Open-angle Glaucoma (OAG)

Also known as: Open-angle glaucoma / Glaucoma, Open-angle / Open angle glaucoma NOS / Pigmentary glaucoma / Open angle glaucoma / Open-angle glaucoma NOS / Open-angle glaucoma, unspecified / Glaucoma simplex

DrugDrug NameDrug Description
DB00484BrimonidineBrimonidine is an alpha-adrenergic agonist and 2-imidazoline derivative that was first introduced in 1996.[A178951] It is considered to be a third generation alpha-2 aadrenergic receptor agonist, since it displays preferential binding at alpha-2 adrenoceptors over alpha-1 receptors.[A179002] Brimonidine displays a higher selectivity toward the alpha-2 adrenergic receptors than [clonidine] or [apraclonidine], which are also alpha-2 adrenergic agonists.[A178969] Alpha-2 adrenergic agonists are members of the ocular hypotensive agent drug class that are used in the chronic treatment of glaucoma. Early treatment and management of glaucoma, which predominantly involves the lowering of intraocular pressure, is critical since glaucoma is considered to be a common cause of blindness worldwide.[A178948,A178969] Ophthalmically, brimonidine is used to lower intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow. Because it is oxidately stable, brimonidine is associated with fewer reports of ocular allergic reactions compared to other alpha-2 adrenergic agonists.[A178969] The ophthalmic solution of brimonidine was first approved by the FDA in 1996 as Alphagan [label] and brimonidine is the only selective alpha-adrenergic receptor agonist approved for chronic treatment in glaucoma.[A36674] Brimonidine is also found in ophthalmic solutions in combination with [brinzolamide] under the market name Simbrinza for the reduction in intraocular pressure. Unlike nonselective beta-blockers used in ocular hypertension, brimonidine is not associated with significantly adverse cardiopulmonary side effects.[A178945] Thus brimonidine is an effective and safe alternative to beta-blockers, in patients with, or at high risk for, cardiopulmonary disease.[A178948] The topical form of brimonidine was approved by the FDA in August 2013 for the symptomatic treatment of persistent facial erythema of rosacea in adults. It is marketed under the brand name Mirvaso.[L6535] Brimonidine is the first topical treatment approved for facial erythema of rosacea.[A178978]
DB01194BrinzolamideBrinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase inhibitor. Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II). Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in intraocular pressure. Brinzolamide is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
DB00869DorzolamideDorzolamide is a carbonic anhydrase (CA) inhibitor. It is used in ophthalmic solutions (Trusopt) to lower intraocular pressure (IOP) in open-angle glaucoma and ocular hypertension.
DB01057EchothiophateA potent, long-acting irreversible cholinesterase inhibitor used as an ocular hypertensive in the treatment of glaucoma. Occasionally used for accomodative esotropia.
DB00654LatanoprostLatanoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a prostaglandin analogue that works by increasing the outflow of aqueous fluid from the eyes. It is also known by the brand name of Xalatan manufactured by Pfizer.
DB01210LevobunololA nonselective beta-adrenoceptor antagonist used in the treatment of glaucoma.
DB00703MethazolamideA carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. [PubChem]
DB13931NetarsudilA Rho kinase inhibitor with norepinephrine transport inhibitory activity that reduces production of aqueous As of December 18, 2017 the FDA approved Aerie Pharmaceutical's Rhopressa (netarsudil ophthalmic solution) 0.02% for the indication of reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Acting as both a rho kinase inhibitor and a norepinephrine transport inhibitor, Netarsudil is a novel glaucoma medication in that it specifically targets the conventional trabecular pathway of aqueous humour outflow to act as an inhibitor to the rho kinase and norepinephrine transporters found there as opposed to affecting protaglandin F2-alpha analog like mechanisms in the unconventional uveoscleral pathway that many other glaucoma medications demonstrate.
DB01085PilocarpineA slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.
DB08819TafluprostA prostaglandin analogue ester prodrug used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. Chemically, tafluprost is a fluorinated analog of prostaglandin F2-alpha. Tafluprost was approved for use in the U.S. on February 10, 2012.
DB00373TimololA beta-adrenergic antagonist similar in action to propranolol. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of migraine disorders and tremor.
DB00287TravoprostTravoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure [FDA Label]. It is a synthetic prostaglandin F2alpha analog [FDA Label]. Having been a well-received therapeutic agent with demonstrated efficacy and safety, travoprost is currently approved by the US FDA as a first-line treatment for lowering intraocular pressure in patients with open-angle glaucoma or ocular hypotension [L5155]. Furthermore, this approval also solidifies the medication as the first and only prostaglandin analog approved by the FDA for first-line treatment of glaucoma patients that does not contain the preservative benzalkonium chloride [L5155]. Moreover, travoprost is also currently approved in the EU for the decrease of elevated intraocular pressure in paediatric patients aged 2 months to < 18 years with ocular hypertension or paediatric glaucoma [L5146, L5152].
DB06826UnoprostoneUnoprostone isopropyl is a prostaglandin analogue. Ophthalmic Solution 0.15% is a synthetic docosanoid. Unoprostone isopropyl has the chemical name isopropyl (+)-(Z)-7-[(1R,2R,3R,5S)-3,5 dihydroxy-2-(3-oxodecyl)cyclopentyl]-5-heptenoate. The main indication of Unoprostane is treatment of glucoma.
