Prostaglandin receptor agonists as antiglaucoma agents (a patent review 2013 – 2018)

ABSTRACT

Introduction: Elevated intraocular pressure (IOP) is the most prevalent risk factor for glaucoma. Prostaglandin analogs are a first-line therapy for glaucoma due to their ability to reduce IOP, once-daily dosing, efficacy, and minimal side-effect profile. Many compounds targeting different PG receptors have been developed in the last years, some of them being in clinical use. Latanoprost, Bimatoprost, Travoprost, and Tafluprost are clinically used as antiglaucoma drugs and act as agonists of the PGF2α receptor. The inability to fully understand the mechanism of action of clinically used PGF2α analogs is thus a strong driver for additional research into the mechanism of action of ocular hypotensive drugs belonging to this class of pharmacological agents.

Areas covered: This review explores the last 5 years (2013–2018), where many patents describing new compounds acting on different prostaglandin receptors, and mainly targeting EP1-4 and FP receptors, were released.

Expert opinion: To date, there has been a growing awareness over recent years of the therapeutic use of novel derivatives as new antiglaucoma pharmaceutical products. Patents involved in discovering new approaches and new molecules for the treatment of glaucoma diseases encouraged the scientific community to increase the variety of drugs available for the treatment of ocular diseases.

KEYWORDS:

• Glaucoma
• prostaglandins
• prostaglandin F2alpha
• EP receptor
• medical therapy

Article highlights

• Prostaglandin receptor agonist agents are the first-line treatment for glaucoma due to their efficacy, lack of relevant systemic side effects and need for fewer instillations

• This article covers new prostaglandin receptor agonist patent applications between 2013 and 2018.

• Structures and the efficacies such as the EC₅₀ values of the representative compounds in various assays are provided.

• Pharmacological evidence for EP₂ and EP₄ prostanoid receptors as novel targets in the treatment of glaucoma

• With the growing scientific and industrial interest in these new drugs, it is probable that some of these new compounds may be available on the market soon.

This box summarizes the key points contained in the article.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.