing new, efficient, and low-toxicity derivatives.