Glaucoma Pipeline 2026: Drugs in Trials & Targets

Remission & chronicity

Spontaneous remission

Progressive optic nerve damage without treatment; average visual field loss 0.5-1.0 dB/year; blindness in 10-20% without treatment; no spontaneous recovery of lost vision

Best-intervention remission

IOP-lowering drops: 20-30% IOP reduction; OHTS trial showed 50% risk reduction for glaucoma development in ocular hypertension; SLT (selective laser trabeculoplasty): IOP reduction 25-30%, equivalent to drops at 3 years (LiGHT trial); trabeculectomy: 35-45% IOP reduction, superior to drops in advanced disease

Gap size

Moderate — IOP control is achievable but compliance is the dominant barrier; neuroprotection remains an unmet need

Primary barrier

biological (neuroprotection) + practice (adherence)

IOP-lowering prevents further damage but cannot restore lost vision; adherence to drop therapy is poor (50-70% of patients non-adherent at 1 year); SLT (laser) as first-line (recommended by LiGHT trial) not universally adopted; once-yearly drop (latanoprostene bunod) and sustained-release implants (Durysta) improving adherence

Biomarker Targets & Therapeutic Agents

Gene targets queried against DGIdb, Open Targets, ChEMBL, PubMed, and Europe PMC. Agents ranked: Clinical > Mechanistic > Correlative.

ADORA1 266 ADRA2A 281 ADRB2 368 CA2 174 CA4 151 CHRM3 333 MYOC 5 OPTN 0 PTGFR 191 ROCK1 228 ROCK2 209

ADORA1

UniProt Ensembl DGIdb Open Targets

Therapeutic Agent	Effect Direction	Evidence Tier	Potency	Source
GS-9667	↑ activates	Mechanistic		DGIdb
SELODENOSON	↑ activates	Mechanistic		DGIdb
IMARADENANT	↓ inhibits	Mechanistic		DGIdb
CAPADENOSON	↑ activates	Mechanistic		DGIdb
4-{2-[(7-AMINO-2-FURAN-2-YL[1,2,4]TRIAZOLO[1,5-A][1,3,5]TRIAZIN-5-YL)AMINO]ETHYL}PHENOL	↓ inhibits	Mechanistic		DGIdb
ATL802	↓ inhibits	Mechanistic		DGIdb
PSB-11	↓ inhibits	Mechanistic		DGIdb
DERENOFYLLINE	↓ inhibits	Mechanistic		DGIdb
MSX-2	↓ inhibits	Mechanistic		DGIdb
PRELADENANT	↓ inhibits	Mechanistic		DGIdb
REGADENOSON ANHYDROUS	↑ activates	Mechanistic		DGIdb
NAMODENOSON	↑ activates	Mechanistic	1240.0 nM (Ki)	DGIdb
PSB603	↓ inhibits	Mechanistic		DGIdb
CAFFEINE	↓ inhibits	Mechanistic		DGIdb
MRS1191	↓ inhibits	Mechanistic		DGIdb
THEOPHYLLINE	↓ inhibits	Mechanistic		DGIdb
ST-1535	↓ inhibits	Mechanistic		DGIdb
(R)-PIA	↑ activates	Mechanistic		DGIdb
T-62	? unclear	Mechanistic		DGIdb
[3H]DPCPX	↓ inhibits	Mechanistic		DGIdb
2-CHLOROADENOSINE	↑ activates	Mechanistic		DGIdb
GS9667	↑ activates	Mechanistic		DGIdb
HEMADO	↑ activates	Mechanistic		DGIdb
L-97-1	↓ inhibits	Mechanistic		DGIdb
DU172	↓ inhibits	Mechanistic		DGIdb
LUF5831	↑ activates	Mechanistic		DGIdb
TECADENOSON	↑ activates	Mechanistic		DGIdb
TRABODENOSON	↑ activates	Mechanistic		DGIdb
ASPIRIN	? unclear	Mechanistic		DGIdb
DEFIBROTIDE	↑ activates	Mechanistic		DGIdb
PBF-680	↓ inhibits	Mechanistic		DGIdb
CHEMBL:CHEMBL59532	? unclear	Mechanistic		DGIdb
BINODENOSON	↑ activates	Mechanistic		DGIdb
MRS5151	↑ activates	Mechanistic		DGIdb
CHROMOCARB	? unclear	Mechanistic		DGIdb
AMP579	↑ activates	Mechanistic		DGIdb
SCH442416	↓ inhibits	Mechanistic		DGIdb
CVT-6883	↓ inhibits	Mechanistic		DGIdb
NECA	↑ activates	Mechanistic	14.0 nM (Ki)	DGIdb
KF26777	↓ inhibits	Mechanistic		DGIdb

Showing top 40 of 266 agents ranked by evidence tier.

