Stevia (Stevia rebaudiana), one of the perennial shrubs that are indigenous to South America, synthesizes diterpene glycosides. Stevia leaves comprise steviol glycosides (SGs) such as stevioside, isosteviol, steviolbioside, and rebaudioside (A-E). These components are low-calorie calories and used as a sugar substitute in foods, beverages, and medications. The goal of the current investigation is to summarize the pharmacological activities with exposed fundamental molecular processes against different diseases. Additionally, we have encapsulated botanical sources, pharmacokinetics, and toxicological profiles of SGs. For this reason, the data (up to date as of July 10, 2024) was retrieved from a variety of credible and authoritative sources, such as Google Scholar, Wiley Online, PubMed, ScienceDirect, Springer Link, Scopus, and Web of Science. Our findings suggested that SGs have potent antidiabetic activity by mimicking insulin actions by regulating the PI3K/AKT pathway. Besides, SGs have a diverse range of pharmacological activities, including antioxidant, anti-inflammatory, antiobesity, antihypertensive, antimicrobial, antidiarrheal, gastroprotective, hepatoprotective, pulmoprotective, and renoprotective activities. Our findings also suggested that SGs have prospective anticancer properties through various molecular pathways. According to studies, SGs are neither mutagenic nor carcinogenic, not teratogenic, and do not provoke acute or subacute toxicity. Taken together, this investigation demonstrates that SGs have enormous promise as a curative agent for the medication of several diseases and disorders.