dimetindene

Small moleculeexperimental

Dimetindene (trade name Fenistil; other name dimethindene maleate) is a potent antipruritic antihistamine, characterized by the small size of its effective dose and its rapidity of action. Dimetindene is an antihistamine/anticholinergic that is a selective H1 antagonist. Its effect sets in after 20 to 60 minutes and lasts several hours. Dimetindene drops as well as Dimetindene syrup is particularly indicated in pediatric practice. Dimetindene is indicated as symptomatic treatment of allergic reactions: urticaria, allergies of the upper respiratory tract such as hay fever and perennial rhinitis, food, and drug allergies; pruritus of various origins, except pruritus due to cholestasis; insect bites. Dimetindene is also indicated for pruritus in eruptive skin diseases such as chicken-pox. Dimetindene can be as an adjuvant in eczema and other pruriginous dermatoses of allergic origin. — NCATS

Clinical trial activity

3 trials · 3 clinical orgs · 0 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Sep 1, 2010 (NCT02094287)

Timeline

2010s

Jan 1, 2010
Earliest Phase 1 Sponsor(trial)
Jan 1, 2013
Earliest Phase 3 Sponsor(trial)

Indications

Approved for

Studied for

Mechanism of action

Histamine H1 receptorANTAGONIST
HRH1 antagonist
Dimetindene is an antihistamine/anticholinergic drug. It is a selective histamine H1 antagonist and binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. As dimetindene only minimally passes across the blood-brain barrier, it is classified as a second generation antihistamine.
- Histamine H1 receptor (HRH1) ↗

Chemistry & pharmacology

Loading structure…

SMILES

CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1

Mol. weight: 292.43 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Racemic Mixture
Inorganic: No
Polymer: No

Oral

Parenteral

Topical

Sources

Also known as

dimethindene
dimethindene
dimethindene
dimethindene
dimethindene
dimethindene maleate
dimethindene maleate
dimethindene maleate
dimethindine
dimetindene
dimetindene
dimetindene
dimetindene
dimetindene
dimetindene
dimetindene
dimetindene maleate
dimetindene maleate
dimetindene maleate
dimetindene maleate
dimetindene maleate
dimetindene maleate
fenostil
forhistal maleate
forhistal maleate
su-6518
su-6518

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT01448057	Phase 3	Jul 1, 2013	Novartis
NCT01026961	Phase 1/Phase 2 (Phase 2)	Sep 1, 2010	Novartis
NCT02094287	N/A	Sep 1, 2010	Humboldt University, University of Hamburg

Showing 3 of 3 trials

Page 1 / 1

Organizations

Research & Development (3)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Novartis	For profit	2	2	2	2010
Humboldt University	Academic/Hospital	1	1	1	2010
University of Hamburg	Academic/Hospital	1	0	1	2010

3 organizations

Page 1 / 1