ADRA2A

UniProt Ensembl DGIdb Open Targets

Therapeutic Agent	Effect Direction	Evidence Tier	Potency	Source
FADOLMIDINE HYDROCHLORIDE	↑ activates	Mechanistic		DGIdb
FIPAMEZOLE	↓ inhibits	Mechanistic		DGIdb
ERGOLOID MESYLATES	↓ inhibits	Mechanistic		DGIdb
BRIMONIDINE	↑ activates	Mechanistic		DGIdb
CLONIDINE HYDROCHLORIDE	↑ activates	Mechanistic		DGIdb
ERGOLOID MESYLATES, USP	? unclear	Mechanistic		DGIdb
SODIUM CHLORIDE	? unclear	Mechanistic		DGIdb
NICERGOLINE	? unclear	Mechanistic		DGIdb
YOHIMBINE	↓ inhibits	Mechanistic	0.42 nM (Ki)	DGIdb
DEXMEDETOMIDINE HYDROCHLORIDE	↑ activates	Mechanistic		DGIdb
GUANIDINE HYDROCHLORIDE	? unclear	Mechanistic		DGIdb
MEPERIDINE HYDROCHLORIDE	? unclear	Mechanistic		DGIdb
BRIMONIDINE TARTRATE	↑ activates	Mechanistic		DGIdb
NOREPINEPHRINE	↑ activates	Mechanistic	66.0 nM (Ki)	DGIdb
MK-912	↓ inhibits	Mechanistic		DGIdb
LOFEXIDINE	↑ activates	Mechanistic		DGIdb
PIRIBEDIL	↓ inhibits	Mechanistic		DGIdb
BENZPHETAMINE	? unclear	Mechanistic		DGIdb
[125I]P-IODOCLONIDINE	↑ activates	Mechanistic		DGIdb
GUANFACINE HYDROCHLORIDE	↑ activates	Mechanistic		DGIdb
DOXAZOSIN MESYLATE	? unclear	Mechanistic		DGIdb
EPINEPHRINE	↑ activates	Mechanistic		DGIdb
DROXIDOPA	↑ activates	Mechanistic		DGIdb
PSEUDOEPHEDRINE POLISTIREX	? unclear	Mechanistic		DGIdb
RX821002	↓ inhibits	Mechanistic		DGIdb
MUSCARINIC TOXIN 3	↓ inhibits	Mechanistic		DGIdb
TOLAZOLINE	↓ inhibits	Mechanistic		DGIdb
PHENTOLAMINE	↓ inhibits	Mechanistic	2.6 nM (Ki)	DGIdb
METHYLDOPATE HYDROCHLORIDE	? unclear	Mechanistic		DGIdb
TETRAHYDROZOLINE HYDROCHLORIDE	↑ activates	Mechanistic		DGIdb
DIPIVEFRIN HYDROCHLORIDE	↑ activates	Mechanistic		DGIdb
NAPHAZOLINE HYDROCHLORIDE	↑ activates	Mechanistic		DGIdb
RAUWOLFIA SERPENTINA	↓ inhibits	Mechanistic	8.2 nM (Ki)	DGIdb
GUANABENZ	↑ activates	Mechanistic		DGIdb
ASENAPINE	? unclear	Mechanistic		DGIdb
SPIROXATRINE	↓ inhibits	Mechanistic		DGIdb
GUANABENZ ACETATE	↑ activates	Mechanistic		DGIdb
BRL44408	↓ inhibits	Mechanistic		DGIdb
BETHANIDINE	? unclear	Mechanistic		DGIdb
LOFEXIDINE HYDROCHLORIDE	↑ activates	Mechanistic		DGIdb

Showing top 40 of 281 agents ranked by evidence tier.

ADRB2

UniProt Ensembl DGIdb Open Targets

Therapeutic Agent	Effect Direction	Evidence Tier	Potency	Source
METAPROTERENOL	↑ activates	Mechanistic		DGIdb
PROPRANOLOL HYDROCHLORIDE	↓ inhibits	Mechanistic		DGIdb
OLODATEROL	↑ activates	Mechanistic		DGIdb
TIMOLOL	↓ inhibits	Mechanistic		DGIdb
CHEMBL:CHEMBL1465049	? unclear	Mechanistic		DGIdb
NOREPINEPHRINE	↑ activates	Mechanistic		DGIdb
EPHEDRINE SULFATE	↑ activates	Mechanistic		DGIdb
LEVALBUTEROL	? unclear	Mechanistic		DGIdb
3-O-METHYLQUERCETIN	? unclear	Mechanistic		DGIdb
RISPERIDONE	? unclear	Mechanistic		DGIdb
CLENBUTEROL	↑ activates	Mechanistic		DGIdb
ARFORMOTEROL	? unclear	Mechanistic		DGIdb
CELIPROLOL	↑ activates	Mechanistic		DGIdb
ISOPROTERENOL	↑ activates	Mechanistic	0.1585 nM (EC50)	DGIdb
MEPHENTERMINE SULFATE	↑ activates	Mechanistic		DGIdb
CARVEDILOL	↓ inhibits	Mechanistic		DGIdb
PROCATEROL	↑ activates	Mechanistic		DGIdb
CHEMBL:CHEMBL590927	? unclear	Mechanistic		DGIdb
TERTATOLOL	? unclear	Mechanistic		DGIdb
FENOTEROL	↑ activates	Mechanistic		DGIdb
MEPINDOLOL	? unclear	Mechanistic		DGIdb
PROPAFENONE	↓ inhibits	Mechanistic		DGIdb
CHEMBL:CHEMBL531322	? unclear	Mechanistic		DGIdb
CARMOTEROL	↑ activates	Mechanistic		DGIdb
PINDOLOL	↓ inhibits	Mechanistic		DGIdb
SALMETEROL	↑ activates	Mechanistic		DGIdb
CGP12177	↓ inhibits	Mechanistic		DGIdb
CLENBUTEROL HYDROCHLORIDE	? unclear	Mechanistic		DGIdb
NADOLOL	↓ inhibits	Mechanistic		DGIdb
DESIPRAMINE	? unclear	Mechanistic		DGIdb
CIMATEROL	↑ activates	Mechanistic		DGIdb
FENOTEROL HBR	? unclear	Mechanistic		DGIdb
RITODRINE	? unclear	Mechanistic		DGIdb
PF-00610355	? unclear	Mechanistic		DGIdb
SOTALOL	↓ inhibits	Mechanistic		DGIdb
TERBUTALINE	↑ activates	Mechanistic		DGIdb
LAS190792	↑ activates	Mechanistic		DGIdb
NORADRENALINE	↑ activates	Mechanistic		DGIdb
LEVOBUNOLOL HYDROCHLORIDE	↓ inhibits	Mechanistic		DGIdb
PENBUTOLOL SULFATE	↓ inhibits	Mechanistic		DGIdb

Showing top 40 of 368 agents ranked by evidence tier.

