Acute ischemic stroke (AIS) remains a leading cause of long-term disability and mortality. The pathophysiological process of AIS is driven by a complex, intertwined ischemic cascade encompassing oxidative stress, neuroinflammation, excitatory amino acid toxicity, and blood-brain barrier damage. Though intravenous thrombolysis and endovascular therapy have dramatically improved the prognosis of patients with AIS, the narrow therapeutic window and ischemia-reperfusion injury still limit the benefits for a considerable proportion of patients. Edaravone dexborneol is a compound neuroprotective agent, composed of edaravone and dexborneol in a 4∶1 ratio, exerting cerebral protection through a synchronized dual-target mechanism of antioxidation and anti-inflammation. In this review, the pharmacological mechanism, clinical research results (including clinical randomized controlled trial studies and real-world studies), combination treatment strategies, applications in special stroke subtypes, and future research directions of edaravone dexborneol are summarized. Furthermore, we explore the potential for individualized precision therapy to guide the rational clinical use of this agent.