Target Information

Target General Infomation
Target ID
T81905
Former ID
TTDS00085
Target Name
Histamine receptor
Target Type
Successful
Disease Asthma [ICD10: J45]
Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4]
Allergy [ICD9: 995.3; ICD10: T78.4]
Breast cancer; Prostate cancer [ICD9: 174, 175, 185; ICD10: C50, C61]
Carcinoid syndrome [ICD10: E34.0]
Diagnostic imaging [ICD9: 331; ICD10: G30, I73.9]
Fibromyalgia [ICD9: 729.1; ICD10: M79.7]
Seasonal allergic rhinitis [ICD9: 472.0, 477; ICD10: J00, J30, J31.0]
BioChemical Class
GPCR rhodopsin
Drugs and Mode of Action
Drug(s) Histamine Phosphate Drug Info Approved Diagnostic imaging [538384]
Repirinast Drug Info Approved Asthma [551871]
Levomequitazine Drug Info Phase 3 Seasonal allergic rhinitis [549265]
ETS-6218 Drug Info Phase 2 Fibromyalgia [549064]
ETX-9101 Drug Info Phase 2 Asthma [548891]
LCB-2183 Drug Info Phase 2 Asthma [533600]
Votucalis ophthalmic Drug Info Phase 2 Allergic rhinitis [521858]
OX-NLA Drug Info Discontinued in Phase 3 Allergic rhinitis [547891]
CP-118 Drug Info Discontinued in Phase 2 Allergic rhinitis [548385]
Tesmilifene Drug Info Discontinued in Phase 2 Breast cancer; Prostate cancer [545850]
KF-15766 Drug Info Terminated Allergy [545862]
REV-598 Drug Info Terminated Carcinoid syndrome [547496]
Antagonist CP-118 Drug Info [548386]
Levomequitazine Drug Info [534548]
OX-NLA Drug Info [551474]
Votucalis ophthalmic Drug Info [550831]
Modulator ETS-6218 Drug Info [550630]
ETX-9101 Drug Info [550630]
Histamine Phosphate Drug Info [556264]
KF-15766 Drug Info [525607]
LCB-2183 Drug Info [533836]
Repirinast Drug Info [526799], [551871]
Tesmilifene Drug Info [531060]
Inhibitor REV-598 Drug Info [547497]
References
Ref 521858ClinicalTrials.gov (NCT00353964) Safety and Efficacy Study of rEV131 in the Treatment of Ocular Inflammation After Cataract Surgery. U.S. National Institutes of Health.
Ref 533600LCB 2183 inhibits tracheal hyperreactivity and pulmonary inflammation in mouse airways. Eur J Pharmacol. 1995 Aug 25;282(1-3):103-9.
Ref 538384FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 000734.
Ref 545850Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005041)
Ref 545862Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005087)
Ref 547496Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016819)
Ref 547891Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020184)
Ref 548385Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025139)
Ref 548891Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030000)
Ref 549064Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031879)
Ref 549265Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034359)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525607Mutational analysis of the antagonist-binding site of the histamine H(1) receptor. J Biol Chem. 1999 Oct 15;274(42):29994-30000.
Ref 526799Mechanism 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.
Ref 531060Effects 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.
Ref 533836LCB 2183 inhibits the inflammation associated with oxazolone-induced contact sensitivity. Int J Immunopharmacol. 1994 Aug;16(8):675-83.
Ref 534548Oxidation 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.
Ref 547497Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016819)
Ref 548386Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025139)
Ref 550630Clinical pipeline report, company report or official report of e-Therapeutics.
Ref 550831CA patent application no. 520580, Histamine binding compounds for treatment method for disease conditions mediated by neutrophils.
Ref 551474Clinical pipeline report, company report or official report of Orexo.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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