CA2

UniProt Ensembl DGIdb Open Targets

Therapeutic Agent	Effect Direction	Evidence Tier	Potency	Source
GUAIACOL	? unclear	Mechanistic		DGIdb
PHENOL	? unclear	Mechanistic		DGIdb
DORZOLAMIDE HYDROCHLORIDE	? unclear	Mechanistic		DGIdb
BRINZOLAMIDE	↓ inhibits	Mechanistic		DGIdb
ACETAZOLAMIDE	↓ inhibits	Mechanistic	12.0 nM (Ki)	DGIdb
CHLOROTHIAZIDE	? unclear	Mechanistic		DGIdb
SULFAMIDE	? unclear	Mechanistic		DGIdb
DICHLORPHENAMIDE	↓ inhibits	Mechanistic	38.0 nM (Ki)	DGIdb
ETHINAMATE	? unclear	Mechanistic		DGIdb
COMPOUND 5B [PMID: 31287314]	↓ inhibits	Mechanistic		DGIdb
SULTHIAME	↓ inhibits	Mechanistic		DGIdb
RECOMBINANT INTERLEUKIN-3	? unclear	Mechanistic		DGIdb
PARABEN	? unclear	Mechanistic		DGIdb
METHAZOLAMIDE	↓ inhibits	Mechanistic	14.0 nM (Ki)	DGIdb
POLMACOXIB	↓ inhibits	Mechanistic		DGIdb
COMPOUND 11 [PMID: 41150938]	↓ inhibits	Mechanistic		DGIdb
FERULIC ACID	? unclear	Mechanistic		DGIdb
PYROGALLOL	↓ inhibits	Mechanistic		DGIdb
TOPIRAMATE	↓ inhibits	Mechanistic		DGIdb
BENZTHIAZIDE	? unclear	Mechanistic		DGIdb
CYCLOTHIAZIDE	? unclear	Mechanistic		DGIdb
SALVIANOLIC ACID A	↓ inhibits	Mechanistic		DGIdb
MAFENIDE	? unclear	Mechanistic	170.0 nM (Ki)	DGIdb
EPOETIN ALFA	? unclear	Mechanistic		DGIdb
COMPOUND 5A [PMID: 31287314]	↓ inhibits	Mechanistic		DGIdb
DORZOLAMIDE	? unclear	Mechanistic	9.0 nM (Ki)	DGIdb
TRICHLORMETHIAZIDE	? unclear	Mechanistic		DGIdb
ACETAZOLAMIDE SODIUM	↓ inhibits	Mechanistic		DGIdb
CURCUMIN	? unclear	Mechanistic		DGIdb
ETHOXZOLAMIDE	↓ inhibits	Mechanistic	8.0 nM (Ki)	DGIdb
COBALT	? unclear	Mechanistic		DGIdb
CHEMBL268177	↓ inhibits	Mechanistic	70.0 nM (Ki)	ChEMBL
CHEMBL268439	↓ inhibits	Mechanistic	2.0 nM (Ki)	ChEMBL
CHEMBL544127	↓ inhibits	Mechanistic	9.0 nM (IC50)	ChEMBL
CHEMBL148167	↓ inhibits	Mechanistic	1.0 nM (Ki)	ChEMBL
CHEMBL358290	↓ inhibits	Mechanistic	42.0 nM (Ki)	ChEMBL
CHEMBL148426	↓ inhibits	Mechanistic	33.0 nM (Ki)	ChEMBL
CHEMBL144766	↓ inhibits	Mechanistic	13.0 nM (Ki)	ChEMBL
CHEMBL356059	↓ inhibits	Mechanistic	10.0 nM (Ki)	ChEMBL
CHEMBL144970	↓ inhibits	Mechanistic	11.0 nM (Ki)	ChEMBL

Showing top 40 of 174 agents ranked by evidence tier.

