Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM5TC43)

Drug Name

AR-12286 Drug Info

Synonyms

AR-11236; AR-12080; AR-12132; CF-286-03; CF-286-04

Indication

Disease Entry	ICD 11	Status	REF
Glaucoma/ocular hypertension	9C61	Phase 2	[1]

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Patented Agent(s)

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Drug(s) Targeting Rho-associated protein kinase (ROCK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Netarsudil	DM0LPI9	Open-angle glaucoma	9C61	Approved	[3]
Ximelegatran	DMU8ANS	Myocardial infarction	BA41-BA43	Approved	[4]
Roclatan	DMVQ5X1	Glaucoma/ocular hypertension	9C61	Phase 3	[5]
AMA-76	DMBWNX5	Glaucoma/ocular hypertension	9C61	Phase 2	[6]
Cethrin	DMD3XMW	Spinal cord injury	ND51.2	Phase 1/2	[7]
Y-39983	DMXSEHF	Glaucoma/ocular hypertension	9C61	Phase 1/2	[8]
STM 434	DMDF29A	Ovarian cancer	2C73	Phase 1	[9]
AT13148	DMYIPKJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
Hexahydro azepinone derivative 1	DMC1ZIX	N. A.	N. A.	Patented	[9]
Isoquinoline sulfonyl derivative 2	DMT5E7M	N. A.	N. A.	Patented	[9]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Rho-associated protein kinase (ROCK)	TTMQO60	NOUNIPROTAC	Modulator	[2]

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References

1	ClinicalTrials.gov (NCT01699464) A Study Assessing the Safety and Ocular Hypotensive Efficacy of AR-12286 in Patients With Elevated Intraocular Pressure for 3 Months. U.S. National Institutes of Health.
2	Ocular hypotensive effect of the Rho kinase inhibitor AR-12286 in patients with glaucoma and ocular hypertension. Am J Ophthalmol. 2011 Nov;152(5):834-41.e1.
3	Effect of 0.04% AR-13324, a ROCK, and norepinephrine transporter inhibitor, on aqueous humor dynamics in normotensive monkey eyes. J Glaucoma. 2015 Jan;24(1):51-4.
4	Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.
5	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
6	AMA0076, a novel, locally acting Rho kinase inhibitor, potently lowers intraocular pressure in New Zealand white rabbits with minimal hyperemia. Invest Ophthalmol Vis Sci. 2014 Feb 18;55(2):1006-16.
7	A phase I/IIa clinical trial of a recombinant Rho protein antagonist in acute spinal cord injury. J Neurotrauma. 2011 May;28(5):787-96.
8	Effects of Y-39983, a selective Rho-associated protein kinase inhibitor, on blood flow in optic nerve head in rabbits and axonal regeneration of retinal ganglion cells in rats.Curr Eye Res. 2011 Oct;36(10):964-70.
9	Rho kinase inhibitors: a patent review (2014 - 2016).Expert Opin Ther Pat. 2017 Apr;27(4):507-515.
10	Company report (Astex)