Novel therapies for glaucoma: a patent review (2013-2019)

ABSTRACT

Introduction: Glaucoma is one of the main leading causes of irreversible blindness in the world. The treatment of this disease relies on the use of drugs able to reduce/control the intraocular pressure (IOP), one of the main risk factors for glaucoma. Current therapies are based on the use of compounds belonging to well-established categories (prostaglandin analogs, β-adrenergic blockers, α-adrenergic agonists, carbonic anhydrase inhibitors, Rho kinase inhibitors, and cholinergic agonists). However, even if they are effective in reducing IOP, important side effects impair patient compliance, accounting for the necessity of novel therapy approaches. Therefore, new targets are emerging as alternative and more complete routes to fight glaucoma disease.

Areas covered: This review provides a comprehensive update on the development state of innovative strategies against glaucoma describing results, administration routes, pharmaceutical compositions, structures, and SARs as well as the related shortcomings within the 2013–2019 range.

Expert opinion: New innovative pharmacological targets have been explored in the last six years, allowing a broader therapeutic arsenal against glaucoma and IOP-related pathologies. The endocannabinoid system and FAAH inhibitors were the most investigated from a medicinal chemistry point of view.

KEYWORDS:

• Glaucoma
• melatonin receptor agonists
• adenosine receptor
• FAAH inhibitors
• endocannabinoids
• RNA interference

Article highlights

• Novel drugs acting upon new targets are studied alone or in combination with well-established therapies.

• In the last six years, most of the patents concern the endocannabinoid system to prevent/treat glaucoma.

• A large plethora of FAAH inhibitors featured by the carbamate moiety are disclosed.

Pharmaceutical compositions are licensed after demonstrating their efficacy in in vivo models with respect to conventional therapies.

This box summarizes 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.