CA4

UniProt Ensembl DGIdb Open Targets

Therapeutic Agent	Effect Direction	Evidence Tier	Potency	Source
TOPIRAMATE	↓ inhibits	Mechanistic	4900.0 nM (Ki)	DGIdb
ACETAZOLAMIDE	↓ inhibits	Mechanistic	220.0 nM (Ki)	DGIdb
COMPOUND 5B [PMID: 31287314]	↓ inhibits	Mechanistic		DGIdb
TRICHLORMETHIAZIDE	? unclear	Mechanistic	449.0 nM (Ki)	DGIdb
SULTHIAME	↓ inhibits	Mechanistic		DGIdb
DICHLORPHENAMIDE	↓ inhibits	Mechanistic	15330.0 nM (Ki)	DGIdb
COMPOUND 5A [PMID: 31287314]	↓ inhibits	Mechanistic		DGIdb
ETHOXZOLAMIDE	↓ inhibits	Mechanistic	93.0 nM (Ki)	DGIdb
ACETAZOLAMIDE SODIUM	↓ inhibits	Mechanistic		DGIdb
SALVIANOLIC ACID A	↓ inhibits	Mechanistic		DGIdb
CHLORTHALIDONE	↓ inhibits	Mechanistic	196.0 nM (Ki)	DGIdb
METHAZOLAMIDE	↓ inhibits	Mechanistic	240.0 nM (Ki)	DGIdb
CHLOROTHIAZIDE	? unclear	Mechanistic		DGIdb
CHEMBL289672	↓ inhibits	Mechanistic	550.0 nM (Ki)	ChEMBL
CHEMBL30168	↓ inhibits	Mechanistic	24.0 nM (Ki)	ChEMBL
CHEMBL6753	↓ inhibits	Mechanistic	355.0 nM (Ki)	ChEMBL
CHEMBL34974	↓ inhibits	Mechanistic	265.0 nM (Ki)	ChEMBL
CHEMBL154106	↓ inhibits	Mechanistic	9.0 nM (Ki)	ChEMBL
CHEMBL32732	↓ inhibits	Mechanistic	29.0 nM (Ki)	ChEMBL
CHEMBL289888	↓ inhibits	Mechanistic	19.0 nM (Ki)	ChEMBL
CHEMBL34317	↓ inhibits	Mechanistic	6.0 nM (Ki)	ChEMBL
CHEMBL285516	↓ inhibits	Mechanistic	8.0 nM (Ki)	ChEMBL
CHEMBL6852	↓ inhibits	Mechanistic	2200.0 nM (Ki)	ChEMBL
CHEMBL262389	↓ inhibits	Mechanistic	430.0 nM (Ki)	ChEMBL
CHEMBL32208	↓ inhibits	Mechanistic	25.0 nM (Ki)	ChEMBL
CHEMBL284694	↓ inhibits	Mechanistic	156.0 nM (Ki)	ChEMBL
CHEMBL286586	↓ inhibits	Mechanistic	6.0 nM (Ki)	ChEMBL
CHEMBL2112275	↓ inhibits	Mechanistic	100.0 nM (Ki)	ChEMBL
CHEMBL6705	↓ inhibits	Mechanistic	1310.0 nM (Ki)	ChEMBL
CHEMBL13646	↓ inhibits	Mechanistic	125.0 nM (Ki)	ChEMBL
CHEMBL32096	↓ inhibits	Mechanistic	36.0 nM (Ki)	ChEMBL
CHEMBL34768	↓ inhibits	Mechanistic	27.0 nM (Ki)	ChEMBL
CHEMBL32982	↓ inhibits	Mechanistic	29.0 nM (Ki)	ChEMBL
CHEMBL7204	↓ inhibits	Mechanistic	3200.0 nM (Ki)	ChEMBL
DORZOLAMIDE	↓ inhibits	Mechanistic	43.0 nM (Ki)	ChEMBL
CHEMBL286449	↓ inhibits	Mechanistic	37.0 nM (Ki)	ChEMBL
CHEMBL286297	↓ inhibits	Mechanistic	40.0 nM (Ki)	ChEMBL
CHEMBL287316	↓ inhibits	Mechanistic	21.0 nM (Ki)	ChEMBL
CHEMBL32836	↓ inhibits	Mechanistic	180.0 nM (Ki)	ChEMBL
CHEMBL1795062	↓ inhibits	Mechanistic	16.0 nM (Ki)	ChEMBL

Showing top 40 of 151 agents ranked by evidence tier.

CHRM3

UniProt Ensembl DGIdb Open Targets

Therapeutic Agent	Effect Direction	Evidence Tier	Potency	Source
OCTOTROPINE METHYLBROMIDE	↓ inhibits	Mechanistic		DGIdb
TIOTROPIUM	↓ inhibits	Mechanistic		DGIdb
BETHANECHOL CHLORIDE	↑ activates	Mechanistic		DGIdb
GLYCOPYRRONIUM TOSYLATE	↓ inhibits	Mechanistic		DGIdb
REVEFENACIN	↓ inhibits	Mechanistic		DGIdb
OXYBUTYNIN	↓ inhibits	Mechanistic		DGIdb
MUSCARINIC TOXIN 7	↓ inhibits	Mechanistic		DGIdb
SOLIFENACIN	↓ inhibits	Mechanistic		DGIdb
ZAMIFENACIN	? unclear	Mechanistic		DGIdb
UMECLIDINIUM BROMIDE	↓ inhibits	Mechanistic		DGIdb
ACLIDINIUM	↓ inhibits	Mechanistic		DGIdb
PROPIOMAZINE	? unclear	Mechanistic		DGIdb
(S)-DIMETINDENE	↓ inhibits	Mechanistic		DGIdb
TERODILINE HYDROCHLORIDE	↓ inhibits	Mechanistic		DGIdb
IPRATROPIUM CATION	↓ inhibits	Mechanistic		DGIdb
PENTYLTHIO-TZTP	↑ activates	Mechanistic		DGIdb
CARBAMOYLCHOLINE	↑ activates	Mechanistic		DGIdb
IPRATROPIUM BROMIDE	↓ inhibits	Mechanistic		DGIdb
DIPHENIDOL	? unclear	Mechanistic		DGIdb
METHYLHOMATROPINE	? unclear	Mechanistic		DGIdb
PROMAZINE	? unclear	Mechanistic		DGIdb
METHSCOPOLAMINE BROMIDE	↓ inhibits	Mechanistic		DGIdb
ACETYLCHOLINE CHLORIDE	↑ activates	Mechanistic		DGIdb
TROPICAMIDE	↓ inhibits	Mechanistic		DGIdb
AZD8683	↓ inhibits	Mechanistic		DGIdb
PIPERTRAMINE	? unclear	Mechanistic		DGIdb
TRIDIHEXETHYL	? unclear	Mechanistic		DGIdb
MEPENZOLATE BROMIDE	↓ inhibits	Mechanistic		DGIdb
TOLTERODINE	↓ inhibits	Mechanistic		DGIdb
FESOTERODINE	? unclear	Mechanistic		DGIdb
HEXOCYCLIUM METHYLSULFATE	↓ inhibits	Mechanistic		DGIdb
SUCCINYLCHOLINE	? unclear	Mechanistic		DGIdb
OLANZAPINE	? unclear	Mechanistic		DGIdb
SOFPIRONIUM BROMIDE	↓ inhibits	Mechanistic		DGIdb
[3H]TIOTROPIUM	↓ inhibits	Mechanistic		DGIdb
ML381	↓ inhibits	Mechanistic		DGIdb
PIPERTRAMINE AMIDE	? unclear	Mechanistic		DGIdb
MEPENZOLATE	↓ inhibits	Mechanistic		DGIdb
ACECLIDINE	↑ activates	Mechanistic		DGIdb
OXOTREMORINE	↑ activates	Mechanistic	210.0 nM (EC50)	DGIdb

