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

References

• Nickells RW, Howell GR, Soto I, et al. Under pressure: cellular and molecular responses during glaucoma, a common neurodegeneration with axonopathy. Annu Rev Neurosci. 2012;35:153–179.
   PubMed Web of Science ®Google Scholar
• Weinreb RN, Aung T, Medeiros FA. The pathophysiology and treatment of glaucoma. A review. JAMA. 2014;311:1901–1911.
   PubMed Web of Science ®Google Scholar
• Greco A, Rizzo MI, De Virgilio A, et al. Emerging concepts in glaucoma and review of the literature. Am J Med. 2016;129:1000.e7–1000.e13.
   PubMed Web of Science ®Google Scholar
• McLaren NC, Moroi SE. Clinical implications of pharmacogenetics for glaucoma therapeutics. Pharmacogenomics J. 2003;3:197–201.
   PubMed Web of Science ®Google Scholar
• Kim KE, Park KH. Update on the prevalence, etiology, diagnosis, and monitoring of normal-tension glaucoma. Asia Pac J Ophthalmol (Phila). 2016;5:23–31.
   PubMed Web of Science ®Google Scholar
• Masini E, Carta F, Scozzafava A, et al. Antiglaucoma carbonic anhydrase inhibitors: a patent review. Expert Opin Ther Pat. 2013;23:705–716.
   PubMed Web of Science ®Google Scholar
• Nocentini A, Ceruso M, Bua S, et al. Discovery of ß-adrenergic receptors blocker-carbonic anhydrase inhibitor hybrids for multitargeted antiglaucoma therapy. J Med Chem. 2018;61:5380–5394.
   PubMed Web of Science ®Google Scholar
• Donegan RK, Lieberman RL. Discovery of molecular therapeutics for glaucoma: challenges, successes, and promising directions. J Med Chem. 2016;59:788–809.
   PubMed Web of Science ®Google Scholar
• Carta F, Supuran CT, Scozzafava A. Novel therapies for glaucoma: a patent review 2007–2011. Expert Opin Ther Pat. 2012;22:79–88.
   PubMed Web of Science ®Google Scholar
• Moshirfar M, Parker L, Birdsong OC, et al. Use of Rho kinase inhibitors in ophthalmology: a review of the literature. Med Hypothesis Discov Innov Ophthalmol. 2018;7:101–111.
   PubMedGoogle Scholar
• Okumura N, Okazaki Y, Inoue R, et al. Rho-associated kinase inhibitor eye drop (Ripasudil) transiently alters the morphology of corneal endothelial cells. Invest Ophthalmol Vis Sci. 2015;56:7560–7567.
   PubMed Web of Science ®Google Scholar
• Dikopf MS, Vajaranant TS, Edward DP. Topical treatment of glaucoma: established and emerging pharmacology. Expert Opin Pharmacother. 2017;18:885–898.
   PubMed Web of Science ®Google Scholar
• Zhong Y, Yang Z, Huang W-C, et al. Adenosine, adenosine receptors and glaucoma: an updated overview. Biochim Biophys Acta. 2013;1830:2882–2890.
   PubMed Web of Science ®Google Scholar
• Shearer TW, Crosson CE. Adenosine A1 receptor modulation of MMP-2 secretion by trabecular meshwork cells. Invest Ophthalmol Vis Sci. 2002;43:3016–3020.
   PubMed Web of Science ®Google Scholar
• Laties A, Rich CC, Stoltz R, et al. A randomized phase 1 dose escalation study to evaluate safety, tolerability, and pharmacokinetics of Trabodenoson in healthy adult volunteers. J Ocul Pharmacol Ther. 2016;32:548–554.
   PubMed Web of Science ®Google Scholar
• Myers JS, Sall KN, DuBiner H, et al. A dose-escalation study to evaluate the safety, tolerability, pharmacokinetics, and efficacy of 2 and 4 weeks of twice-daily ocular Trabodenoson in adults with ocular hypertension or primary open-angle glaucoma. J Ocul Pharmacol Ther. 2016;32:555–562.
