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

General Information of Drug (ID: DM17ONX)

Drug Name
Fexofenadine Drug Info
Synonyms
Carboxyterfenadine; Fexofendine; Terfenadine acid metabolite; Terfenadine carboxylate; F 9427; MDL 16455; Allegra (TN); Fastofen (TN); Fexofenadine (INN); Fexofenadine [INN:BAN]; Telfast (TN); Terfenadine-COOH; Terfenidine carboxylate, MDL 16455; Tilfur (TN); 2-[4-(1-hydroxy-4-{4-[hydroxy(diphenyl)methyl]piperidin-1-yl}butyl)phenyl]-2-methylpropanoic acid; 2-[4-[1-hydroxy-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butyl]phenyl]-2-methylpropanoic acid; 4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)-1-piperidinyl)butyl)-alpha,alpha-dimethylbenzeneacetic acid
Indication
Disease Entry ICD 11 Status REF
Allergic rhinitis CA08.0 Approved [1]
Seasonal allergic rhinitis CA08.01 Approved [2]
Therapeutic Class
Antiallergic Agents
Cross-matching ID
PubChem CID
3348
ChEBI ID
CHEBI:5050
CAS Number
CAS 83799-24-0
TTD Drug ID
DM17ONX
VARIDT Drug ID
DR00026
ACDINA Drug ID
D00273

Molecule(s) Related to 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 Highest Status REF
Multidrug resistance-associated protein 3 (ABCC3) DTQ3ZHF MRP3_HUMAN Approved [4]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Approved [5]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Approved [6]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Approved [7]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Approved [8]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [9]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Histamine H1 receptor (H1R) DTT HRH1 5.972 5.7 5.816 6.002
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Organic cation transporter 1 (SLC22A1) DTP `OCT1 10.261 4.162 4.07 3.797
Multidrug resistance-associated protein 3 (ABCC3) DTP MRP3 7.688 7.801 5.548 6.957
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 8.165 6.597 6.591 6.397
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 4.365 4.466 3.248 2.632
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 8.873 2.17 2.485 3.322
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Allergic rhinitis
ICD Disease Classification CA08.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Histamine H1 receptor (H1R) DTT HRH1 6.74E-01 0.13 0.43
P-glycoprotein 1 (ABCB1) DTP P-GP 6.54E-01 1.95E-01 4.04E-01
Organic cation transporter 1 (SLC22A1) DTP SLC22A1 6.27E-01 5.04E-02 1.96E-01
Multidrug resistance-associated protein 3 (ABCC3) DTP MRP3 9.17E-01 -6.21E-03 -3.18E-02
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 7.68E-01 -7.76E-02 -1.74E-01
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 7.98E-01 1.52E-01 2.97E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 8.56E-01 3.16E-02 2.99E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

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: 4819).
2 Fexofenadine FDA Label
3 Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
4 Involvement of multiple efflux transporters in hepatic disposition of fexofenadine. Mol Pharmacol. 2008 May;73(5):1474-83.
5 Intestinal drug transporter expression and the impact of grapefruit juice in humans. Clin Pharmacol Ther. 2007 Mar;81(3):362-70.
6 The effects of the SLCO2B1 c.1457C>T polymorphism and apple juice on the pharmacokinetics of fexofenadine and midazolam in humans. Pharmacogenet Genomics. 2011 Feb;21(2):84-93.
7 Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1. Biochem Pharmacol. 2010 Dec 1;80(11):1746-53.
8 Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. Drug Metab Dispos. 2005 Oct;33(10):1477-81.
9 Effect of itraconazole on the pharmacokinetics and pharmacodynamics of fexofenadine in relation to the MDR1 genetic polymorphism. Clin Pharmacol Ther. 2005 Aug;78(2):191-201.