Showing top 40 of 333 agents ranked by evidence tier.

MYOC

UniProt Ensembl DGIdb Open Targets

Therapeutic Agent	Effect Direction	Evidence Tier	Potency	Source
CHEMBL1384068	↓ inhibits	Mechanistic	11000.0 nM (Kd)	ChEMBL
CHEMBL1432046	↓ inhibits	Mechanistic	650.0 nM (Kd)	ChEMBL
CHEMBL339587	↓ inhibits	Mechanistic	99.0 nM (Kd)	ChEMBL
APIGENIN	↓ inhibits	Mechanistic	41600.0 nM (Kd)	ChEMBL
GW305074X	↓ inhibits	Mechanistic	33500.0 nM (Kd)	ChEMBL

OPTN

UniProt Ensembl DGIdb Open Targets

Pipeline results not yet available for this target. Run the pipeline to populate.

PTGFR

UniProt Ensembl DGIdb Open Targets

Therapeutic Agent	Effect Direction	Evidence Tier	Potency	Source
MB-28767	↑ activates	Mechanistic		DGIdb
SEPETAPROST	↑ activates	Mechanistic		DGIdb
TRAVOPROST	↑ activates	Mechanistic		DGIdb
BIMATOPROST	↑ activates	Mechanistic		DGIdb
LATANOPROST	↑ activates	Mechanistic		DGIdb
DINOPROSTONE	↑ activates	Mechanistic	250.0 nM (EC50)	DGIdb
DINOPROST TROMETHAMINE	↑ activates	Mechanistic		DGIdb
DINOPROST	↑ activates	Mechanistic	43.0 nM (IC50)	DGIdb
BAY-6672	↓ inhibits	Mechanistic	22.0 nM (IC50)	DGIdb
ENPROSTIL	↑ activates	Mechanistic		DGIdb
BIMATOPROST (FREE ACID FORM)	↑ activates	Mechanistic		DGIdb
ILOPROST	↑ activates	Mechanistic		DGIdb
CLOPROSTENOL	↑ activates	Mechanistic	2.0 nM (IC50)	DGIdb
LAROPIPRANT	? unclear	Mechanistic	9991.0 nM (Ki)	DGIdb
LATANOPROST (FREE ACID FORM)	↑ activates	Mechanistic		DGIdb
AL-12182	↑ activates	Mechanistic		DGIdb
TAFLUPROST	↑ activates	Mechanistic		DGIdb
13,14-DIHYDRO-16-M-CHLOROPHENOXY-W-TETRANOR-PGF1&ALPHA;	↑ activates	Mechanistic		DGIdb
AS604872	↓ inhibits	Mechanistic		DGIdb
CARBOPROST TROMETHAMINE	↑ activates	Mechanistic		DGIdb
PGD2	↑ activates	Mechanistic		DGIdb
L-888,607	↑ activates	Mechanistic		DGIdb
SULPROSTONE	↑ activates	Mechanistic		DGIdb
CARBACYCLIN	↑ activates	Mechanistic		DGIdb
[3H]PGF2&ALPHA;	↑ activates	Mechanistic		DGIdb
U46619	↑ activates	Mechanistic		DGIdb
BUTAPROST	? unclear	Mechanistic		DGIdb
FLUPROSTENOL	↑ activates	Mechanistic	3.6 nM (EC50)	DGIdb
LATANOPROSTENE BUNOD	↑ activates	Mechanistic		DGIdb
TAFLUPROST ACID	↑ activates	Mechanistic		DGIdb
AL12180	↑ activates	Mechanistic		DGIdb
CARBOPROST	? unclear	Mechanistic		Open Targets
CHEMBL88974	↓ inhibits	Mechanistic	330.0 nM (IC50)	ChEMBL
CHEMBL88275	↓ inhibits	Mechanistic	32.0 nM (IC50)	ChEMBL
CHEMBL315519	↓ inhibits	Mechanistic	6100.0 nM (IC50)	ChEMBL
CHEMBL89096	↓ inhibits	Mechanistic	11000.0 nM (IC50)	ChEMBL
CHEMBL90450	↓ inhibits	Mechanistic	350.0 nM (IC50)	ChEMBL
CHEMBL2114230	↓ inhibits	Mechanistic	71.0 nM (IC50)	ChEMBL
CHEMBL173499	↓ inhibits	Mechanistic	29.0 nM (IC50)	ChEMBL
CHEMBL434173	↓ inhibits	Mechanistic	90.0 nM (IC50)	ChEMBL

Showing top 40 of 191 agents ranked by evidence tier.

