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

General Information of Drug (ID: DMRGF9Q)

• Drug Name: APD-916 Drug Info
• Synonyms: Histamine H3 antagonists (sleep disorder), Arena; Biphenyl derivatives/aryl ethers/anilines (sleep disorder), Arena

Indication

Disease Entry	ICD 11	Status	REF
Sleep-wake disorder	7A00-7B2Z	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 24879170
  TTD Drug ID: DMRGF9Q

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	[6]
JNJ-39220675	DM0WY3H	Alcohol dependence	6C40.2	Phase 2	[7]
AZD-5213	DMOZ04X	Alzheimer disease	8A20	Phase 2	[8]
Bavisant	DM6CVZ5	Attention deficit hyperactivity disorder	6A05.Z	Phase 2	[9]
ABT-288	DM7X54F	Alzheimer disease	8A20	Phase 2	[10]
SAR-110894	DMCLEXM	Alzheimer disease	8A20	Phase 2	[8]
ABT-652	DMLEO2Z	Diabetic neuropathy	8C0Z	Phase 2	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

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

References

• [1] ClinicalTrials.gov (NCT01093508) Single-dose Safety Study of APD916 in Healthy Volunteers. U.S. National Institutes of Health.
• [2] Identification of biaryl sulfone derivatives as antagonists of the histamine H receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916). Bioorg Med Chem Lett. 2012 Jan 1;22(1):71-5.
• [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] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [7] 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.
• [8] SAR110894, a potent histamine H receptor antagonist, displays procognitive effects in rodents. Pharmacol Biochem Behav. 2012 Aug;102(2):203-14.
• [9] 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.
• [10] A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia.J Alzheimers Dis.2014;42(3):959-71.
• [11] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032225)