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

General Information of Drug (ID: DMOMP9U)

• Drug Name: Cetirizine Drug Info
• Synonyms: Cetiderm; Cetirizin; Cetirizina; Cetirizinum; Cetryn; Setir; Virlix; Ziptek; Zirtek; Zyrlex; Cetirizina [Spanish]; Cetirizinum [Latin]; Cetrizine Hcl; Hitrizin Film Tablet; Cetiderm (TN); Cetirizine (INN); Cetirizine [INN:BAN]; P-071; Reactine (TN); Zyrtec (TN); [(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethyl)oxy]acetic acid; (2-(4-((4-Chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)acetic acid; (2-{4-[(4-Chloro-phenyl)-phenyl-methyl]-piperazin-1-yl}-ethoxy)-acetic acid; (2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid; 2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid; 2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic acid

Indication

Disease Entry	ICD 11	Status	REF
Allergic rhinitis	CA08.0	Approved	[1]
Common cold	CA00	Approved	[2]
Seasonal allergic rhinitis	CA08.01	Approved	[2]
Vasomotor/allergic rhinitis	CA08	Approved	[2]

• Therapeutic Class: Antiallergic Agents
• Cross-matching ID:
  PubChem CID: 2678
  ChEBI ID: CHEBI:3561
  CAS Number: CAS 83881-51-0
  TTD Drug ID: DMOMP9U
  VARIDT Drug ID: DR00177
  INTEDE Drug ID: DR2269
  ACDINA Drug ID: D00116

Molecule-Related Drug Atlas

Drug(s) Targeting Histamine H1 receptor (H1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ergotidine	DM78IME	Osteoarthritis	FA00-FA05	Approved	[5]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[6]
Azelastine	DMXTMBJ	Allergic conjunctivitis	9A60.02	Approved	[7]
Fexofenadine	DM17ONX	Allergic rhinitis	CA08.0	Approved	[8]
Cinnarizine	DM7U5QJ	Meniere disease	AB31.0	Approved	[9]
Diphenhydramine	DMKQTBA	Hyperemesis gravidarum		Approved	[7]
Doxepin	DMPI98T	Anxiety		Approved	[10]
Chlorpheniramine	DM5URA2	Allergic rhinitis	CA08.0	Approved	[7]
Epinastine	DMX0K3Q	Allergic conjunctivitis	9A60.02	Approved	[11]
Desloratadine	DM56YN7	Allergic rhinitis	CA08.0	Approved	[12]

Drug(s) Transported By P-glycoprotein 1 (ABCB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amoxicillin	DMUYNEI	Acute otitis media	AB00	Approved	[13]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[14]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[15]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[16]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[15]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[15]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[17]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[15]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[18]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[19]

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	[3]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[4]

References

• [1] 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: 1222).
• [2] Cetirizine FDA Label
• [3] Design, synthesis and histamine H1-receptor antagonistic activity of some novel 4-amino-2-(substituted)-5-(substituted) aryl-6-[(substituted aryl) amino] pyrimidines. Arzneimittelforschung. 2009;59(5):243-7.
• [4] Stereoselective and multiple carrier-mediated transport of cetirizine across Caco-2 cell monolayers with potential drug interaction. Chirality. 2010 Jul;22(7):684-92.
• [5] Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
• [6] 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.
• [7] 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.
• [8] Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
• [9] Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
• [10] Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
• [11] 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.
• [12] Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
• [13] Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
• [14] MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
• [15] Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
• [16] Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
• [17] Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
• [18] Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
• [19] Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.