Pharmacological targeting of the mechanistic target of rapamycin (mTOR) has emerged as a promising strategy in ophthalmology, given mTOR’s central role in regulating cellular growth, metabolism, autophagy, and survival across various ocular tissues. mTOR inhibitors, such as rapamycin (sirolimus) and its analogs (rapalogs), have demonstrated therapeutic potential in modulating pathological angiogenesis, inflammation, fibrosis, and neurodegeneration in multiple ophthalmic disorders. In the anterior segment, mTOR inhibition has shown benefit in delaying cataractogenesis and modulating fibrosis in corneal wound healing and glaucoma surgery. In the posterior segment, mTOR modulators are under investigation for their roles in suppressing choroidal neovascularization in age-related macular degeneration (AMD), preserving photoreceptors in retinitis pigmentosa, and enhancing retinal ganglion cell survival in glaucomatous optic neuropathy. Systemic and intraocular formulations are being evaluated to optimize tissue specificity, minimize adverse effects, and overcome barriers related to ocular bioavailability. As our understanding of mTOR’s tissue-specific roles deepens, its pharmacological manipulation offers a versatile platform for targeted interventions in both anterior and posterior segment diseases.