Details
Stereochemistry | ACHIRAL |
Molecular Formula | C17H20N4O.2ClH |
Molecular Weight | 369.289 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.NC(=O)C1=CN=C2N1CCC3=C(C=CC=C3)C24CCNCC4
InChI
InChIKey=BOYLPLUVCXUHDJ-UHFFFAOYSA-N
InChI=1S/C17H20N4O.2ClH/c18-15(22)14-11-20-16-17(6-8-19-9-7-17)13-4-2-1-3-12(13)5-10-21(14)16;;/h1-4,11,19H,5-10H2,(H2,18,22);2*1H
Vapitadine (R129160; Hivenyl™) is an antihistamine that Barrier Therapeutics is developing as a treatment for allergic reactions of the skin, such as those associated with hives and for the itch associated with atopic dermatitis. Vapitadine is a new selective, non-sedative H1antihistamine. In several in vitro and in vivo pharmacological models, vapitadine is at least as potent as cetirizine (Zyrtec®) and does not penetrate the blood-brain barrier. An advantage of vapitadine over other antihistamines may be the absence of the sedation, even at high doses. Vapitadine had been in phase II clinical trials for the treatment of patients with atopic dermatitis. However, no development has been reported.
Originator
Sources: https://adisinsight.springer.com/drugs/800020866
Curator's Comment: Vapitadine was originally discovered by Johnson&Johnson, then licensed to Stiefel Laboratories (acquired by GlaxoSmithKline in 2009).
Approval Year
Sample Use Guides
In healthy volunteers vapitadine dose-dependently inhibits the histamine-induced wheal and flare reaction. Vapitadine shows a fast onset of action (within 1 hour) as well as a long-lasting (>24 hours) antihistaminic activity (from 10 mg onwards). Vapitadine does not induce sedation up to the highest dose tested (150 mg o.d. for 8 days).
After a one-week run-in period, 43 adult patients with atopic dermatitis were randomized to treatment with oral vapitadine 60 mg twice daily (n=22) or placebo (n=21) for one week.
Route of Administration:
Oral
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C29578
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ACTIVE MOIETY
SUBSTANCE RECORD