While effective control of intraocular pressure (IOP) remains an essential element of glaucoma management, our increasing understanding of the role of vascular and neuroprotective dysfunctions strongly suggest the development of therapeutic strategies that target the multifactorial nature of the disease. The pharmacological armamentarium of treatment options for glaucoma is substantial and includes beta-blockers, cholinergic agents, alpha2 agonists, other adrenergic drugs, topical and systemic carbonic anhydrase inhibitors, a prostaglandin analogue, and osmotics. Unoprostone isopropyl, a novel drug from the new class of docosanoids that are potential modulators of retinal function, effectively reduces mild to moderate IOP elevations and has the potential to offer vascular and neuroprotective properties. In addition, a clinical trial evaluating the effects of unoprostone isopropyl and timolol maleate on cardiovascular function in healthy patients during exercise found that unoprostone isopropyl does not exhibit effects on heart rate. A pulmonary function study demonstrated that unoprostone isopropyl did not differ significantly from placebo in either primary or secondary variables, suggesting that the drug lacks pulmonary effects consistent with beta-blockade or FP-agonism. This lack of systemic effects may improve quality of life and compliance. Finally, clinical trials show that unoprostone isopropyl is a safe and effective adjunct to timolol maleate and to latanaprost; when added to latanaprost, unoprostone isopropyl produced additional IOP reductions. Conclusion: Unoprostone isopropyl is an effective and safe therapeutic option for patients with mild to moderate IOP elevations, those in whom beta-blockers are contraindicated, and those with mild to moderate stable asthma.