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

General Information of Drug (ID: DMSUFW6)

• Drug Name: SSR-125047 Drug Info
• Synonyms: Tolrestat; TOLRESTAT; 82964-04-3; Alredase; Lorestat; Tolrestatin; Tolrestatum; Tolrestatum [Latin]; AY-27773; 2-(6-Methoxy-N-methyl-5-(trifluoromethyl)naphthalene-1-carbothioamido)acetic acid; UNII-0T93LG5NMK; AY 27773; AY-27,773; CHEMBL436; 0T93LG5NMK; CHEBI:48549; LUBHDINQXIHVLS-UHFFFAOYSA-N; N-{[6-methoxy-5-(trifluoromethyl)naphthalen-1-yl]carbonothioyl}-N-methylglycine; NCGC00183862-01; N-(6-Methoxythio-5-(trifluoromethyl)-1-naphthoyl)sarcosine; N-{[6-methoxy-5-(trifluoromethyl)-1-naphthyl]carbonothioyl}-N-methylglycine

Indication

Disease Entry	ICD 11	Status	REF
Schizophrenia	6A20	Phase 1	[1]
Diabetic cataract	9B10.21	Withdrawn from market	[2]

• Cross-matching ID:
  PubChem CID: 53359
  ChEBI ID: CHEBI:48549
  CAS Number: CAS 82964-04-3
  TTD Drug ID: DMSUFW6

Molecule-Related Drug Atlas

Drug(s) Targeting Aldose reductase (AKR1B1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Epalrestat	DM5OGK0	Diabetic neuropathy	8C0Z	Approved	[4]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[5]
Fidarestat	DMZL1I8	Diabetic complication	5A2Y	Phase 3	[6]
Ranirestat	DMD5QRS	Diabetic neuropathy	8C0Z	Phase 3	[7]
CONTIGOSIDE B	DMX9V8K	Thrombosis	DB61-GB90	Phase 2/3	[8]
BNV-222	DMYFQJL	Diabetic neuropathy	8C0Z	Phase 2/3	[7]
BNV-222	DMYFQJL	Diabetic neuropathy	8C0Z	Phase 2/3	[9]
LIDORESTAT	DMA0RI9	Diabetic complication	5A2Y	Phase 2	[10]
QR-333	DMKVIWM	Diabetic neuropathy	8C0Z	Phase 2	[11]
ADMVA	DM819CO	Diabetic complication	5A2Y	Phase 2	[7]

Drug(s) Targeting Opioid receptor sigma 1 (OPRS1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dextromethorphan	DMUDJZM	Allergic rhinitis	CA08.0	Approved	[12]
Dextromethorphan Polistirex	DMEHCY5	Dry cough	MD12	Approved	[13]
CM-2395	DMASPWR	Schizophrenia	6A20	Phase 3	[14]
AVP-786	DMV1SOR	Alzheimer disease	8A20	Phase 3	[15]
ADX N05	DMLBYRA	Mood disorder	6A60-6E23	Phase 3	[16]
Igmesine	DMH97XA	Major depressive disorder	6A70.3	Phase 2	[17]
OPC-14523	DMB1WF3	Bulimia nervosa	6B81	Phase 2	[18]
ANAVEX 2-73	DM67OU4	Alzheimer disease	8A20	Phase 1	[19]
SA-5845	DM6XZRL	Central nervous system disease	8A04-8D87	Phase 1	[20]
SSR-125329A	DMG6NI8	Immune System disease	4A01-4B41	Phase 1	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Aldose reductase (AKR1B1)	TTFBNVI	ALDR_HUMAN	Inhibitor	[3]
Opioid receptor sigma 1 (OPRS1)	TT5TPI6	SGMR1_HUMAN	Binder	[1]

References

• [1] The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
• [2] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7404).
• [3] Aldose reductase inhibitors: an update. Ann Pharmacother. 1993 Jun;27(6):751-4.
• [4] Long-term effect of epalrestat, an aldose reductase inhibitor, on the development of incipient diabetic nephropathy in Type 2 diabetic patients. J Diabetes Complications. 2001 Sep-Oct;15(5):241-4.
• [5] Inhibition of human lens aldose reductase by flavonoids, sulindac and indomethacin. Biochem Pharmacol. 1983 Jul 1;32(13):1995-8.
• [6] Clinical efficacy of fidarestat, a novel aldose reductase inhibitor, for diabetic peripheral neuropathy: a 52-week multicenter placebo-controlled double-blind parallel group study. Diabetes Care. 2001 Oct;24(10):1776-82.
• [7] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2768).
• [8] Effect of Polygonum hydropiper sulfated flavonoids on lens aldose reductase and related enzymes. J Nat Prod. 1996 Apr;59(4):443-5.
• [9] ClinicalTrials.gov (NCT02332005) 12-Month Efficacy and Safety of Diepalrestat in Adults With Diabetic Peripheral Neuropathy, a DB, Placebo-Controlled Study (DE-DPN). U.S. National Institutes of Health.
• [10] Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors ... J Med Chem. 2005 May 5;48(9):3141-52.
• [11] A multicenter, double-blind, safety study of QR-333 for the treatment of symptomatic diabetic peripheral neuropathy. A preliminary report. J Diabetes Complications. 2005 Sep-Oct;19(5):247-53.
• [12] Dextromethorphan/quinidine: AVP 923, dextromethorphan/cytochrome P450-2D6 inhibitor, quinidine/dextromethorphan. Drugs R D. 2005;6(3):174-7.
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [14] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
• [15] Antitussives and substance abuse. Subst Abuse Rehabil. 2013 Nov 6;4:75-82.
• [16] Clinical pipeline report, company report or official report of SK BioPhamaceuticals.
• [17] Antiamnesic and neuroprotective effects of donepezil against learning impairments induced in mice by exposure to carbon monoxide gas. J Pharmacol Exp Ther. 2006 Jun;317(3):1307-19.
• [18] Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001 Dec;41(8):976-88.
• [19] 2011 Pipeline of Anavex.
• [20] Tumor imaging with 2 sigma-receptor ligands, 18F-FE-SA5845 and 11C-SA4503: a feasibility study. J Nucl Med. 2004 Nov;45(11):1939-45.
• [21] SSR125329A, a high affinity sigma receptor ligand with potent anti-inflammatory properties. Eur J Pharmacol. 2002 Dec 5;456(1-3):123-31.