Drug intelligence / Profile preview

cidoxepin

Development stage
Unknown
Lead developer
Elorac
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Topical
01

Overview

Cidoxepin is the (cis or Z) stereoisomer of doxepin, a tricyclic antidepressant. While doxepin is widely used for major depressive disorder, anxiety disorders, chronic urticaria (hives), and insomnia, cidoxepin specifically refers to this single stereoisomer rather than the racemic mixture found in standard doxepin formulations. The mechanism of action involves inhibition of serotonin and norepinephrine reuptake in the central nervous system as well as antihistaminic, anticholinergic, antiadrenergic, and antiserotonergic effects. Cidoxepin has been assigned an International Nonproprietary Name (INN) but is not marketed under any brand name or widely available as a distinct pharmaceutical product[5].

Other names
cis-doxepinZ-doxepincidoxepin hydrochloride
02

Targets

SERT (Sodium-dependent serotonin transporter)HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)NET (Norepinephrine Transporter)ADRA1A (α1A)

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