   PubMed Web of Science ®Google Scholar
• Cairns EA, Baldridge WH, Kelly ME. The endocannabinoid system as a therapeutic target in glaucoma. Neural Plast. 2016;10. Article ID 9364091.
   Web of Science ®Google Scholar
• Kohno M, Hasegawa H, Inoue A, et al. Identification of N-arachidonylglycine as the endogenous ligand for orphan G-protein-coupled receptor GPR18. Biochem Biophys Res Commun. 2006;347:827–832.
   PubMed Web of Science ®Google Scholar
• Nucci C, Bari M, Spanò A, et al. Potential roles of (endo)cannabinoids in the treatment of glaucoma: from intraocular pressure control to neuroprotection. Prog Brain Res. 2008;173:451–464.
   PubMed Web of Science ®Google Scholar
• Spadoni G, Bedini A, Furiassi L, et al. Identification of bivalent ligands with melatonin receptor agonist and fatty acid amide hydrolase (FAAH) inhibitory activity that exhibit ocular hypotensive effect in the rabbit. J Med Chem. 2018;61:7902–7916.
   PubMed Web of Science ®Google Scholar
• Hudson BD, Beazley M, Szczesniak A-M, et al. Indirect sympatholytic actions at β-adrenoceptors account for the ocular hypotensive actions of cannabinoid receptor agonists. J Pharmacol Exp Ther. 2011;339:757–767.
   PubMed Web of Science ®Google Scholar
• Labar G, Michaux C. Fatty acid amide hydrolase: from characterization to therapeutics. Chem Biodivers. 2007;4:1882–1902.
   PubMed Web of Science ®Google Scholar
• Nucci C, Gasperi V, Tartaglione R, et al. Involvement of the endocannabinoid system in retinal damage after high intraocular pressure-induced ischemia in rats. Invest Ophthalmol Vis Sci. 2007;48:2997–3004.
   PubMed Web of Science ®Google Scholar
• Tosini G, Baba K, Hwang CK, et al. Melatonin: an underappreciated player in retinal physiology and pathophysiology. Exp Eye Res. 2012;103:82–89.
   PubMed Web of Science ®Google Scholar
• Agorastos A, Huber CG. The role of melatonin in glaucoma: implications concerning pathophysiological relevance and therapeutic potential. J Pineal Res. 2011;50:1–7.
   PubMed Web of Science ®Google Scholar
• Martínez-Águila A, Fonseca B, Pérez de Lara MJ, et al. Effect of melatonin and 5-methoxycarbonylamino-N-acetyltryptamine on the intraocular pressure of normal and glaucomatous mice. J Pharmacol Exp Ther. 2016;357:293–299.
   PubMed Web of Science ®Google Scholar
• Crooke A, Huete-Toral F, Martínez-Águila A, et al. Melatonin and its analog 5-methoxycarbonylamino-N-acetyltryptamine potentiate adrenergic receptor-mediated ocular hypotensive effects in rabbits: significance for combination therapy in glaucoma. J Pharmacol Exp Ther. 2013;346:138–145.
   PubMed Web of Science ®Google Scholar
• Guzman-Aranguez A, Loma P, Pintor J. Small-interfering RNAs (siRNAs) as a promising tool for ocular therapy. Br J Pharmacol. 2013;170:730–747.
   PubMed Web of Science ®Google Scholar
• Palobiofarma SL. Thiazole modulators of A3 adenosine receptors. EP3248964 A1. 2015.
   Google Scholar
• Inotek Pharmaceuticals Corporation. Method of providing ocular neuroprotection. US 2014/0275128 A1. 2014.
   Google Scholar
• Handok Inc. Compounds antagonizing A3 adenosine receptor, method for preparing them, and medical-use thereof. WO 2017/123058 A1. 2017.
