Details
Stereochemistry | RACEMIC |
Molecular Formula | C32H41NO2 |
Molecular Weight | 471.6734 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(C)C1=CC=C(C=C1)C(O)CCCN2CCC(CC2)C(O)(C3=CC=CC=C3)C4=CC=CC=C4
InChI
InChIKey=GUGOEEXESWIERI-UHFFFAOYSA-N
InChI=1S/C32H41NO2/c1-31(2,3)26-18-16-25(17-19-26)30(34)15-10-22-33-23-20-29(21-24-33)32(35,27-11-6-4-7-12-27)28-13-8-5-9-14-28/h4-9,11-14,16-19,29-30,34-35H,10,15,20-24H2,1-3H3
Molecular Formula | C32H41NO2 |
Molecular Weight | 471.6734 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19660947 |
40.0 nM [Ki] |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
406.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1576325/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
FEXOFENADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
458.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1576325/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
FEXOFENADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
1.544 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6113858/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
TERFENADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
4.519 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6113858/ |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
TERFENADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2720.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1576325/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
FEXOFENADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2712.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1576325/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
FEXOFENADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
11.864 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6113858/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
TERFENADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
44.341 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6113858/ |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
TERFENADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
12.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1576325/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
FEXOFENADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
11.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1576325/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
FEXOFENADINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
Doses
Dose | Population | Adverse events |
---|---|---|
180 mg 2 times / day multiple, oral Highest studied dose Dose: 180 mg, 2 times / day Route: oral Route: multiple Dose: 180 mg, 2 times / day Sources: |
healthy, 18-40 |
Other AEs: Electrocardiogram QTc interval prolonged... Other AEs: Electrocardiogram QTc interval prolonged (12.5%) Sources: |
60 mg 2 times / day multiple, oral Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 18-45 |
Disc. AE: Headache... Other AEs: Somnolence... AEs leading to discontinuation/dose reduction: Headache (grade 2-3, 8.3%) Other AEs:Somnolence (grade 1, 4.15%) Sources: |
120 mg 1 times / day multiple, oral Recommended Dose: 120 mg, 1 times / day Route: oral Route: multiple Dose: 120 mg, 1 times / day Sources: |
unhealthy, 19-66 |
Disc. AE: Nausea, Headache... AEs leading to discontinuation/dose reduction: Nausea (2.4%) Sources: Headache (2.4%) |
60 mg single, oral Recommended |
healthy, 23-40 |
|
240 mg single, oral Highest studied dose |
healthy, 23-47 |
Other AEs: Driving ability disturbed... |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Electrocardiogram QTc interval prolonged | 12.5% | 180 mg 2 times / day multiple, oral Highest studied dose Dose: 180 mg, 2 times / day Route: oral Route: multiple Dose: 180 mg, 2 times / day Sources: |
healthy, 18-40 |
Somnolence | grade 1, 4.15% | 60 mg 2 times / day multiple, oral Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 18-45 |
Headache | grade 2-3, 8.3% Disc. AE |
60 mg 2 times / day multiple, oral Recommended Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: |
unhealthy, 18-45 |
Headache | 2.4% Disc. AE |
120 mg 1 times / day multiple, oral Recommended Dose: 120 mg, 1 times / day Route: oral Route: multiple Dose: 120 mg, 1 times / day Sources: |
unhealthy, 19-66 |
Nausea | 2.4% Disc. AE |
120 mg 1 times / day multiple, oral Recommended Dose: 120 mg, 1 times / day Route: oral Route: multiple Dose: 120 mg, 1 times / day Sources: |
unhealthy, 19-66 |
Driving ability disturbed | 240 mg single, oral Highest studied dose |
healthy, 23-47 |
PubMed
Title | Date | PubMed |
---|---|---|
Mechanism of terfenadine block of ATP-sensitive K(+) channels. | 2000 Aug |
|
Loratadine blockade of K(+) channels in human heart: comparison with terfenadine under physiological conditions. | 2000 Jan |
|
Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. | 2000 May 26 |
