Details of the Drug

General Information of Drug (ID: DM17ONX)

Drug 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
Indication
Disease Entry ICD 11 Status REF
Allergic rhinitis CA08.0 Approved [1], [2]
Therapeutic Class
Antiallergic Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 501.7
Topological Polar Surface Area (xlogp) 3
Rotatable Bond Count (rotbonds) 10
Hydrogen Bond Donor Count (hbonddonor) 3
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 1367 mcgh/L [3]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 299 mcg/L [3]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 1-3 h [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [4]
Bioavailability
The bioavailability of drug is 33% [3]
Clearance
The renal clearance of drug is 4.32 L/h [3]
Elimination
Approximately 80% of an ingested dose is eliminated in the feces, likely largely unchanged due to fexofenadine's limited metabolism, and 11% is eliminated in the urine [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 11 - 15 hours [3]
Metabolism
The drug is metabolized via the hepatic [3]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 5.1257 micromolar/kg/day [6]
Vd
The volume of distribution (Vd) of drug is 5.4-5.8 L/kg [5]
Chemical Identifiers
Formula
C32H39NO4
IUPAC Name
2-[4-[1-hydroxy-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butyl]phenyl]-2-methylpropanoic acid
Canonical SMILES
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
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
Cross-matching ID
PubChem CID
3348
ChEBI ID
CHEBI:5050
CAS Number
83799-24-0
DrugBank ID
DB00950
TTD ID
D01KPV
VARIDT ID
DR00026
ACDINA ID
D00273

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 [7], [8]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 3 (ABCC3) DTQ3ZHF MRP3_HUMAN Substrate [9]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [10]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Substrate [11]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [12]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [13]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [14]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

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 (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Fexofenadine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Midostaurin DMI6E0R Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Midostaurin. Acute myeloid leukaemia [2A60] [76]
Arn-509 DMT81LZ Moderate Accelerated clearance of Fexofenadine due to the transporter induction by Arn-509. Acute myeloid leukaemia [2A60] [76]
Gilteritinib DMWQ4MZ Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Gilteritinib. Acute myeloid leukaemia [2A60] [77]
Dronedarone DMA8FS5 Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Dronedarone. Angina pectoris [BA40] [78]
Clarithromycin DM4M1SG Minor Decreased clearance of Fexofenadine due to the transporter inhibition by Clarithromycin. Bacterial infection [1A00-1C4Z] [79]
Troleandomycin DMUZNIG Minor Decreased clearance of Fexofenadine due to the transporter inhibition by Troleandomycin. Bacterial infection [1A00-1C4Z] [79]
Ag-221 DMS0ZBI Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Ag-221. BCR-ABL1-negative chronic myeloid leukaemia [2A41] [77]
Erdafitinib DMI782S Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Erdafitinib. Bladder cancer [2C94] [80]
Tucatinib DMBESUA Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Tucatinib. Breast cancer [2C60-2C6Y] [81]
PF-04449913 DMSB068 Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by PF-04449913. Chronic myelomonocytic leukaemia [2A40] [76]
Ivacaftor DMZC1HS Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Ivacaftor. Cystic fibrosis [CA25] [82]
MK-8228 DMOB58Q Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by MK-8228. Cytomegaloviral disease [1D82] [83]
Itraconazole DMCR1MV Minor Decreased clearance of Fexofenadine due to the transporter inhibition by Itraconazole. Fungal infection [1F29-1F2F] [79]
Miconazole DMPMYE8 Minor Decreased clearance of Fexofenadine due to the transporter inhibition by Miconazole. Fungal infection [1F29-1F2F] [79]
Ketoconazole DMPZI3Q Minor Decreased clearance of Fexofenadine due to the transporter inhibition by Ketoconazole. Fungal infection [1F29-1F2F] [79]
GS-5885 DMSL3DX Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by GS-5885. Hepatitis virus infection [1E50-1E51] [84]
Rifampin DMA8J1G Moderate Accelerated clearance of Fexofenadine due to the transporter induction by Rifampin. HIV-infected patients with tuberculosis [1B10-1B14] [85]
Fostemsavir DM50ILT Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [86]
Bempedoic acid DM1CI9R Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Bempedoic acid. Hyper-lipoproteinaemia [5C80] [87]
BMS-201038 DMQTAGO Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by BMS-201038. Hyper-lipoproteinaemia [5C80] [88]
Tolvaptan DMIWFRL Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Tolvaptan. Hypo-osmolality/hyponatraemia [5C72] [77]
Capmatinib DMYCXKL Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Capmatinib. Lung cancer [2C25] [89]
Ibrutinib DMHZCPO Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Ibrutinib. Mature B-cell lymphoma [2A85] [76]
Lasmiditan DMXLVDT Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Lasmiditan. Migraine [8A80] [90]
Nilotinib DM7HXWT Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Nilotinib. Myeloproliferative neoplasm [2A20] [91]
Rolapitant DM8XP26 Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Rolapitant. Nausea/vomiting [MD90] [92]
Lonafarnib DMGM2Z6 Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Lonafarnib. Premature ageing appearance [LD2B] [93]
Enzalutamide DMGL19D Moderate Accelerated clearance of Fexofenadine due to the transporter induction by Enzalutamide. Prostate cancer [2C82] [94]
Darolutamide DMV7YFT Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [76]
Fostamatinib DM6AUHV Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Fostamatinib. Thrombocytopenia [3B64] [95]
Eltrombopag DMOGFIX Moderate Decreased clearance of Fexofenadine due to the transporter inhibition by Eltrombopag. Thrombocytopenia [3B64] [96]
⏷ Show the Full List of 31 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Allura red AC dye E00338 33258 Colorant
Aspartame E00402 134601 Flavoring agent
D&C red no. 28 E00491 6097185 Colorant
D&C red no. 33 E00261 19116 Colorant
FD&C blue no. 1 E00263 19700 Colorant
Kyselina citronova E00014 311 Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Butylhydroxyanisole E00308 24667 Antimicrobial preservative; Antioxidant
Carmellose sodium E00625 Not Available Disintegrant
Crospovidone E00626 Not Available Disintegrant
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferric oxide black E00522 16211978 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Ferrous oxide E00241 14945 Colorant
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 400 E00653 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 4000 E00654 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 6000 E00655 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium bicarbonate E00424 516892 Alkalizing agent; Diluent
Sodium chloride E00077 5234 Diluent; Tonicity agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triacetin E00080 5541 Humectant; Plasticizing agent; Solvent
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Colcothar yellow E00436 518696 Colorant
Haematite red E00236 14833 Colorant
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
Pregelatinized starch E00674 Not Available Binding agent; Diluent; Disintegrant
⏷ Show the Full List of 38 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Fexofenadine 30 mg tablet 30 mg Oral Tablet Oral
Fexofenadine 30 mg tablet 30 mg Disintegrating Oral Tablet Oral
Fexofenadine Hydrochloride 180mg tablet 180mg Tablet Oral
Fexofenadine Hydrochloride 60mg tablet 60mg Tablet Oral
Fexofenadine 180 mg tablet 180 mg Oral Tablet Oral
Fexofenadine 60 mg tablet 60 mg Oral Tablet Oral
Fexofenadine 180 mg tablet 180 mg 24 HR Extended Release Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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