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

General Information of Drug (ID: DMRNJPY)

• Drug Name: GSK835726 Drug Info
• Synonyms: Galnon trifluoroacetate salt; Galnon trifluoroacetate salt, > 7-((9-Fluorenylmethoxycarbonyl)cyclohexylalanyllysyl) amino-4-methylcoumarin trifluoroacetate salt

Indication

Disease Entry	ICD 11	Status	REF
Allergic rhinitis	CA08.0	Discontinued in Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 16219413
  TTD Drug ID: DMRNJPY

Molecule-Related Drug Atlas

Drug(s) Targeting Histamine H3 receptor (H3R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pitolisant	DM8RFNJ	Excessive daytime sleepiness	MG42	Approved	[3]
SUVN-G3031	DM3BO8G	Cognitive impairment	6D71	Phase 3	[4]
JNJ-17216498	DM1GRCU	Narcolepsy	7A20	Phase 2	[5]
GSK239512	DMBJMZC	Alzheimer disease	8A20	Phase 2	[2]
JNJ-39220675	DM0WY3H	Alcohol dependence	6C40.2	Phase 2	[6]
AZD-5213	DMOZ04X	Alzheimer disease	8A20	Phase 2	[7]
Bavisant	DM6CVZ5	Attention deficit hyperactivity disorder	6A05.Z	Phase 2	[8]
ABT-288	DM7X54F	Alzheimer disease	8A20	Phase 2	[9]
SAR-110894	DMCLEXM	Alzheimer disease	8A20	Phase 2	[7]
ABT-652	DMLEO2Z	Diabetic neuropathy	8C0Z	Phase 2	[10]

Drug(s) Targeting Histamine H1 receptor (H1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ergotidine	DM78IME	Osteoarthritis	FA00-FA05	Approved	[11]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[12]
Azelastine	DMXTMBJ	Allergic conjunctivitis	9A60.02	Approved	[13]
Fexofenadine	DM17ONX	Allergic rhinitis	CA08.0	Approved	[14]
Cinnarizine	DM7U5QJ	Meniere disease	AB31.0	Approved	[15]
Diphenhydramine	DMKQTBA	Hyperemesis gravidarum		Approved	[13]
Doxepin	DMPI98T	Anxiety		Approved	[16]
Chlorpheniramine	DM5URA2	Allergic rhinitis	CA08.0	Approved	[13]
Epinastine	DMX0K3Q	Allergic conjunctivitis	9A60.02	Approved	[17]
Desloratadine	DM56YN7	Allergic rhinitis	CA08.0	Approved	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H1 receptor (H1R)	TTTIBOJ	HRH1_HUMAN	Antagonist	[2]
Histamine H3 receptor (H3R)	TT9JNIC	HRH3_HUMAN	Antagonist	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028154)
• [2] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61.
• [6] JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats. Psychopharmacology (Berl). 2011 Apr;214(4):829-41.
• [7] SAR110894, a potent histamine H receptor antagonist, displays procognitive effects in rodents. Pharmacol Biochem Behav. 2012 Aug;102(2):203-14.
• [8] Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder. CNS Drugs. 2012 May 1;26(5):421-34.
• [9] A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia.J Alzheimers Dis.2014;42(3):959-71.
• [10] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032225)
• [11] Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
• [12] Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
• [13] Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
• [14] Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
• [15] Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
• [16] Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
• [17] Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
• [18] Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.