   Google Scholar
• Tsai JC, Chang HW. Comparison of the effects of brimonidine 0.2% and timolol 0.5% on retinal nerve fiber layer thickness in ocular hypertensive patients: a prospective, unmasked study. J Ocul Pharmacol Ther. 2005;21:475–482.
   PubMed Web of Science ®Google Scholar
• Krupin T, Liebmann JM, Greenfield DS, et al. A randomized trial of brimonidine versus timolol in preserving visual function: results from the low-pressure glaucoma treatment study. Am J Ophthalmol. 2011;151:671–681.
   PubMed Web of Science ®Google Scholar
• Quay WB. Increases in volume, fluid content, and lens weight of eyes following systemic administration of melatonin. J Pineal Res. 1984;1:3–13.
   PubMed Web of Science ®Google Scholar
• Meyer-Bothling U, Bron AJ, Osborne NN. Topical application of serotonin or the 5-HT1-agonist 5-CT intraocular pressure in rabbits. Invest Ophthalmol Vis Sci. 1993;34:3035–3042.
   PubMed Web of Science ®Google Scholar
• Osborne NN. Serotonin and melatonin in the iris/ciliary processes and their involvement in intraocular pressure. Acta Neurobiol Exp (Wars). 1994;54(Suppl):57–64.
   PubMedGoogle Scholar
• Alarma-Estrany P, Guzman-Aranguez A, Huete F, et al. Design of novel melatonin analogs for the reduction of intraocular pressure in normotensive rabbits. J Pharmacol Exp Ther. 2011;337:703–709.
   PubMed Web of Science ®Google Scholar
• Carvalho AF, Sharma MS, Brunoni AR, et al. The safety, tolerability and risks associated with the use of newer generation antidepressant drugs: a critical review of the literature. Psychother Psychosom. 2016;85:270–288.
   PubMed Web of Science ®Google Scholar
• Conway S, Canning SJ, Howell HE, et al. Characterisation of human melatonin mt(1) and mt(2) receptors by CRE-luciferase reporter assay. Eur J Pharmacol. 2000;390:15–24.
   PubMed Web of Science ®Google Scholar
• Millan MJ, Gobert A, Lejeune F, et al. The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways. J Pharmacol Exp Ther. 2003;306:954–964.
   PubMed Web of Science ®Google Scholar
• Pescosolido N, Gatto V, Stefanucci A, et al. Oral treatment with the melatonin agonist agomelatine lowers the intraocular pressure of glaucoma patients. Ophthalmic Physiol Opt. 2015;35:201–205.
   PubMed Web of Science ®Google Scholar
• Universidad Complutense de Madrid. The use of a melatonin analogue for the reduction of intraocular pressure. WO 2013/060908 A1. 2013.
   Google Scholar
• Auspex Pharmaceuticals, Inc. Cyclopropyl dihydrobenzofuran modulators of melatonin receptors. WO 2016/109359 A1. 2016.
   Google Scholar
• Farm to Farma, Inc. Cannabinoid formulations and method of making the same. US 2018/0133272 A1. 2018.
   Google Scholar
• Zengin G, Menghini L, Di Sotto A, et al. Chromatographic analyses, in vitro biological activities and cytotoxicity of Cannabis sativa L. essential oil: a multidisciplinary study. Molecules. 2018;23:3266.
   Web of Science ®Google Scholar
• Ferrante C, Recinella L, Ronci M, et al. Multiple pharmacognostic characterization on hemp commercial cultivars: focus on inflorescence water extract activity. Food Chem Toxicol. 2019;125:452–461.
   PubMed Web of Science ®Google Scholar
• Indiana University Research and Technology Corporation. A dual CB1/GPR18-based signaling system in the murine eye regulates intraocular pressure in a sex dependent manner. WO 2018/232225 A1. 2018.
   Google Scholar
• Rhodes Technologies. Pharmaceutical compositions for the treatment of ophthalmic conditions. WO 2019/045994 A1. 2019.
