Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT7CXIM)

• DTT Name: Histamine receptor (HR)
• Gene Name: HR
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: NOUNIPROTAC
• TTD ID: T81905

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Histamine Phosphate	DMV7IM6	Diagnostic imaging	N.A.	Approved	[2]
Repirinast	DM6KI0D	Asthma	CA23	Approved	[1]

5 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Levomequitazine	DMAYC76	Seasonal allergic rhinitis	CA08.01	Phase 3	[3]
ETS-6218	DMV96BY	Fibromyalgia	MG30.01	Phase 2	[4]
ETX-9101	DMZOA2L	Asthma	CA23	Phase 2	[4]
LCB-2183	DMY4IWC	Asthma	CA23	Phase 2	[5]
Votucalis	DMW4LTI	Allergic rhinitis	CA08.0	Phase 2	[6]

5 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
OX-NLA	DMPEHBJ	Allergic rhinitis	CA08.0	Discontinued in Phase 3	[7]
CP-118	DMNJD9H	Allergic rhinitis	CA08.0	Discontinued in Phase 2	[8]
Tesmilifene	DMPB36I	Breast cancer	2C60-2C65	Discontinued in Phase 2	[9]
KF-15766	DMNZ1LR	Allergy	4A80-4A85	Terminated	[10]
REV-598	DM314CZ	Carcinoid syndrome	5B10	Terminated	[11]

References

• [1] Mechanism of action of MY-1250, an active metabolite of Repirinast, in inhibiting histamine release from rat mast cells. Br J Pharmacol. 1992 Mar;105(3):587-90.
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [3] Oxidation of histamine H1 antagonist mequitazine is catalyzed by cytochrome P450 2D6 in human liver microsomes. J Pharmacol Exp Ther. 1998 Feb;284(2):437-42.
• [4] Clinical pipeline report, company report or official report of e-Therapeutics.
• [5] LCB 2183 inhibits the inflammation associated with oxazolone-induced contact sensitivity. Int J Immunopharmacol. 1994 Aug;16(8):675-83.
• [6] CA patent application no. 520580, Histamine binding compounds for treatment method for disease conditions mediated by neutrophils.
• [7] Clinical pipeline report, company report or official report of Orexo.
• [8] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025139)
• [9] Effects of tesmilifene, a substrate of CYP3A and an inhibitor of P-glycoprotein, on the pharmacokinetics of intravenous and oral docetaxel in rats. J Pharm Pharmacol. 2010 Aug;62(8):1084-8.
• [10] Mutational analysis of the antagonist-binding site of the histamine H(1) receptor. J Biol Chem. 1999 Oct 15;274(42):29994-30000.
• [11] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016819)