ROCK1

UniProt Ensembl DGIdb Open Targets

Therapeutic Agent	Effect Direction	Evidence Tier	Potency	Source
BELUMOSUDIL MESYLATE	↓ inhibits	Mechanistic		DGIdb
ALSTERPAULLONE	? unclear	Mechanistic		DGIdb
COMPOUND 8 [PMID: 17480064]	? unclear	Mechanistic		DGIdb
CYC-116	? unclear	Mechanistic		DGIdb
GSK180736A	↓ inhibits	Mechanistic		DGIdb
FASUDIL	↓ inhibits	Mechanistic	530.0 nM (Ki)	DGIdb
CENISERTIB	? unclear	Mechanistic		DGIdb
NETARSUDIL DIMESYLATE	↓ inhibits	Mechanistic		DGIdb
JNJ-7706621	? unclear	Mechanistic		DGIdb
AT-13148	↓ inhibits	Mechanistic		DGIdb
SP-600125	? unclear	Mechanistic		DGIdb
CORTISTATIN A	↓ inhibits	Mechanistic		DGIdb
PF-562271	? unclear	Mechanistic		DGIdb
CHEMBL:CHEMBL1997335	? unclear	Mechanistic		DGIdb
Y-39983	↓ inhibits	Mechanistic		DGIdb
LAUROGUADINE	? unclear	Mechanistic		DGIdb
DE-104	↓ inhibits	Mechanistic		DGIdb
GSK269962A	↓ inhibits	Mechanistic		DGIdb
BAY 61-3606	? unclear	Mechanistic		DGIdb
NETARSUDIL	↓ inhibits	Mechanistic		DGIdb
COMPOUND 33 [PMID: 19364658]	↓ inhibits	Mechanistic		DGIdb
RKI-1447	↓ inhibits	Mechanistic		DGIdb
ROCK INHIBITOR 3	↓ inhibits	Mechanistic		DGIdb
GSK429286A	↓ inhibits	Mechanistic		DGIdb
SAR-407899	↓ inhibits	Mechanistic		DGIdb
LINIFANIB	? unclear	Mechanistic		DGIdb
CHEMBL:CHEMBL546797	? unclear	Mechanistic		DGIdb
VX-702	? unclear	Mechanistic		DGIdb
VEROSUDIL	↓ inhibits	Mechanistic		DGIdb
G&OUML; 6976	? unclear	Mechanistic		DGIdb
HSD1590	↓ inhibits	Mechanistic		DGIdb
BELUMOSUDIL	↓ inhibits	Mechanistic		DGIdb
COMPOUND E22 [PMID: 31298542]	↓ inhibits	Mechanistic		DGIdb
KENPAULLONE	? unclear	Mechanistic		DGIdb
GW441756X	? unclear	Mechanistic		DGIdb
NINVOSUDIL	↓ inhibits	Mechanistic		DGIdb
COMPOUND 35 [PMID: 20684608]	↓ inhibits	Mechanistic		DGIdb
CHEMBL:CHEMBL365617	? unclear	Mechanistic		DGIdb
ILORASERTIB	? unclear	Mechanistic		DGIdb
NVP-TAE684	? unclear	Mechanistic		DGIdb

Showing top 40 of 228 agents ranked by evidence tier.

ROCK2

UniProt Ensembl DGIdb Open Targets

Therapeutic Agent	Effect Direction	Evidence Tier	Potency	Source
G&OUML; 6976	? unclear	Mechanistic		DGIdb
NINVOSUDIL	↓ inhibits	Mechanistic		DGIdb
PF-562271	? unclear	Mechanistic		DGIdb
CHEMBL:CHEMBL365617	? unclear	Mechanistic		DGIdb
AT-13148	↓ inhibits	Mechanistic		DGIdb
GSK269962A	↓ inhibits	Mechanistic		DGIdb
HSD1590	↓ inhibits	Mechanistic		DGIdb
ZM447439	? unclear	Mechanistic		DGIdb
FASUDIL	↓ inhibits	Mechanistic	1900.0 nM (IC50)	DGIdb
COMPOUND 32 [PMID: 20471253]	↓ inhibits	Mechanistic		DGIdb
SAR407899	↓ inhibits	Mechanistic		DGIdb
SP-600125	? unclear	Mechanistic		DGIdb
PH-797804	? unclear	Mechanistic		DGIdb
DE-104	↓ inhibits	Mechanistic		DGIdb
ROCK INHIBITOR 3	↓ inhibits	Mechanistic		DGIdb
SNS-314	? unclear	Mechanistic		DGIdb
CENISERTIB	? unclear	Mechanistic		DGIdb
NETARSUDIL DIMESYLATE	↓ inhibits	Mechanistic		DGIdb
CYC-116	? unclear	Mechanistic		DGIdb
NVP-TAE684	? unclear	Mechanistic		DGIdb
RHO KINASE INHIBITOR IV	↓ inhibits	Mechanistic		DGIdb
PROGESTERONE	? unclear	Mechanistic		DGIdb
COMPOUND 8 [PMID: 25898023]	↓ inhibits	Mechanistic		DGIdb
SAR-407899	↓ inhibits	Mechanistic		DGIdb
AMA0076	↓ inhibits	Mechanistic		DGIdb
SOVESUDIL	↓ inhibits	Mechanistic		DGIdb
COMPOUND 22 [PMID: 20462760]	↓ inhibits	Mechanistic		DGIdb
VEROSUDIL	↓ inhibits	Mechanistic		DGIdb
KENPAULLONE	? unclear	Mechanistic		DGIdb
RIPASUDIL	↓ inhibits	Mechanistic		DGIdb
LAUROGUADINE	? unclear	Mechanistic		DGIdb
THROMBIN ALFA	? unclear	Mechanistic		DGIdb
BELUMOSUDIL MESYLATE	↓ inhibits	Mechanistic		DGIdb
NETARSUDIL	↓ inhibits	Mechanistic		DGIdb
VANDETANIB	? unclear	Mechanistic		DGIdb
RKI-1447	↓ inhibits	Mechanistic		DGIdb
GW441756X	? unclear	Mechanistic		DGIdb
CORTISTATIN A	↓ inhibits	Mechanistic		DGIdb
AST-487	? unclear	Mechanistic		DGIdb
COMPOUND 11D [DOI: 10.1039/C0MD00194E]	↓ inhibits	Mechanistic		DGIdb

