Purpose <p>To present an overview of emerging pharmacological strategies for the prevention and treatment of proliferative vitreoretinopathy (PVR).</p> Methods <p>This review critically examines recent experimental and clinical evidence on pharmacological agents targeting key pathogenic mechanisms of PVR, including epithelial–mesenchymal transition, profibrotic cytokine signaling (TGF-β, PDGF, VEGF), and inflammation-driven tissue remodeling. Investigated compounds include clinically tested substances such as daunorubicin, 5-fluorouracil, corticosteroids, anti-VEGF agents, methotrexate, isotretinoin, decorin and infliximab, as well as newer experimental approaches including Topotecan, Melphalan, ROCK-Inhibitors and gene-regulated therapies. Mechanistic insights into receptor crosstalk, intracellular signaling cascades, and cell survival pathways are integrated with findings from preclinical models and clinical studies.</p> Results <p>Several agents have shown anti-proliferative and anti-inflammatory effects in vitro and in vivo, with methotrexate and infliximab emerging as particularly promising candidates. However, clinical data remain heterogeneous, and no pharmacological agent has yet received regulatory approval for PVR treatment. Risk stratification based on preoperative PVR, vitreous hemorrhage, or ocular trauma may help optimize patient selection in future trials.</p> Conclusion <p>Pharmacological modulation of PVR is conceptually well supported by preclinical data, but clinical translation remains limited. Well-designed randomized trials in clearly defined high-risk populations are needed to validate efficacy, determine optimal treatment windows, and develop standardized protocols for both prophylaxis and therapy.</p>