DrugDrug NameTargetType
DB00484BrimonidineAlpha-2A adrenergic receptortarget
DB00484BrimonidineAlpha-2B adrenergic receptortarget
DB00484BrimonidineAlpha-2C adrenergic receptortarget
DB00484BrimonidineAldehyde oxidaseenzyme
DB01194BrinzolamideCarbonic anhydrase 1target
DB01194BrinzolamideCarbonic anhydrase 2target
DB01194BrinzolamideCytochrome P450 3A4enzyme
DB01194BrinzolamideCarbonic anhydrase 5A, mitochondrialtarget
DB01194BrinzolamideCarbonic anhydrase 4target
DB01194BrinzolamideCarbonic anhydrase 3target
DB00869DorzolamideCarbonic anhydrase 2target
DB00869DorzolamideCarbonic anhydrase 1target
DB00869DorzolamideCarbonic anhydrase 4target
DB00869DorzolamideCytochrome P450 2C9enzyme
DB00869DorzolamideCytochrome P450 3A4enzyme
DB00869DorzolamideCarbonic anhydrase 3target
DB01057EchothiophateSerum albumincarrier
DB00654LatanoprostProstaglandin F2-alpha receptortarget
DB00654LatanoprostSolute carrier organic anion transporter family member 2B1transporter
DB00654LatanoprostSolute carrier family 22 member 1transporter
DB01210LevobunololBeta-1 adrenergic receptortarget
DB01210LevobunololBeta-2 adrenergic receptortarget
DB01210LevobunololCytochrome P450 2D6enzyme
DB00703MethazolamideCarbonic anhydrase 1target
DB00703MethazolamideSolute carrier family 22 member 6transporter
DB00703MethazolamideCytochrome P450 2C19enzyme
DB00703MethazolamideCytochrome P450 2D6enzyme
DB00703MethazolamideCytochrome P450 2E1enzyme
DB00703MethazolamideCytochrome P450 3A4enzyme
DB00703MethazolamideCarbonic anhydrase 4target
DB00703MethazolamideCarbonic anhydrase 2target
DB00703MethazolamideCarbonic anhydrase 7target
DB00703MethazolamideCarbonic anhydrase 3target
DB13931NetarsudilRho-associated protein kinase 1target
DB13931NetarsudilRho-associated protein kinase 2target
DB13931Netarsudilsolute carrier family 6 member 2target
DB01085PilocarpineMuscarinic acetylcholine receptor M1target
DB01085PilocarpineMuscarinic acetylcholine receptor M2target
DB01085PilocarpineCytochrome P450 2A6enzyme
DB01085PilocarpineMuscarinic acetylcholine receptor M3target
DB01085PilocarpineCytochrome P450 2E1enzyme
DB01085PilocarpineCytochrome P450 3A4enzyme
DB01085PilocarpineMuscarinic acetylcholine receptor M4target
DB08819TafluprostProstaglandin F2-alpha receptortarget
DB08819TafluprostProstaglandin G/H synthase 2enzyme
DB00373TimololBeta-1 adrenergic receptortarget
DB00373TimololBeta-2 adrenergic receptortarget
DB00373TimololCytochrome P450 2D6enzyme
DB00373TimololMultidrug resistance protein 1transporter
DB00373TimololCytochrome P450 2C19enzyme
DB00287TravoprostProstaglandin F2-alpha receptortarget
DrugDrug NamePhaseStatusCount
DB00905Bimatoprost1 / 2Completed2
DB12295Evodenoson1 / 2Completed1
DB00654Latanoprost1 / 2Completed1
DB00373Timolol1 / 2Completed3
DB05288Anecortave acetate2Completed2
DB01381Ginkgo biloba2Completed1
DB15071Omidenepag isopropyl2Completed1
DB12977Simenepag isopropyl2Completed2
DB05288Anecortave acetate2 / 3Completed1
DB05288Anecortave acetate2 / 3Withdrawn1
DB00869Dorzolamide2 / 3Completed1
DB00373Timolol2 / 3Completed1
DB00195Betaxolol3Unknown Status1
DB11660Latanoprostene Bunod3Completed2
DB00373Timolol3Active Not Recruiting2
DB01234Dexamethasone4Active Not Recruiting1
DB00588Fluticasone propionate4Completed1
DB00654Latanoprost4Not Yet Recruiting2
DB11660Latanoprostene Bunod4Not Yet Recruiting1
DB13931Netarsudil4Active Not Recruiting1
DB11077Polyethylene glycol 4004Completed1
DB11060Polyvinyl alcohol4Completed1
DB00373Timolol4Not Yet Recruiting1
DB00684Tobramycin4Active Not Recruiting1
DB00287Travoprost4Active Not Recruiting2
DB00905BimatoprostNot AvailableCompleted9
DB00484BrimonidineNot AvailableCompleted1
DB00869DorzolamideNot AvailableWithdrawn1
DB00654LatanoprostNot AvailableCompleted1
DB00305MitomycinNot AvailableUnknown Status1
DB01085PilocarpineNot AvailableCompleted1
DB00373TimololNot AvailableCompleted5
DB00373TimololNot AvailableWithdrawn1
DB00287TravoprostNot AvailableCompleted2