Terfenadine
Terfenadine was a first-generation selective peripheral histamine H1 receptor antagonist that was among the first non-sedating antihistamines, used for allergic rhinitis and urticaria. It was withdrawn from most markets due to its propensity to cause life-threatening QT prolongation and torsades de pointes arrhythmias, particularly when combined with CYP3A4 inhibitors or in patients with hepatic dysfunction, as the parent compound is cardiotoxic at higher plasma levels. Its active metabolite fexofenadine, which lacks cardiac toxicity, replaced terfenadine and remains in clinical use.
Molekularmasse
471,7000 g/mol
LogP
6,60
TPSA
43,70 Ų
Lipinski-Regel der Fünf
Bestanden
Wirkmechanismus
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
2D-Struktur
Cite this structure
Embed this structure
SMILES
CC(C)(C)c1ccc(C(O)CCCN2CCC(C(O)(c3ccccc3)c3ccccc3)CC2)cc1
InChI
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
HBD / HBA
2 / 3
Rotierbare Bindungen
9
Schwere Atome
35
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Häufig gestellte Fragen
Terfenadine was a first-generation selective peripheral histamine H1 receptor antagonist that was among the first non-sedating antihistamines, used for allergic rhinitis and urticaria. It was withdrawn from most markets due to its propensity to cause life-threatening QT prolongation and torsades de pointes arrhythmias, particularly when combined with CYP3A4 inhibitors or in patients with hepatic dysfunction, as the parent compound is cardiotoxic at higher plasma levels. Its active metabolite fexofenadine, which lacks cardiac toxicity, replaced terfenadine and remains in clinical use.
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.
Yes, Terfenadine is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL17157. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 5405. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
Medizinischer Haftungsausschluss
This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
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