Drug intelligence / Profile preview

carbenoxolone

Development stage
Unknown
Lead developer
AkzoNobel
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

Carbenoxolone is a synthetic derivative of glycyrrhetinic acid, a constituent of licorice root, with a steroid-like structure. It is primarily used for the treatment of peptic ulcers, esophageal and oral ulceration, and inflammation. Carbenoxolone acts by protecting the mucosal barrier from acid-pepsin attack and increasing mucosal mucin production. Its mechanism of action includes potent inhibition of 11β-hydroxysteroid dehydrogenase (11β-HSD), thereby controlling the reversible conversion between inactive cortisone and active cortisol as well as 11-dehydrocorticosterone to corticosterone. This influences endogenous glucocorticoid activity and participates in corticosteroid receptor-mediated anti-inflammatory responses. Additionally, carbenoxolone is recognized as a modestly potent blocker of gap junctions (connexins), which are important for intercellular communication in various tissues[1][5][6][8]. The drug has been used both orally (for gastrointestinal conditions) and topically (for mouth ulcers). Electrolyte imbalance—especially hypokalemia—is a notable side effect when used systemically[4][8].

Brand names
Carbosan
Other names
carbenoxolonaglycyrrhetinic acid derivative
02

Targets

HSD11B2 (11β-HSD2)NMDAR (Glutamate receptor ionotropic, NMDA)HSD11B1 (11-beta-hydroxysteroid dehydrogenase type 1)Connexin (Connexin family)

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