   Google Scholar
• Fondazione Istituto Italiano di Tecnologia. O-alkyl triazolyl carbamates as inhibitors of fatty acid amide hydrolase (FAAH). WO 2015/007613 A1. 2015.
   Google Scholar
• The Regents of the University of California and Fondazione Istituto Italiano di Tecnologia. Inhibitors of fatty acid amide hydrolase (FAAH) enzyme with improved oral bioavailability and their use as medicaments. WO 2015/157313 A1. 2015.
   Google Scholar
• Bial-Portela & Ca, S.A. Imidazolecarboxamides and their use as FAAH inhibitors. WO 2015/012708 A1. 2015.
   Google Scholar
• Käsnänen H, Myllymäki MJ, Minkkilä A, et al. 3-Heterocycle-phenyl N-alkylcarbamates as FAAH inhibitors: design, synthesis and 3D-QSAR studies. ChemMedChem. 2010;5:213–231.
   PubMed Web of Science ®Google Scholar
• Bial-Portela & Ca, S.A. Urea compounds and their use as FAAH enzyme inhibitors. WO 2015/016728 A1. 2015.
   Google Scholar
• Fire A, Xu S, Montgomery MK, et al. Potent and specific genetic interference by double-stranded RNA in Caenorhabditis elegans. Nature. 1998;391:806–811.
   PubMed Web of Science ®Google Scholar
• Elbashir SM, Harborth J, Lendeckel W, et al. Duplexes of 21-nucleotide RNAs mediate RNA interference in cultured mammalian cells. Nature. 2001;411:494–498.
   PubMed Web of Science ®Google Scholar
• Sylentis SAU siRNA and their use in methods and compositions for the treatment and/or prevention of eye conditions. WO 2014/037686 A1. 2014.
   Google Scholar
• Sylentis SAU siRNA and their use in methods and compositions for the treatment and/or prevention of eye conditions. US 2015/0259677 A1. 2015.
   Google Scholar
• Sylentis SAU siRNAs and their use in methods and compositions for the treatment and/or prevention of eye conditions. WO 2015/132303 A1. 2015.
   Google Scholar
• Moreno-Montañés J, Sádaba B, Ruz V, et al. Phase 1 clinical trial of SYL040012, a small interfering RNA targeting ß-adrenergic receptor 2, for lowering intraocular pressure. Mol Ther. 2014;22:226–232.
   PubMed Web of Science ®Google Scholar
• Gonzalez V, Palumaa K, Turman K, et al. Phase 2 of bamosiran (SYL040012), a novel RNAi based compound for the treatment of increased intraocular pressure associated to glaucoma. Invest Ophthalmol Vis Sci. 2014;55:564.
   Web of Science ®Google Scholar
• Calera MR, Topley HL, Liao Y, et al. Connexin43 is required for production of the aqueous humor in the murine eye. J Cell Sci. 2006;119:4510–4519.
   PubMed Web of Science ®Google Scholar
• Arrowhead pharmaceuticals Corp. RNAi-mediated inhibition of connexin 43 for treatment of IOP-related conditions. US 2016/0002638 A1. 2016.
   Google Scholar
• Ramya KV, Aswani DV, Ashim KM. Hypoxia-inducible factor-1 (HIF-1): a potential target for intervention in ocular neovascular diseases. Curr Drug Targets. 2013;14:919–935.
   PubMed Web of Science ®Google Scholar
• Arrowhead pharmaceuticals Corp. RNAi-mediated inhibition of frizzled related protein-1 for treatment of glaucoma. US 2015/0307882 A1. 2015.
   Google Scholar
• Tam LCS, Reina-Torres E, Sherwood JM, et al. Enhancement of outflow facility in the murine eye by targeting selected tight-junctions of Schlemm’s canal endothelia. Sci Rep. 2017;7:40717.