Showing top 40 of 209 agents ranked by evidence tier.

Clinical Trials

Drug, biologic and supplement trials (treatment or prevention) from ClinicalTrials.gov whose main condition is Glaucoma: recruiting, active or completed, most recently updated first. Data retrieved 2026-10-28.

A Study About the Safety of ASP2767 and Whether it Helps People With Glaucoma-Related Optic Nerve Damage Recruiting

NCT07770685 Phase: 1/2 Started: 2026-10-07

Open-angle glaucoma is the most common type of glaucoma, a disease that damages the nerves in the eye and can lead to vision loss. Current treatments include eye drops, laser treatment, and surgery that help lower eye pressure. However, they do not work for everyone, and the disease may continue to ...

Topical Insulin for Glaucoma Recruiting

NCT05206877 Phase: 1 Started: 2022-04-01

The purpose of this Phase 1 trial is to determine the safety over 1-2 months of topic sterile human recombinant insulin on subjects with optic neuropathies (glaucoma, ischecmic optic neuropathy, and optic disc drusen).

Unravelling the Effects of Nicotinamide/Pyrroloquinolone Quinone /Citicoline/Homotaurine Fixed Combination on Contrast Sensitivity, Quality of Life, and Reading Performance in Glaucoma Completed

NCT07861243 Phase: N/A Started: 2025-11-01

Glaucoma is a chronic, progressive neuro-ophthalmic condition that leads to irreversible loss of retinal ganglion cells (RGCs) and is the second leading cause of blindness worldwide. It is associated with elevated intraocular pressure (IOP), but many patients continue to experience vision loss even ...

REGN22530 for Adults With Primary Open Angle Glaucoma or Ocular Hypertension Recruiting

NCT07675824 Phase: 1/2 Started: 2026-09-08

This study will test an experimental drug called REGN22530 ("study drug") to see if it can help treat people with primary open angle glaucoma or ocular hypertension. REGN22530 is an experimental drug that is designed to bind with a protein in the eye that has been shown to cause a buildup of fluid i...

A Study to Evaluate Efficacy and Safety of YSBP Compared to Lumigan in Patients With Glaucoma or Ocular Hypertension Recruiting

NCT07661329 Phase: 3 Started: 2026-06-02

This study is to establish non-inferiority of a preservative free formulation of Bimatoprost ophthalmic solution 0.01% (YSBP) of YS Life Science Co., Ltd. compared to LUMIGAN® (bimatoprost ophthalmic solution) 0.01% of AbbVie INC in subjects with primary open angle glaucoma (POAG) or ocular hyperten...

Phase 2 Trial to Evaluate the Safety and Efficacy of the Second Generation Travoprost Intracameral Implant Recruiting

NCT07075718 Phase: 2 Started: 2025-06-12

Evaluate the Safety and Efficacy of the Second Generation Travoprost Intracameral Implant

A Phase II Trial of G01 Eye Drops for Glaucomatous Optic Neuropathy Recruiting

NCT07777861 Phase: 2 Started: 2026-03-18

This is a randomized, double-masked, placebo-controlled Phase II clinical trial. The primary objective is to explore the efficacy of G01 Eye Drops in the treatment of optic nerve injury associated with open-angle glaucoma, providing supportive evidence for the design of subsequent clinical trials. T...

Study of QLS-111-FDC in Open-Angle Glaucoma or Ocular Hypertension Completed

NCT07354516 Phase: 2/3 Started: 2026-03-18

Firecrest study is evaluating the intraocular pressure (IOP)-lowering effect, safety, and tolerability of Qlaris' preservative free \[PF\], fixed-dose combination \[FDC\] investigational product (IP) in subjects with open-angle glaucoma (OAG) or ocular hypertension (OHT).

Phase 2 Study of BL1107 Eye Drops vs. Timolol in Adults With Primary Open Angle Glaucoma or Ocular Hypertension Completed

NCT07168902 Phase: 2 Started: 2025-10-24

Phase 2 Study of BL1107 Eye Drops vs. Timolol in Adults with Primary Open Angle Glaucoma or Ocular Hypertension

Long-term Safety and Efficacy Extension Trial of Bimatoprost SR Completed

NCT03891446 Phase: 3 Started: 2019-03-27

This study will evaluate the long-term safety and efficacy of Bimatoprost Sustained Release (SR) in patients with open-angle glaucoma or ocular hypertension who completed 1 of the 4 Phase 3 Bimatoprost SR studies (192024-091, -092, -093, or -095) and received Bimatoprost SR or who received commercia...

Evaluate Efficacy and Safety of PA5108 Ocular Implants in Primary Open Angle Glaucoma or Ocular Hypertension Active Not Recruiting

NCT06964191 Phase: 2 Started: 2025-05-31

The goal of this clinical trial is to determine the dose of PA5108 Ocular Implant that is effective and safe for the reduction of intraocular pressure in adult patients with open-angle glaucoma or ocular hypertension, compared to the standard treatment therapy.

