An evidence-based review of unoprostone isopropyl ophthalmic solution 0.15% for glaucoma: place in therapy

Abstract

Glaucoma is a progressive, neurodegenerative optic nerve disease that can cause significant visual morbidity and affects over 60 million people worldwide. The only known modifiable risk factor for glaucoma at this time is elevated intraocular pressure (IOP), which may be treated with medications, laser therapy, and/or incisional surgery. Topical ocular medications are commonly used as first-line therapy for glaucoma, although side effects may limit their use. Unoprostone is a novel 22-carbon ocular hypotensive agent that may be advantageous in treating some patients with open angle glaucoma or ocular hypertension. Unlike the 20-carbon prostanoids, such as latanoprost, that lower IOP primarily through an increase in uveoscleral outflow, unoprostone may lower IOP through increased aqueous outflow via the conventional trabecular meshwork pathway. Although not as efficacious as other prostanoids, unoprostone is effective for IOP reduction both as monotherapy and adjunctive therapy with timolol. Unoprostone has decreased affinity for the prostaglandin F2α receptor, which may explain its well tolerated ocular and systemic side effect profile compared with other prostanoids.

Network Meta-analysis for Clinical Practice Guidelines: A Case Study on First-Line Medical Therapies for Primary Open-Angle Glaucoma

“…A notable exception is unoprostone, which was the least effective drug in the 2004 and 2009 network meta-analyses despite the high ranking of all other prostaglandins. Indeed, there is uncertainty as to whether unoprostone should be classified as a prostaglandin analogue (38, 39). …”

Novel Therapies for Tongue Squamous Cell Carcinoma Patients with High-Grade Tumors

“…Iloprost could also improve endobronchial dysplasia and prevent the development of lung cancer. ZINC8214703, namely, unoprostone, could reduce intraocular pressure and treat glaucoma [ 47 ]. ZINC85537014, namely, cobicistat, has the ability to treat human immunodeficiency virus (HIV) infection [ 48 ] and increase the response rates of anticancer drugs [ 49 ].…”

A Novel Convergent Synthesis of the Potent Antiglaucoma Agent Tafluprost

“…The discovery of potent and efficacious intraocular pressure (IOP) lowering PGF 2α analogs 1 – 5 ( Figure 1 ) has revolutionized the treatment of ocular hypertension, a major risk factor for progression of the irreversible blinding disease glaucoma [ 1 , 2 ]. Until recently, free isopropyl ester prodrugs, i.e., unoprostone ( 1 , Rescula), latanoprost ( 2 , Xalatan) and travoprost ( 3 , Travatan), and one amide prodrug bimatoprost ( 4 , Lumigan) of ω-chain modified PGF 2α analogs have been used as first line therapy for the treatment of open angle glaucoma and ocular hypertension due to their potent IOP-lowering efficacy, low likelihood of systemic adverse effects, once-daily dosing and good patient adherence [ 3 , 4 , 5 , 6 ]. However, all the available commercial preparations of 1 – 4 contain preservatives to maintain the sterility of the solutions, which may impair topical tolerance of these IOP-lowering agents during long-term use [ 7 ].…”