   PubMed Web of Science ®Google Scholar
• The College of The Holy & Undiv. Trinity of Queen Elizabeth Near Dublin, Imperial Innovations Ltd, Duke University. RNAi therapy for treatment and/or prevention of glaucoma. WO 2017/191077 A1. 2017.
   Google Scholar
• Phio Pharmaceuticals Corp. RNA interference in ocular indications. US 2016/0115482 A1.2016.
   Google Scholar
• Adams CM, Stacy R, Rangaswamy N, et al. Glaucoma – next generation therapeutics: impossible to possible. Pharm Res. 2019;36:25.
   Web of Science ®Google Scholar
• Jain A, Zode G, Kasetti RB, et al. CRISPR-Cas9-based treatment of myocilin-associated glaucoma. Proc Natl Acad Sci USA. 2017;114:11199–11204.
   PubMed Web of Science ®Google Scholar
• Editas Medicine. Crispr-cas systems having destabilization domain. WO 2018/005873 A1. 2018.
   Google Scholar
• Isarna Therapeutics Gmbh. Tgf-beta oligonucleotide for use in treatment of ophthalmic diseases. WO 2018/087359 A1. 2018.
   Google Scholar
• Pfeiffer N, Voykov B, Renieri G, et al. First-in-human phase I study of ISTH0036, an antisense oligonucleotide selectively targeting transforming growth factor beta 2 (TGF-ß2), in subjects with open-angle glaucoma undergoing glaucoma filtration surgery. PLoS One. 2017;12:e0188899.
   PubMed Web of Science ®Google Scholar
• Defert O, Boland S. Rho kinase inhibitors: a patent review (2014–2016). Expert Opin Ther Pat. 2017;27:507–515.
   PubMed Web of Science ®Google Scholar
• Yadav KS, Rajpurohit R, Sharma S. Glaucoma: current treatment and impact of advanced drug delivery systems. Life Sci. 2019;221:362–376.
   PubMed Web of Science ®Google Scholar
• Kaufman PL, Mohr ME, Riccomini SP, et al. Glaucoma drugs in the pipeline. Asia Pac J Ophthalmol (Phila). 2018;7:345–351.
   PubMed Web of Science ®Google Scholar
• Mietzner R, Breunig M. Causative glaucoma treatment: promising targets and delivery systems. Drug Discov Today. 2019. pii:S1359–6446(18)30403–3.
   PubMed Web of Science ®Google Scholar
• Negri L, Ferreras A, Iester M. Timolol 0.1% in glaucomatous patients: efficacy, tolerance, and quality of life. J Ophthalmol. 2019;2019: 1–12. Article ID 4146124.
   PubMedGoogle Scholar
• Granchi C, Caligiuri I, Minutolo F, et al. A patent review of Monoacylglycerol Lipase (MAGL) inhibitors (2013–2017). Expert Opin Ther Pat. 2017;27:1341–1351.
   PubMed Web of Science ®Google Scholar
• Poyomtip T. Roles of Toll-Like receptor 4 for cellular pathogenesis in primary open-angle glaucoma: a potential therapeutic strategy. J Microbiol Immunol Infect. 2019;52:201–206.
   PubMedGoogle Scholar
• Sun HJ, Xue DD, Lu BZ, et al. A novel synthetic steroid of 2,3,5-trihydroxy-androst-6-one alleviates the loss of rat retinal ganglion cells caused by acute intraocular hypertension via inhibiting the inflammatory activation of microglia. Molecules. 2019;24:252.
   Web of Science ®Google Scholar
• Saccà SC, Corazza P, Gandolfi S, et al. Substances of interest that support glaucoma therapy. Nutrients. 2019;11:239.
   Web of Science ®Google Scholar
• Quaranta L, Riva I, Biagioli E, et al.; CoQun® Study Group. Evaluating the effects of an ophthalmic solution of coenzyme Q10 and vitamin E in open-angle glaucoma patients: a study protocol. Adv Ther. 2019. DOI:10.1007/s12325-019-01023-3
   Web of Science ®Google Scholar