Ginkgo biloba is an ancient plant species that is thought to provide a variety of health benefits to living organisms and contains plenty of bioactive components, making it a chemically diversified plant. G. biloba has been shown to have a variety of medicinal and pharmacological properties, including anticancer, antidementia, antidiabetic, antiobesity, antilipidemic, antimicrobial, antioxidant, antilipid peroxidation, antiplatelet, anti-inflammatory, hepatoprotective, antidepressant, antiaging, immunomodulatory, antihypertensive, and neuroprotective effects and is frequently used to treat neurological, cardiovascular, and respiratory diseases, such as tardive dyskinesia. Therefore, this review described the therapeutic applications of G. biloba. In addition to describing the therapeutic potential, this review also evaluates the chemical constituents, toxicity, adverse effect, synergistic effect, and the clinical studies of this plant which have been utilized for therapeutic benefits but have demonstrated other consequences. The capacity of G. biloba components to act as free radical scavengers is critical, and combining its extract with other plant extracts has been shown to synergistically boost antioxidant properties. G. biloba used long-term or at high doses that resulted in some adverse effects. Severe drug interactions have also been reported in both animals and humans when combined with other medications. The available data established from both preclinical and clinical studies confirm the potential of G. biloba plant extract in various diseases. Besides, the safety and efficacy of G. biloba continue to require verification through additional experimentation to guide medicinal use.