This review provides insights into the mechanism underlying the pathogenesis of myopia and potential targets for clinical intervention. Although the etiology of myopia involves both environmental and genetic factors, recent evidence has suggested that the prevalence and severity of myopia appears to be affected more by environmental factors. Current pharmacotherapeutics are aimed at inhibiting environmentally induced changes in visual input and subsequent changes in signaling pathways during myopia pathogenesis and progression. Recent studies on animal models of myopia have revealed specific molecules potentially involved in the regulation of eye development. Among them, the dopamine receptor plays a critical role in controlling myopia. Subsequent studies have reported pharmacotherapeutic treatments to control myopia progression. In particular, atropine treatment yielded favorable outcomes and has been extensively used; however, current studies are aimed at optimizing its efficacy and confirming its safety. Furthermore, future studies are required to assess the efficacy of combinatorial use of low-dose atropine and contact lenses or orthokeratology.