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

Abstract

Introduction: Glaucoma is one of the main leading causes of irreversible blindness in the word. 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 analogues, 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.

Hypotensive Effect of Nanomicellar Formulation of Melatonin and Agomelatine in a Rat Model: Significance for Glaucoma Therapy

“…In this respect, glaucoma patients can take advantage of molecules exerting IOP-lowering effects and neuroprotective actions at the same time [26]. If one considers that several patients continue to experience glaucoma progression despite IOP reduction, then novel therapies need to be urgently developed [6] and basic research is actively involved in investigating molecules with potential application as anti-glaucoma agents.…”

“…However, these therapies are not without adverse effects and their efficacy is also subject to a reduction after prolonged use. In addition, there are patients who continue to experience glaucoma progression despite IOP reduction, thus indicating the necessity of additional therapeutic approaches [6]. For instance, neuroprotective molecules, eventually preventing retinal ganglion cell degeneration, have been reported to halt or delay glaucoma progression when used alone or in combination with IOP-lowering drugs [7].…”

The management of glaucoma and macular degeneration

“…Glaucoma [1][2][3][4][5][6][7][8] and macular degeneration [9][10][11] are among the ophthalmologic diseases increasingly affecting the aging population worldwide. It is estimated that around 76 million patients will suffer of glaucoma in 2020, whereas the prevalence in the population between 40 and 80 years old is expected to increase to 111.8 million in 2040 [2].…”

“…Both conditions are neuropathies and are associated with vision loss, eventually leading to blindness. Glaucoma is a multifactorial disease, with the most salient feature being an elevated intraocular pressure (IOP), which still is nowadays the only clinically modifiable risk factor for its development and progression [3][4][5][6]. Macular degeneration, also denominated agerelated macular degeneration (AMD) is characterized by the loss of vision in the central part of the visual field, involving the central part of the retina where the macula is found [9][10][11].…”

“…Blurred vision and/or visual hallucinations may also occur in AMD patients. These conditions, together with glaucoma, represent the leading causes of blindness in the industrialized countries [1][2][3][4][5][6]9]. AMD is classified in two main types, the dry or non-neovascular AMD, with a prevalence of 90% among the affected patients [11], and the wet, or neovascular AMD, which involves abnormal neo-vascularization under or nearby the macula [12,13].…”