[KJ-TFC-005] Phase 3 Study, Evaluate the Efficacy and Safety of TFC-003 in Patients With Primary Open-Angle Glaucoma or Ocular Hypertension Recruiting

NCT07662759 Phase: 3 Started: 2025-12-09

\[KJ-TFC-005\] Phase 3 Study, Evaluate the Efficacy and Safety of TFC-003 in Patients With Primary Open-Angle Glaucoma or Ocular Hypertension

Effect of Rhopressa on Intraocular Pressure (IOP) in Patients With Primary Open-Angle Glaucoma or Ocular Hypertension Post-SLT Active Not Recruiting

NCT06865144 Phase: 4 Started: 2025-06-27

The purpose of this study is to collect data about how Rhopressa affects IOP in patients who have had an SLT procedure in both eyes.

AGN-193408 SR in the Treatment of Open-angle Glaucoma or Ocular Hypertension Active Not Recruiting

NCT04499248 Phase: 1/2 Started: 2020-11-16

This is a multicenter, open-label, dose escalation (Cohort 1) to masked, randomized, parallel-groups (Cohort 2) and (Cohort 3) study to evaluate the safety and efficacy of AGN-193408 SR in participants with open-angle glaucoma or ocular hypertension

A Phase III Study in Subjects With Primary Open Angle Glaucoma or Ocular Hypertension in China Active Not Recruiting

NCT06666855 Phase: 3 Started: 2024-11-28

This is a Phase III Study that includes a single arm, open-label, multi-dose PK study cohort and a randomized, evaluator-masked, active drug-control multicenter study. Subjects diagnosed with POAG (Primary Open Angle Glaucoma) or OHT (Ocular Hypertension) who meet eligibility criteria will washout o...

Agents Found By Disease-Level Search

Searched directly from “Glaucoma” via ClinicalTrials.gov interventions and Open Targets' disease→drug data — independent of the 11-gene target panel above. This surfaces agents whose mechanism doesn't route through a curated gene (combination therapies, standard-of-care drugs, targets outside the panel).

50 agents shown (approved or with trial evidence) — 47 not found by the gene-target search above.

Latanoprost

Approved · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT02622334 NCT02531152 NCT01175902

SENSIMED TriggerfishNOT in gene-target list

· 3 trials · source: ClinicalTrials.gov
NCT01028664 NCT00966108 NCT01347229

TrabeculectomyNOT in gene-target list

· 3 trials · source: ClinicalTrials.gov
NCT00666237 NCT05340647 NCT04727411

BevacizumabNOT in gene-target list

Phase 3 · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT01263834 NCT01166594

Mitomycin CNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT01263834 NCT00666237

timolol maleate 0.5%NOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT00273481 NCT00735449

Netarsudil

Approved · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT06449352

Brimonidine

Approved · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT06449352

RO5093151NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02622334

portable CCTVNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01262209

Telescopes, telemicroscopes and microscopesNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01262209

Absorptive filtersNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01262209

VISION5 ProductNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01943721

dorzolamide-timolol-brimonidineNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01062971

OPC-1085EL ophthalmic solutionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02105272

Latanoprost ophthalmic solutionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02105272

BrudyGlaucoNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07322965

Travoprost 0.004% BAK-freeNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01510145

SD-OCT AngiographyNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03109665

SD-OCTNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03109665

Determining quality of lifeNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03967145

Corneal topography: OPD-ScanNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04602923

Corneal topography: PentacamNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04602923

SOLX Gold ShuntNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01282346

Bimatoprost (SR)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03850782

TEMPO iMOvifaNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06186388

Value Pricing SubsidiesNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02271269

ASOCTNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05209204

PentacamNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05209204

Travoprost 0.004% ophthalmic solutionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01464424

Bimatoprost 0.01% ophthalmic solutionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01464424

CiticolineNOT in gene-target list

Phase 3 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT07567651

Phacoemulsification with GoniosynechialysisNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06952153

Trabeculectomy with 5FUNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06952153

DE-117 ophthalmic solutionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02822729

Timolol ophthalmic solutionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02822729

DE-126 Ophthalmic Solution 0.002% QDNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04742283

Timolol Maleate Ophthalmic Solution 0.5% BIDNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04742283

physical activityNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07599241

Bimatoprost 0.03%, LatanoprostNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00347841

travoprost 0.004% (drug)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00308945

latanoprost 0.005% (drug)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00308945

Ginkgo bilobaNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02376114

dorzolamide 2%/timolol maleate 0.5% fixed combinationNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00273481

latanoprost 0.005%/timolol maleate 0.5% fixed combinationNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00273481

DSLT enables newly diagnosed patients to remain well controlled and off medicationsNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06933836

Virtual Reality Visual Field (VR-VF)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07063537

dorzolamide/timololNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01175902

PhacoemulsificationNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02049333

Endoscopic Cycloplasty (ECPL)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02049333

Generated by the Open Source Medicine Foundation Biomarker Pipeline — 2026-10-08. Data sources: DGIdb, Open Targets, ChEMBL, PubMed, ClinicalTrials.gov. Not medical advice.

Glaucoma

Remission & chronicity

Biomarker Targets & Therapeutic Agents

ADORA1

ADRA2A

ADRB2

CA2

CA4

CHRM3

MYOC

OPTN

PTGFR

ROCK1

ROCK2

Clinical Trials

Agents Found By Disease-Level Search

The research patients need, made open source.

Conditions

Data

Tools

Foundation