Schlemm's canal (SC), as the primary pathway for aqueous humor drainage, maintains intraocular pressure balance by regulating aqueous outflow. Abnormalities in its structure and function are closely associated with elevated intraocular pressure and the development of glaucoma. Research on SC aids in elucidating the mechanisms behind outflow resistance and exploring new avenues to enhance aqueous drainage, thereby providing a foundation for the development of new drugs aimed at lowering intraocular pressure and treating glaucoma. Currently, our understanding of the mechanisms regulating SC development and functionality remains limited, with a lack of specific therapeutic strategies targeting SC. In recent years, advancements in measurement and imaging technologies have revealed the molecular and cellular mechanisms underlying SC development, leading to the identification of key regulatory targets. This has enhanced our understanding of SC structural and functional regulation. Furthermore, innovative applications of SC as a target for intraocular pressure-lowering medications and surgical interventions are continually expanding. This article systematically reviews the research on the structure and function of SC, summarizes the key molecular and cellular regulatory mechanisms, and discusses the latest advancements in SC-targeted pharmacological and surgical therapies, providing new insights for the clinical diagnosis and management of glaucoma.