terfenadine
Trade name: Seldane
Approved
Jun 1, 1985
Terfenadine under brand name Seldane was used for the treatment of allergic rhinitis and allergic skin disorders but was withdrawn because of the serious side effect, heart rhythm problems. Terfenadine is a potent antagonist of histamine H1-receptor-mediated responses. — NCATS
Clinical trial activity
0 trials · 0 clinical orgs · 1 marketing orgs
Timeline
1980s
- Jun 1, 1985
Earliest FDA Approval
Indications
Approved for
Mechanism of action
- Histamine H1 receptorANTAGONIST
HRH1 antagonist
In humans, terfenadine is well absorbed and it is metabolized by two routes, i.e. N-dealkylation to azacyclonol and hydroxylation of the t-butyl group to form hydroxyterfenadine. Hydroxyterfenadine undergoes subsequent oxidation to the corresponding carboxylic acid, which is thought to be the biologically active antihistamine.
Approval history
- approvedJun 1, 1985
Chemistry & pharmacology
SMILES
CC(C)(C)C1=CC=C(C=C1)C(O)CCCN2CCC(CC2)C(O)(C3=CC=CC=C3)C4=CC=CC=C4- Mol. weight
- 471.6734 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTerfenadine ↗
- NCATS7BA5G9Y06Q ↗
- ChEMBLCHEMBL17157 ↗
Also known as
- antihistamine
- antihistamine
- histafen
- histafen 120
- racemic terfenadine
- rmi-9918
- rmi-9918
- (rs)-1-(4-tert-butylphenyl)-4-{4-[hydroxy(diphenyl)methyl]piperidin-1-yl}-butan-1-ol
- (rs)-1-(4-tert-butylphenyl)-4-{4-[hydroxy(diphenyl)methyl]piperidin-1-yl}-butan-1-ol
- seldane
- seldane
- seldane
- seldane
- terfenadin
- terfenadin
- terfenadina
- terfenadina
- terfenadine
- terfenadine
- terfenadine
- terfenadine
- terfenadine
- terfenadine
- terfenadine
- terfenadine
- terfenadine
- terfénadine
- terfénadine
- terfenadinum
- terfenadinum
- terfenor
- terfenor fte
- terfex
- terfex
- terfinax 120
- terfinax 60
- ternadin
- triludan
- triludan
- triludan fte
Organizations
Marketing (1)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Hoechst | For profit | NDA | — |