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

General Information of Drug (ID: DM0LPI9)

• Drug Name: Netarsudil Drug Info
• Synonyms: UNII-W6I5QDT7QI; W6I5QDT7QI; Netarsudil mesylate; Netarsudil [USAN]; AR-11324 free base; Netarsudil [USAN:INN]; Netarsudil (USAN/INN); GTPL9322; SCHEMBL16036278; ZINC113149554; AR11324; AR-11324; ester 60; 1628418-15-4

Indication

Disease Entry	ICD 11	Status	REF
Open-angle glaucoma	9C61	Approved	[1]
Glaucoma/ocular hypertension	9C61	Phase 2	[2]

• Cross-matching ID:
  PubChem CID: 66599893
  CAS Number: CAS 1254032-66-0
  TTD Drug ID: DM0LPI9
  ACDINA Drug ID: D01281

Molecule-Related Drug Atlas

Drug(s) Targeting Norepinephrine transporter (NET)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[3]
Amitriptyline	DMK7F9S	Depression	6A70-6A7Z	Approved	[4]
Imipramine	DM2NUH3	Depression	6A70-6A7Z	Approved	[5]
Desipramine	DMT2FDC	Attention deficit hyperactivity disorder	6A05.Z	Approved	[3]
Cocaine	DMSOX7I	Anaesthesia	9A78.6	Approved	[6]
Bupropion	DM5PCS7	Depression	6A70-6A7Z	Approved	[7]
Tapentadol hydrochloride	DMXLSH3	Acute pain	MG31	Approved	[8]
Venlafaxine	DMR6QH0	Anxiety disorder	6B00-6B0Z	Approved	[7]
Trimipramine	DM1SC8M	Major depressive disorder	6A70.3	Approved	[9]
Duloxetine	DM9BI7M	Depression	6A70-6A7Z	Approved	[10]

Drug(s) Targeting Rho-associated protein kinase 1 (ROCK1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SAR-407899	DMF95KD	Diabetic nephropathy	GB61.Z	Phase 2	[11]
H-1152	DM8XH3S	Pulmonary arterial hypertension	BB01.0	Phase 2	[12]
INS-117548	DMA46DO	Glaucoma/ocular hypertension	9C61	Phase 1	[13]
GSK269962A	DM5I2HL	Inflammation	1A00-CA43.1	Clinical trial	[14]
PMID28048944-Compound-19	DMPT3V9	N. A.	N. A.	Patented	[15]
PMID28048944-Compound-3	DM1BN74	N. A.	N. A.	Patented	[15]
PMID28048944-Compound-7	DMXZ368	N. A.	N. A.	Patented	[15]
PMID28048944-Compound-4	DMJAUWG	N. A.	N. A.	Patented	[15]
PMID28048944-Compound-5	DMAB987	N. A.	N. A.	Patented	[15]
PMID28048944-Compound-6	DM5RCBV	N. A.	N. A.	Patented	[15]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ximelegatran	DMU8ANS	Myocardial infarction	BA41-BA43	Approved	[16]
Roclatan	DMVQ5X1	Glaucoma/ocular hypertension	9C61	Phase 3	[13]
AR-12286	DM5TC43	Glaucoma/ocular hypertension	9C61	Phase 2	[17]
AMA-76	DMBWNX5	Glaucoma/ocular hypertension	9C61	Phase 2	[18]
Cethrin	DMD3XMW	Spinal cord injury	ND51.2	Phase 1/2	[19]
Y-39983	DMXSEHF	Glaucoma/ocular hypertension	9C61	Phase 1/2	[20]
STM 434	DMDF29A	Ovarian cancer	2C73	Phase 1	[15]
AT13148	DMYIPKJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[21]
Hexahydro azepinone derivative 1	DMC1ZIX	N. A.	N. A.	Patented	[15]
Isoquinoline sulfonyl derivative 2	DMT5E7M	N. A.	N. A.	Patented	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Norepinephrine transporter (NET)	TTAWNKZ	SC6A2_HUMAN	Modulator	[2]
Rho-associated protein kinase (ROCK)	TTMQO60	NOUNIPROTAC	Modulator	[2]
Rho-associated protein kinase 1 (ROCK1)	TTZN7RP	ROCK1_HUMAN	Inhibitor	[1]

References

• [1] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [2] 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.
• [3] Augmentation effect of combination therapy of aripiprazole and antidepressants on forced swimming test in mice. Psychopharmacology (Berl). 2009 Sep;206(1):97-107.
• [4] Treatment of comorbid pain with serotonin norepinephrine reuptake inhibitors. CNS Spectr. 2008 Jul;13(7 Suppl 11):22-6.
• [5] Invivo antioxidant status: a putative target of antidepressant action. Prog Neuropsychopharmacol Biol Psychiatry. 2009 Mar 17;33(2):220-8.
• [6] Differential involvement of the norepinephrine, serotonin and dopamine reuptake transporter proteins in cocaine-induced taste aversion. Pharmacol Biochem Behav. 2009 Jul;93(1):75-81.
• [7] Clinically relevant drug interactions with new generation antidepressants and antipsychotics. Ther Umsch. 2009 Jun;66(6):485-92.
• [8] 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
• [9] Antidepressants suppress production of the Th1 cytokine interferon-gamma, independent of monoamine transporter blockade. Eur Neuropsychopharmacol. 2006 Oct;16(7):481-90.
• [10] Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42.
• [11] The Rho kinase inhibitor SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. J Hypertens. 2012 May;30(5):980-9.
• [12] Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
• [13] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [14] Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98.
• [15] Rho kinase inhibitors: a patent review (2014 - 2016).Expert Opin Ther Pat. 2017 Apr;27(4):507-515.
• [16] Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.
• [17] 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.
• [18] 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.
• [19] 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.
• [20] 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.
• [21] Company report (Astex)