|
Effect of oxatomide, an antiallergic agent, on QT interval in dogs. | 2001 |
|
Evaluation of drug-induced QT interval prolongation: implications for drug approval and labelling. | 2001 |
|
Uptake and efflux of the peptidic delta-opioid receptor agonist. | 2001 Apr 6 |
|
Second generation antihistamines in the treatment of seasonal allergic rhinitis due to Parietaria and cypress pollen. | 2001 Dec |
|
Assessing the effect of intranasal steroids on growth. | 2001 Jul |
|
[Effect of olopatadine hydrochloride, a novel antiallergic agent, on the QT interval in dogs]. | 2001 Jun |
|
The effect of rifampin administration on the disposition of fexofenadine. | 2001 Mar |
|
Loratadine and terfenadine interaction with nefazodone: Both antihistamines are associated with QTc prolongation. | 2001 Mar |
|
A descriptive analysis of the use and cost of new-generation antihistamines in the treatment of allergic rhinitis: a retrospective database analysis. | 2001 May |
|
Controlled comparison of the efficacy and safety of cetirizine 10 mg o.d. and fexofenadine 120 mg o.d. in reducing symptoms of seasonal allergic rhinitis. | 2001 May |
|
Fexofenadine decreases sensitivity to and montelukast improves recovery from inhaled mannitol. | 2001 May |
|
The canine Purkinje fiber: an in vitro model system for acquired long QT syndrome and drug-induced arrhythmogenesis. | 2001 May |
|
Inhibition of depolarization-induced [3H]noradrenaline release from SH-SY5Y human neuroblastoma cells by some second-generation H(1) receptor antagonists through blockade of store-operated Ca(2+) channels (SOCs). | 2001 Nov 1 |
|
[Efficacy and safety of fexofenadine and cetirizine in the treatment of allergic rhinitis]. | 2001 Nov-Dec |
|
Development and evaluation of high throughput functional assay methods for HERG potassium channel. | 2001 Oct |
|
[Comparative antihistamine and anti-allergic effects of various antihistamine preparations]. | 2002 |
|
Effects of antihistamines on leukotriene and cytokine release from dispersed nasal polyp cells. | 2002 |
|
The relationship of clinical QT prolongation to outcome in the conscious dog using a beat-to-beat QT-RR interval assessment. | 2002 Aug |
|
Antihistamines in late-phase clinical development for allergic disease. | 2002 Feb |
|
Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine. | 2002 Jan |
|
Determination of fexofenadine in human plasma and urine by liquid chromatography-mass spectrometry. | 2002 Jan 25 |
|
Fexofenadine modulates T-cell function, preventing allergen-induced airway inflammation and hyperresponsiveness. | 2002 Jul |
|
Role of lung inflammatory mediators as a cause of exercise-induced arterial hypoxemia in young athletes. | 2002 Jul |
|
Simultaneous determination of fexofenadine and its related compounds by HPLC. | 2002 Jul 20 |
|
Drug eruption and liver injury caused by terfenadine and oxatomide. | 2002 Jul-Aug |
|
Effect of St John's wort on the pharmacokinetics of fexofenadine. | 2002 Jun |
|
Are herbal products dietary supplements or drugs? An important question for public safety. | 2002 Jun |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6129869
Terfenadine 20 mg 3 times a day
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:25:30 GMT 2025
by
admin
on
Mon Mar 31 18:25:30 GMT 2025
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Record UNII |
7BA5G9Y06Q
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Record Status |
Validated (UNII)
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NCI_THESAURUS |
C29578
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WHO-ATC |
R06AX12
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WHO-VATC |
QR06AX12
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LIVERTOX |
939
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CFR |
21 CFR 216.24
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D016593
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256-710-8
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758627
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Terfenadine
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SUB10920MIG
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C29494
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3674
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7BA5G9Y06Q
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42330
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2600
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CHEMBL17157
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665802
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m10576
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100000082708
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2608
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6508
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