Drug Information

Drug (ID: DG00019) and It's Reported Resistant Information

Name	Fexofenadine
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 Click to Show/Hide
Indication	In total 1 Indication(s) Vasomotor/allergic rhinitis [ICD-11: CA08] Approved [1]
Structure
Target	Histamine H1 receptor (H1R)	HRH1_HUMAN	[1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula	C32H39NO4
IsoSMILES	CC(C)(C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O)C(=O)O
InChI	1S/C32H39NO4/c1-31(2,30(35)36)25-17-15-24(16-18-25)29(34)14-9-21-33-22-19-28(20-23-33)32(37,26-10-5-3-6-11-26)27-12-7-4-8-13-27/h3-8,10-13,15-18,28-29,34,37H,9,14,19-23H2,1-2H3,(H,35,36)
InChIKey	RWTNPBWLLIMQHL-UHFFFAOYSA-N
PubChem CID	3348
ChEBI ID	CHEBI:5050
TTD Drug ID	D01KPV
VARIDT ID	DR00026
DrugBank ID	DB00950

Type(s) of Resistant Mechanism of This Drug

IDUE: Irregularity in Drug Uptake and Drug Efflux

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-12: Respiratory system diseases

Click to Show/Hide the Resistance Disease of This Class

Seasonal allergic rhinitis [ICD-11: CA08]

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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
Irregularity in Drug Uptake and Drug Efflux (IDUE)		Click to Show/Hide
Key Molecule: ATP-binding cassette sub-family B5 (ABCB5)			[1]
Molecule Alteration	Expression	Down-regulation	Molecule Info
Sensitive Disease	Seasonal allergic rhinitis [ICD-11: CA08.0]		Disease Info
Experimental Note	Identified from the Human Clinical Data
Experiment for Molecule Alteration	qPCR
Experiment for Drug Resistance	Ussing chamber system assay
Mechanism Description	Digoxin and fexofenadine (each 5 uM) were selected as P-gp substrates, and sulfasalazine and rosuvastatin (each 5 uM) were selected as BCRP substrates to evaluate the efflux transport mediated by P-gp and BCRP. PSC833 (15 uM) and ko143 (15 uM) were used as typical inhibitors of P-gp and BCRP, respectively. Serosal-to-mucosal transport of all the tested P-gp and BCRP substrate drugs was significantly decreased or tended to decrease in the presence of P-gp/BCRP inhibitor cocktail.

References

Ref 1	Characterization of the Human Intestinal Drug Transport with Ussing Chamber System Incorporating Freshly Isolated Human Jejunum. Drug Metab Dispos. 2021 Jan;49(1):84-93. doi: 10.1124/dmd.120.000138. Epub 2020 Oct 21.